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Pharmaceutical Formulation - Science topic

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I have herbal extracts obtained by maceration in 80% ethanol that are desired to be evaluated for their wound healing activity using excision and incision wound model on albino rats.
Although the extracts are prepared using the same solvent they have different solubility profile in water (some form clear solution while others results in a homogeneous suspension).
We intend to formulate the extracts into a semisolid dermal preparation using either aqueous cream base or simple ointment base as they are the most frequently used bases with the least intrinsic efficacy.
Is there a suitable method to measure and compare the release of the extracts from the aqueous cream base and the simple ointment base in order to evaluate their suitability.
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Dear Jun,
yes, there are methods.Just read the attached article.
regards
Horst Liebl
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Need to know about the excipients.
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Greetings every one l am asking about the steps of fusion method for the preparation of effervescent granules?
Waterbath was used for heating of citric acid to liberate H2O , then other ingredients were added , no granules were formed . What may be the problem?
Any suggestions ?
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I did forced degradation studies on an ocular eye drops formulation. Is it possible to calculate the stability and shelf life of the formulation using that data (which is in actual the % degradation)?
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Hi
This guideline could be useful as well, ICH Topic Q 1 E Evaluation of Stability Data
Best regards
Tomasz
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I plan to used a Bourne reaction system or similar to study reactive mixing. I wish to vary the viscosity of the system between experiments to understand how the viscosity influences the reactive mixing. This could normally be done using different concentrations of CMC or other additive. However during the Bourne reaction systems a neutralization reaction occurs resulting in change in pH which affects many additives and alters the viscosity.
Does anyone know a compound which can be used to increase the viscosity of an aqueous solution such that the viscosity is stable over a range of pHs?
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Dear Michel, you could employ HPMC as an additive in the reactions for increasing the viscosity of the system, I'm attaching a technical brochure of one of the HPMC brand names where you could find various grades of different molecular weights. In general, HPMC is nonionic and the viscosities of their solutions are stable over a wide range of pH, in my experience pH 2-12 will not affect the solution viscosity, thus there may be a gradual loss of viscosity at higher temperatures or after long periods of standing, especially with high-viscosity solutions.
On the other hand, the hydration time of HPMC will be higher under pH less than 7, so you will have to design your experimental work to obtain the desired viscosity before running the reaction you need to perform.
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Some drugs appear to be more quickly absorbed by the body with smaller particle size while some undergo better sustained release with larger particles. Why?
Is it related to the absorption mechanism (capillary action for smaller particles vs. lymphatic system for larger) by any means?
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As the particle size decreases, Surface area increases , and simultaneously dissolution rate increases. It causes increase in solubility and so more quickly absorbed by the body. As accordingly larger particles have slow dissolution rate and gives sustained release effects.
Intramuscular injections mostly contains insoluble particles in aqueous solvent or soluble particles in non aqueous solvent. Prolonged release also occurs due to other factors like blood supply, drug properties. Larger particles provide maintenance dose.
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Hi
Can anyone suggest me a recent and simple topic on pharmaceutical formulation development for seminar presentation. Regards.
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Doctor @Shafq Al-azzawi
Thank you very much for your reply
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An indicator of a biological state
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Biomarker is the Early biological signal. Actually it is something New or Chang in the protein which act as marker. According to the such protein signal we can design drug molecules .Biomarker is helpful to New drug development.
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Need any reference or information that magnesium stearate will reduce the activitu of sodium stearyl fumarate. Also want to understand the role of lubrication time for sodium stearyl fumarate.
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Magnesium stearate is hydrophobic in nature, over Lubrication leads to create hydrophobic layer, this cause dissolution, Dt, tablet harness issue.
magnesium stearate is not compatible with many API.
Effectiveness of lubricant depend on optimum Concentration, particle size of magnesium stearate.
2% of SSF + 0.5% of magnesium stearate give better results
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I am currently working on a pharmaceutical formulation development and want to know the effect of change of the starting materials and process of a formulation and the process. I want to sort out the data output received from the software and to determine if it is useful for me. Thus if anyone could provide me with the data input and the output from Minitab for any experiment from any field it will be highly appreciated.(Just need to know which of the input parameters are material and which are process).
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interested
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During formulation of syrup , the after taste is feel bitter because of tween 80's bitter taste. How to use tween 80 to avoid that.
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Hey, even if it's probably not that relevant anymore - you could try sucralose as sweetener. Works pretty well!
Regards,
Niklas
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Force feeder wheel speed is very important particularly for those formulations that are very sensitive to over-lubrication. High residence time and speed of force feeder wheel are equally responsible for over-lubrication. On the other hand, low speed of force feeder wheel could cause fill weight variation and there by tablet weight variation. Therefore, force feeder speed needs to be optimized. Is there any equation/concept available to optimize force feeder wheel speed optimization?
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ratio turret 1: fill-o-mat 0.5-0.8 of turret speed
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This is in order to determine the gastrointestinal behavior of microcapsules.
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Can anybody confirm the preparation of SGF with enzymes.
Is it 3.2gms pepsin+2.0gms sodium chloride and 7.0 ml of hydrochloric acid in one litre.( As per usp)
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Particularly for BCS class II drugs such as NSAIDs
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Hello all
I am also trying to make pellets of Famciclovir 250mg. Its an orodispersible formulation in which the pellets should dissolve in Stomach. The total weight of the tablet should not be more than 800mg. Can anyone suggest what are the extrusion aids and binder combinations for this product.
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I am working on tablet dosage form development of amorphous API. My API in tablet is in amorphous form and likely to convert to crystalline form on shelf. I wanted to monitor the fraction of API that might be converting to crystalline form. Tablet weight is 500 mg and contains API 50 mg ie 10% w/w. Other ingredients in tablet includes MCC, Aerosil and Mg Stearate. I am searching for nondestructive technique that enables chracterization of solid form of API in intact tablet. 
Thank you
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To quantify fraction of crystalline conversion, You require to break tablet and need to convert in in powder state. From Time to time, you may take X ray diffraction spectra and find out percentage of drug thats converted into crystalline state.
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Chitosan coated lipid vesicle system for ocular delivery.
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I have prepared a topical mosquito repellent patch by incorporating a volatile compound in it. The volatile compound is supposed to get released in to the environment. To obtain the release of volatile, the content of the volatile compound is determined at each time interval with the help of calibration curve. For example, at 0 hour the content is  "X" and at 1 hour the content is "Y". Apparently the release of volatile compound at 1 hour will be =X-Y.   Am I doing the right way or is there any other procedure to calculate it. Moreover, I do not know the exact procedure to calculate the cumulative % release of volatile. Someone please help.
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Dear Johirul,
I think your procedure is correct when your active matter can be volatile and not other components in ur final formulation....that means if some other components evaporated along ur active one u may consider total amount as ur active n thats why the procedure included some errors in this case....if u hv done enough experiments for constructing ur calibration curve ...I think yes you can do calculation by that...but make sure u hv enough exp. in ur cal. curve n first verify it by some unknown samples..... 
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As per IP titanium dioxide has water soluble substance as a test parameter. It's limit is 0.5% (W/W). What does it indicate if the result is obtained more that 0.5% and what does that lead to in the pharmaceutical formulation?
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Dear Sir. Concerning your issue about the significance of water soluble substance parameter of titanium dioxide in pharmaceutical formulation. Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics. so when you analyze the titanium dioxide in its pharmaceutical formulations you must carry out the water soluble substance parameter. The most frequently encountered problem when preparing drugs in effervescent form is that drugs is a molecule which is insoluble in water and slightly soluble in alcohol. It has been seen that effervescent formulations comprising the active agent drugs having low solubility dissolve slowly when they are put in water during use and some part of the formulation remains without dissolving and therefore a homogeneous solution cannot be obtained. This reduces absorption and bioavailability of drugs and therefore the patient cannot take sufficient active agent required for an efficient treatment. I think the following below link and the attached file may help you in your analysis:
Thanks
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moleculer weight of protein and generation of dendrimer are important for drug formulation, ıts size- zeta potential. which chemical bonds are observed?
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Dedrimer generation is highly considered in case of protein conjugation.  So choose within 2nd to 4th generation dendrimer. If you want to go further conjugate some biopolymer to reduce toxicity. 
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I performed a dissolution test on number of nano formulation that contains my drug with different stabilizers that have different concentrations
but when it came to dissolution test all the drug was released in less than 10 min compared to the raw drug which took 90 min . after that the UV spectrophotometer stops reading  the absorbance , like the drug isn't available in the samples
I changed the volume of the media from 500 to 250
the amount of the formulation to 10, 25, 50 mg
the rotation speed from 100 rpm to 50 rpm
the filtration with  non, 0.45 um, 0.22 um
used both apperatus1 and 2 
used a sinker
nothing seemed to change the result
has anybody faced this problem before ? how can I asses the drug release in this case
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How are you preparing your nanoparticles? Have you consider a change in the crystalline form of the API - this would definitely affect the solubility of the drug, being aligned with the results you mention. 
Other issues, regarding the analytical method itself, like filter compatibility, selectivity of the UV method - were those accounted for also? What dissolution media are you using?
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when comparing comparative dissolution of our product (Cefpodoxime 200 mg F.C.T) with Cefpodoxime Proxetil Tablets (Innovator), and according to USP; at pH 3.0 (Glycine), our product showed 45% after 10 mins, while the innovator showed 100% after 10 mins; in turn, at pH 1.2 (0.1N HCl), our product showed 100% after 10 mins, while the innovator showed 35% after 10 mins., although both are acidic!
Our product contains carmellose calcium, hydroxypropyl cellulose low substituted, sodium lauryl sulphate, magnesium stearate and lactose monohydrate (as much as close to the innovator).
Based on our data collection, Cefpodoxime Proxetil is BCS 4 (low solubility and low permeability) and has high molecular weight.
Any further details upon your request
Could you please help me to investigate this problem?
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Hi Ahmed, I think the issue is the formation of "diffusion layers" enhancing the solubility of your product. these layers are formed due to alkaline nature of your product matrix. so please measure the pH of 1% solution of your product and the innovator one. You will need to change one or more of the excepients beside sodium lauryl sulphate may play important role in that aspect
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I am working on control release of drug by PLGA PEG PLGA copolymer. this polymer is very sticky. I could not dissolve this polymer? please guide me how can i dissolve this polymer well? How can i sterile this polymer for cell culture and invivo? filter is not good 
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This kind the system is really difficult to sterilize. Normally you can not use autoclave sterilization or filtration.
You need to put your material in a open vial inside of the container with alcohol and let for 24 hours. The alcohol will evaporate, and the alcohol vapor will disinfectant everything inside of the container (included the polymer).
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NLCs were prepared by probe sonication technique. Prepation prepared after sonication was found to be clear with no sediments after centrifugation. Organic acid (medium chain length) was chosen as drug. Size of drud loaded NLC was around 30-50nm while that for blank was around 100-200nm.
Also product obtained after lyophization was in a paste form and not solid, is it acceptable?
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Dear Deepinder,
It seems there is some physico-chemical interaction between your drug and the lipid used for preparation of nano-structured lipid carriers.
I think you should study this interaction first through performing some experiments for example DSC, XRD or FTIR  which suits your drug and polymer structures.
The bigger size of your blank NLCs compared to your loaded NLCs  also the unstable freeze-dried product might confirm my assumption.
I totally agree with previous replies offered by other colleges regarding changing the preparation conditions.  
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Hello! I'm doing a literature review regarding injectable formulations and I noticed a convention of using lactic acid within the formulation. The handbook of pharmaceutical excipients lists the purpose of lactic acid as an acidulant. I couldn't find any reference relating to the purpose/rationale behind using acidulants within an injectable formulation. 
Best regards! 
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Dear Jehad,
Lactic acid may be used in injectable formulations for the production of biodegradable polymers and microspheres, such as poly(D-lactic acid), used in drug delivery systems.
for more on this compound, please see page 355 in the attached file.
Hoping this will be helpful,
Rafik
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a Formula of anti-hypertensive drug ,very poor water solubility 
the formula contain sodium hydroxide+meglumin+mannitol
we tried wet granulation by using 70% ethanol dissolved in it sodium hydroxide.
the problem is that the granules remain wet and never dry, even after exposing to heat 50 c in oven for several hour, and if the granules exposed to room temperature and moister it become more soft.
we also suspecting in SODIUM HYDROXIDE ! which is highly liquefied at room temp and moisture.
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Dear Abdeen,
As I understood from your problem, you are trying to increase the solubility of your drug, which has low water solubility. There are some other methods also to prepare the fast dissolving tablets. So, you can try with other methods.
If want to use this particular method only then change the base as other researchers have specified in their suggestions.
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I am wondering for the suitable method for the preparation of microspheres of water soluble drug. I tried for emulsion solvent difussion method (o/w) but I found less drug entrapment. I also tried w/o method (containing aqueous phase and liquid parafin as oil phase and emulsifier) but microspheres were not formed. Please suggest suitable method for the same.
Thanking You all for replying my questions earlier. 
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You're welcome. The first method is called W1/O/W2 and not O1/W/O2
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I work with a 2 similar but structurally different PEGylated polymeric nanoparticles encapsulating a traditional chemotherapeutic drug. The nanoparticles are developed to be administered orally. Preliminary efficacy studies shows good tumor control compared to free drug for both nanoparticle formulation. But size distribution studies of the drug encapsulated nanoparticles shows 2 peaks (suggesting breakdown of nanoparticles at acidic gastric pH), implying drug release as soon as nanoparticles reach stomach for one and significant difference in size (small size about 60 nm at pH 2, 120 nm at pH 7 and 150 nm size at pH 8) with a single peak for the other. What does these results imply? Why is there a size difference with pH.
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1. Extreme acidic pH can induce hydrolysis of some polymers which might affect the size and stability of the nanoparticles.
2. The pH can influence the hydrophobicity of the polymer or drug. (please see the article attached)
3. The pH can affect the charge on the polymer and hence the size. The pKa of the polymer and drug can answer why there is an increase in size when the pH is basic.
More details on the nature of the polymer and drug can be helpful.
Explanation based on Electrostatic Interaction: Assuming it is a cationic polymer,
When using cationic polymers, the charge density of polymers increases in acidic pH. This increase in charge can either increase or decrease the size of the nanoparticles based on the counter-ions (e.g. drug, salt) present in the medium. 
Increase in Size: If there is no counter-ions to neutralize the charge, then the repulsive force between the chains of the polymer can lead to formation of less compact nanoparticles. Hence increase in size in acidic pH.
Decrease in Size: If there drug acts as a counter-ion, then there would be stronger interaction between the drug and polymer, resulting in more compact nanoparticles.
The vice versa would be true for negatively charged polymers.
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facing problems in drug and excipient selection
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SYED MOHIUDDIN SYED IQBAL PATEL, most probably you are working on improving oral bioavaialbility of poor water souble drug. Therefore you sholud check status of surfactants/emulsifires, either they are safe for oral use, most of nonionic surfactants are considered safe for oral use as they are biodegradable. Secondly you sholud select emulsifier of relatively low HLB value for obtaining nanoglobules which will entrap lipophilic drug more efficiently offereing better entrapment efficiency. you can also use cosurfactant alongwith other excepients. Focuus on research articles and reviews  like "solubility enhancement of poorly water soluble drug by nanoemulsification technique". Study articles of good impact factor journal. These articles will also give lot of information, and you will feel easy, cheers
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Any physiological logic behind the mesh size?
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In USP, 10 # size is to pass all type pf granules or particle even big size as of 1.5 to 2 mm size  like sprinkle granules and coated beads etc. Disintegrating apparatus is having some big size mesh to avoid blockage too because it does not effect on DT time.
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I have a precipitated dried sample of hemoglobin and I am using urea/β-ME solution to solublize the precipitated samples of hemoglobin. However, the hemoglobin sample is not solublizing after vortex and soaking it for a while in the urea/β-ME solution. I am trying to find another resolublzing solution that could be strong enough to solublize the Hemoglobin sample in order to run Bradford assay and find out the amount of Hemoglobin in the sample. 
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Dear Abdulkareem Ali Alanezi,
The following link contains a study published in 1936 (80 years ago) by Morrison & Hisey on how to dissolve dry hemoglobin.
Hoping this will be helpful,
Rafik
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Dear Folks, struggling for a good intra-nasal delivery of vaccine although my vaccine is working perfectly by SC and IM routes. Tried with same IN route but is not working. Could you please suggest about the possible excipients or compounding materials to formulate, so it will be staying into the nasal cavity or thereby lungs for a while. It's need to be stayed as well as uptaken by antigen presenting cells, macrophages or other immune cells for better IgA or IgG response. Do I need to think about something to be included in the vaccine that can help or enhance the penetration of intranasal membrane barrier or mucous around the nostril's or nasal cavity? Your advice or suggestions will be highly appreciated. Thanks.
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Hi
This two links I think help you, read carefully
Search Results
Strategies for intranasal delivery of vaccines
www.ncbi.nlm.nih.gov › NCBI › Literature › PubMed Central (PMC)
by M Zaman - ‎2013 - ‎Cited by 22 - ‎Related articles
Jul 12, 2012 - This review describes vaccine formulations designed for mucosal delivery to the nasal-associated lymphoid tissue, via intranasal administration ...
You've visited this page 2 times. Last visit: 6/11/16
Advantages of Intranasal Vaccination and Considerations on Device ...
www.ncbi.nlm.nih.gov › NCBI › Literature › PubMed Central (PMC)
by M Birkhoff - ‎2009 - ‎Cited by 6 - ‎Related articles
Oral and Intramuscular vaccination has been considered till date as the ultimate ways, but nasal route offers advantages such as ease of self administration and ...
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Where can I find the article about cinitapride formulation ,pharmacology of all dosage form ?
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thanks Rohit
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I have developed polymeric patch by incorporating polymers and drugs and characterized by different analytical tools including SEM, DSC and others. The product is undergone accelerated stability testing for six months at 40 degree temperature and 75 relative humidity. The physical property have been evaluated at different time points. The drug content was also dtermined at different time points. But I don't have exact idea to detrmine chemical stability of the product during the course stability testing. Whether thermogravimetric analysis will be sufficient to confirm the chemical stability or is there any other technique to confirm chemical stability of the product. Please explain.
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Dear Johirul Islam
Please go through the ICH guidelines for the stability studies. Please have a look of ICH Q1C guidelines. I also recommend AFM studies for the surface roughness and XRD for any crystal changes in the patches.
with best wishes
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We prepared four liposomal formulations varying in their main phospholipid constituents. These preparation consisted of PEG2000-DSPE (5% mole ratio), Chol (38%) and either of HSPC, DPPC, DMPC and Egg-PC with the respective transition temperature (Tc) of 55, 40, 28, 0 centigrade degrees plus 0.3% DiD fluorescent dye as tracer. Upon treating C26 colon carcinoma Cells in vitro with these liposomes in PBS, the result of the flow cytometry of the washed cells was contrary to what I presumed. After 3 hour incubation of cells with liposomes at 37 centigrade degree, more fluorescent intensity was found HSPE-, DPPC-, DMPC- and Egg-PC-liposome-treated cells, respectively. I thought that the dye was transferred to cells more intensively from Egg-PC-, DMPC-, DPPC-, and HSPC-liposomes, respectively. As the pore defects in these liposomes can lead to the Dye leakage from liposome to cell. Please present your comment.
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It seems to me, you are wrong. This dye – is hydrophobic. So it locates in membrane. Dye can be associate with cell by 2 ways:
 1. by transferring at collision Ls with the cell;
2. at adsorption Ls on cell surface (with possible subsequent internalization).  
I think, in your case second event occurs.
Try to search in PubMed by a masked "liposomes interact with cells"  AND "phase transition temperature", or something similar.
Apparently, solid liposomes adhere to cells better than liquid liposomes.
About term “pore defects in liposomes” I know a little.
In any case, for substance in the membrane, pore in the membrane are irrelevant.
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i have a problem with this drug..
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Not knowing the purpose of your study, it is a little challenging to answer. As carried out in several of the previous answers, solubilizing agents will help to overcome the solubility issue. A very efficient solubilizing agent for fenofibrate, which at the same time is in current use for oral drug formulations is Labrasol (registerd trademark). At 37 degC in our hands fenofibrate is about a thousand times more soluble in 0.6% aqueous solution of Labrasol as compared to buffer. But, in our experience, many drug compounds are not absorbed better than mere aqueous solutions despite the oftenly tremendously increased concentration of drug in solution. See eg DOI 10.1002/jps.23979 or doi:10.1016/j.ejpb.2011.04.010
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I'm doing a project plan for new formula which included new active ingredient. The preparation of active ingredient will be included in this project. I was asking about a validation method for the manufacturing of this newly active ingredient and if there is any health organization make a regulation to organize this process?
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if there is well established system in your country regarding validation protocols than you should follow it other wise follow Validation protocols mentioned by FDA.
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 The shelf-life of a pharmaceutical product is estimated based on the rate of degradation of the API. This rate of degradation is estimated based on the assay results of API during the product stability study.
During conduct of accelerated stability study of a pharmaceutical products, degradants must also be assayed. How the assay results of degradation products will be used for estimation of the shelf-life of a pharmaceutical product?
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The degradation products and impurities assay(s) aren't typically used to estimate the pharmaceutical product shelflife...just the API.  But the degradation and impurities are important in the risk assessment of safety of the API and are assessed over the shelf life of the product.  Most jurisdictions have set some threshold limits for degradants/impurities on the basis that very low levels are unlikely to be harmful.  If your degradants/impurities are well characterised and have known toxicity profiles then an argument can be made to what allowable limits should be (provided the API remains within the prescribed assay limits)..likewise a degradant/impurity could render the pharmaceutical unsaleable if it reaches a toxic level prior to the API falling outside specified limits.
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Dear All
We have combined a phytoconstituent with Active pharmaceutical Ingredient(API) in a tablet. Kindly guide me in assessing the toxicity of the formulation using some model
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Dear Renuka,
The following is the method to be carried out for the assessment of LD 50 (oral acute toxicity) of any chemical compound (pharmaceutical or drug):
DESCRIPTION OF THE METHOD
Selection of animal species
The preferred rodent species is the rat, although other rodent species may be used. Normally females are used (9). This is because literature surveys of conventional LD50 tests show that, although there is little difference in sensitivity between the sexes, in those cases where differences are observed
females are generally slightly more sensitive (11). However if knowledge of the toxicological or toxicokinetic properties of structurally related chemicals indicates that males are likely to be more sensitive, then this sex should be used. When the test is conducted in males adequate justification should be provided.
Healthy young adult animals of commonly used laboratory strains should be employed. Females should be nulliparous and non-pregnant. Each animal, at the commencement of its dosing, should be between 8 and 12 weeks old and its weight should fall in an interval within + 20 % of the mean weight of any previously dosed animals. 
Housing and feeding conditions
The temperature in the experimental animal room should be 22ºC (+ 3ºC). Although the relative humidity should be at least 30% and preferably not exceed 70% other than during room cleaning the aim should be 50-60%. Lighting should be artificial, the sequence being 12 hours light, 12 hours dark. For feeding, conventional laboratory diets may be used with an unlimited supply of drinking water. Animals may be group-caged by dose, but the number of animals per cage must not interfere with clear observations of each animal.
Preparation of animals
The animals are randomly selected, marked to permit individual identification, and kept in their cages for at least 5 days prior to dosing to allow for acclimatisation to the laboratory conditions.
Preparation of doses
In general test substances should be administered in a constant volume over the range of doses to be tested by varying the concentration of the dosing preparation. Where a liquid end product or mixture is to be tested however, the use of the undiluted test substance, ie at a constant concentration, may be more relevant to the subsequent risk assessment of that substance, and is a requirement of some regulatory authorities. In either case, the maximum dose volume for administration must not be exceeded. The maximum volume of liquid that can be administered at one time depends on the size of the test animal. In
rodents, the volume should not normally exceed 1mL/100g of body weight: however in the case of aqueous solutions 2 mL/100g body weight can be considered. With respect to the formulation of the dosing preparation, the use of an aqueous solution/suspension/emulsion is recommended wherever possible, followed in order of preference by a solution/suspension/emulsion in oil (e.g. corn oil) and then possibly solution in other vehicles. For vehicles other than water the toxicological characteristics of the vehicle should be known. Doses must be prepared shortly prior to administration unless the stability of the preparation over the period during which it will be used is known and shown to be acceptable.
For PROCEDURE: Administration of doses, Limit test.  OBSERVATIONS: Body weight , Pathology  DATA AND REPORTING: Data, Test report & LITERATURE
see the following link:
Hoping this will be helpful,
Rafik
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I have tried to separate it using centrifugation at 12000 rpm for 10 min. 
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Tangential Flow Filtration 
You can avoid dilution (which is happening during GFC/GPC) and you can further concentrate the liposomal solution (Ultrafiltration) and you can remove untrapped drug from liposomal solution and buffer exchange with final formulation buffer.
Advantages : 
1. Avoid dilutions and you can further concentrate the liposomal solution
2. Buffer exchange or Dia-filtration : When you select the right MWCO of your TFF membrane ( Cassette / Hollow fiber) , you can retain your desired liposomal solution in retentate side and untrapped drug and other low molecular weight impurities and salt will be removed in diafiltration. You can also use and customize dia-filtration buffer wisely.
Please write me on ymk108@yahoo.com if you need further support.
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we are working on niosomal formulation of hydrophobic drug. Upon centrifugation, the drug precipitated out. Give a suitable(feasible) method of purification.
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Dear Madam,
Mainly three method used for the measurement of encapsulation efficiency:
1. Dialysis
The aqueous niosomal dispersion is dialyzed in a dialysis tubing against phosphate buffer or normal saline or glucose solution.
2. Gel Filtration
The unentrapped drug is removed by gel filtration of niosomal dispersion through a Sephadex‐G‐ 50 column and elution with phosphate buffered saline or normal saline.
3. Centrifugation
The niosomal suspension is centrifuged and the supernatant is separated. The pellet is washed and then resuspended to obtain a niosomal suspension free from unentrapped drug.
For further reference, below article may be useful you:
Niosomes: Novel sustained release nonionic stable vesicular systems — An overview
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What are various types of mechanical characterization techniques for pharmaceutical dosage forms?
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Dear Raja,
We can perform the following mechanical characterization techniques for tablets:
Hardness
Friability
Thickness after compression
Regards,
Abhishek
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currently i am working with cyanocobalamin and i need help for literature about cyanocobalamin vit B12 if any one have literature about this please send me
thank you
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Dear Jayesh,
The following review covers the answer to your question:
Photo, thermal and chemical degradation of riboflavin
Muhammad Ali Sheraz*§, Sadia Hafeez Kazi, Sofia Ahmed, Zubair Anwar
and Iqbal Ahmad
Beilstein J. Org. Chem. 2014, 10, 1999–2012.
doi:10.3762/bjoc.10.208
Abstract
Riboflavin (RF), also known as vitamin B2, belongs to the class of water-soluble vitamins and is widely present in a variety of food products. It is sensitive to light and high temperature, and therefore, needs a consideration of these factors for its stability in food products and pharmaceutical preparations. A number of other factors have also been identified that affect the stability of RF. These factors include radiation source, its intensity and wavelength, pH, presence of oxygen, buffer concentration and ionic strength, solvent polarity and viscosity, and use of stabilizers and complexing agents. A detailed review of the literature in this field has been made and all those factors that affect the photo, thermal and chemical degradation of RF have been discussed. RF undergoes degradation through several mechanisms and an understanding of the mode of photo- and thermal degradation of RF may help in the stabilization of the vitamin. A general scheme for the photodegradation of RF is presented.
To view the full review article, please see attached file.
Hoping this will be helpful,
Rafik
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Hi is there any ingredient or design which can improve the magnesium absorption in the body. Generally only 50% of magnesium is absorbed into the body and remaining is excreted before it gets absorbed. 
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Need More Magnesium? 10 Signs to Watch For
Symptoms of poor magnesium intake can include muscle cramps, facial tics, poor sleep, and chronic pain. It pays to ensure that you get adequate magnesium before signs of deficiency occur.
But how can you know whether you’re getting enough?
According to population studies of average magnesium intake, there’s a good chance that you’re not.
Less than 30% of U.S. adults consume the Recommended Daily Allowance (RDA) of magnesium. And nearly 20% get only half of the magnesium they need daily to remain healthy.
DO I GET ENOUGH MAGNESIUM?
One method of assessing your magnesium status is to simply contact your health care provider and request detailed magnesium testing. Yet magnesium assessment is typically done using blood serum testing, and these tests can be misleading. Only 1% of magnesium in the body is actually found in blood, and only .3% is found in blood serum, so clinical blood serum testing may not successfully identify magnesium deficiency.
What to do?
Fortunately, it’s possible to get a sense of where your intake may lie simply by asking yourself a few questions about your lifestyle, and watching for certain signs and signals of low magnesium levels.
Learn how to read your signs below, and find out what you can do to ensure magnesium balance and good health. If you answer yes to any of the following questions, you may be at risk for low magnesium intake.
1. Do you drink carbonated beverages on a regular basis?
Most dark colored sodas contain phosphates. These substances actually bind with magnesium inside the digestive tract, rendering it unavailable to the body. So even if you are eating a balanced diet, by drinking soda with your meals you are flushing magnesium out of your system.4 5 6
The average consumption of carbonated beverages today is more than ten times what it was in 1940.7This skyrocketing increase is responsible for both reduced magnesium and calcium availability in the body.8 9
2. Do you regularly eat pastries, cakes, desserts, candies or other sweet foods?
Refined sugar is not only a zero magnesium product but it also causes the body to excrete magnesium through the kidneys. The process of producing refined sugar from sugar cane removes molasses, stripping the magnesium content entirely.
And sugar does not simply serve to reduce magnesium levels. Sweet foods are known by nutritionists as “anti-nutrients”. Anti-nutrients like sweets are foods that replace whole nutritious foods in the diet, yet actually consume nutrients when digested, resulting in a net loss. Because all foods require vitamins and minerals to be consumed in order to power the process of digestion, it’s important to choose foods that “put back” vital nutrients, and then some.
The more sweet foods and processed baked goods you have in your diet, the more likely you are deficient in magnesium and other vital nutrients.
3. Do you experience a lot of stress in your life, or have you recently had a major medical procedure such as surgery?
Both physical and emotional stress can be a cause of magnesium deficiency.
Stress can be a cause of magnesium deficiency, and a lack of magnesium tends to magnify the stress reaction, worsening the problem. In studies, adrenaline and cortisol, byproducts of the “fight or flight” reaction associated with stress and anxiety, were associated with decreased magnesium.4
Because stressful conditions require more magnesium use by the body, all such conditions may lead to deficiency, including both psychological and physical forms of stress such as surgery, burns, and chronic disease.
4. Do you drink coffee, tea, or other caffeinated drinks daily?
Magnesium levels are controlled in the body in large part by the kidneys, which filter and excrete excess magnesium and other minerals. But caffeine causes the kidneys to release extra magnesium regardless of body status.
If you drink caffeinated beverages such as coffee, tea and soda regularly, your risk for magnesium deficiency is increased.
5. Do you take a diuretic, heart medication, asthma medication, birth control pills or estrogen replacement therapy?
The effects of certain drugs have been shown to reduce magnesium levels in the body by increasing magnesium loss through excretion by the kidneys.
See also:
For a complete list of the specific drugs which can affect magnesium levels, read our article, Causes of a Lack of Magnesium.
6. Do you drink more than seven alcoholic beverages per week?
The effect of alcohol on magnesium levels is similar to the effect of diuretics: it lowers magnesium available to the cells by increasing the excretion of magnesium by the kidneys. In studies, clinical magnesium deficiency was found in 30% of alcoholics.10
Increased alcohol intake also contributes to decreased efficiency of the digestive system, as well as Vitamin D deficiency, both of which can contribute to low magnesium levels.11
7. Do you take calcium supplements without magnesium or calcium supplements with magnesium in less than a 1:1 ratio?
Studies have shown that when magnesium intake is low, calcium supplementation may reduce magnesium absorption and retention.12 13 14 And, whereas calcium supplementation can have negative effects on magnesium levels, magnesium supplementation actually improves the body’s use of calcium.7
Though many reports suggest taking calcium to magnesium in a 2:1 ratio, this figure is largely arbitrary. The ideal ratio for any individual will vary depending on current conditions as well as risk factors for deficiency.
However, several researchers now support a 1:1 calcium to magnesium ratio for improved bone support and reduced risk of disease. This is due not only to the increased evidence pointing to widespread magnesium deficiency, but also concerns over the risk of arterial calcification when low magnesium stores are coupled with high calcium intake.
According to noted magnesium researcher Mildred Seelig:
The body tends to retain calcium when in a magnesium-deficient state. Extra calcium intake at such a time could cause an abnormal rise of calcium levels inside the cells, including the cells of the heart and blood vessels… Given the delicate balance necessary between calcium and magnesium in the cells, it is best to be sure magnesium is adequate if you are taking calcium supplements.”8
8. Do you experience any of the following:
Anxiety?
Times of hyperactivity?
Difficulty getting to sleep?
Difficulty staying asleep?
The above symptoms may be neurological signs of magnesium deficiency. Adequate magnesium is necessary for nerve conduction and is also associated with electrolyte imbalances that affect the nervous system. Low magnesium is also associated with personality changes and sometimes depression.
Read more:
For a complete list of the signs of magnesium deficiency, read our article, Symptoms of Low Magnesium.
9. Do you experience any of the following:
Painful muscle spasms?
Muscle cramping?
Fibromyalgia?
Facial tics?
Eye twitches, or involuntary eye movements?
Neuromuscular symptoms such as these are among the classic signs of a potential magnesium deficit.
Without magnesium, our muscles would be in a constant state of contraction.
Magnesium is a required element of muscle relaxation, and without it our muscles would be in a constant state of contraction. Calcium, on the other hand, signals muscles to contract. As noted in the book The Magnesium Factor, the two minerals are “two sides of a physiological coin; they have actions that oppose one another, yet they function as a team.”8
Chvostek’s Sign and Trousseau’s Sign are both clinical tests for involuntary muscle movements, and both may indicate either calcium or magnesium deficiency, or both. In fact, magnesium deficiency may actually appear as calcium deficiency in testing, and one of the first recommendations upon receiving low calcium test results is magnesium supplementation.
Read more:
For a complete list of the conditions associated with magnesium deficiency, read our article,Symptoms of Low Magnesium.
To learn more about the role of magnesium in muscle function, see How Magnesium Functions in the Body.
10. Did you answer yes to any of the above questions and are also age 55 or older?
Older adults are particularly vulnerable to low magnesium status. It has been shown that aging, stress and disease all contribute to increasing magnesium needs, yet most older adults actually take in less magnesium from food sources than when they were younger.
In addition, magnesium metabolism may be less efficient as we grow older, as changes the GI tract and kidneys contribute to older adults absorbing less and retaining less magnesium.15
If you are above 55 and also showing lifestyle signs or symptoms related to low magnesium, it’s particularly important that you work to improve your magnesium intake. When body stores of magnesium run low, risks of overt hypomagnesaemia (magnesium deficiency) increase significantly.
HOW CAN YOU KNOW FOR CERTAIN IF YOU HAVE A DEFICIENCY?
Magnesium’s impact is so crucial and far reaching that symptoms of its absence reverberate throughout the body’s systems. This makes signs of its absence hard to pin down with absolute precision, even for cutting edge researchers.  Doctors Pilar Aranda and Elena Planells noted this difficulty in their report at the International Magnesium Symposium of 2007:
The clinical manifestations of magnesium deficiency are difficult to define because depletion of this cation is associated with considerable abnormalities in the metabolism of many elements and enzymes. If prolonged, insufficient magnesium intake may be responsible for symptoms attributed to other causes, or whose causes are unknown.”
Among researchers, magnesium deficiency is known as the silent epidemic of our times, and it is widely acknowledged that definitive testing for deficiency remains elusive. Judy Driskell, Professor, Nutrition and Health Sciences at the University of Nebraska, refers to this “invisible deficiency” as chronic latent magnesium deficiency, and explains:
Normal serum and plasma magnesium concentrations have been found in individuals with low magnesium in [red blood cells] and tissues. Yet efforts to find an indicator of subclinical magnesium status have not yielded a cost-effective one that has been well validated.”16
Yet while the identification of magnesium deficiency may be unclear, its importance is undeniable.
Magnesium activates over 300 enzyme reactions in the body, translating to thousands of biochemical reactions happening on a constant basis daily. Magnesium is crucial to nerve transmission, muscle contraction, blood coagulation, energy production, nutrient metabolism and bone and cell formation.
Considering these varied and all-encompassing effects, not to mention the cascading effect magnesium levels have on other important minerals such as calcium and potassium, one thing is clear – long term low magnesium intake is something to be avoided.
WHAT CAN YOU DO TO INCREASE MAGNESIUM INTAKE?
The Magnesium Miracle, by Carolyn Dean, M.D. N.D.
The longer your intake remains low, the more likelihood your bodily stores will be diminished, leaving you exposed to some of the more troubling side effects of long term deficiency. According to Dr. Carolyn Dean, M.D., N.D., and expert on magnesium therapy, adequate magnesium can improve heart health, prevent stroke and obesity, and improve mood and memory.
If you answered no to all of the above questions, you may be able to rely on high food sources of magnesium, like those described in our article onMagnesium in the Diet.
Yet for many people, especially those with diseases and symptoms associated with low magnesium, active magnesium supplementation may be a crucial element of returning to good health.
In her book, The Magnesium Miracle, Dr. Dean notes that achieving adequate magnesium through foods is notoriously difficult, stating:
I’m convinced that to get enough magnesium today, you need to take supplements.”4
Transdermal magnesium does not have the side effects of oral supplements.
One of the most effective ways to improve your magnesium levels is to combine a healthy diet with transdermal magnesium.
Many of the factors which contribute to low magnesiumstores are caused by inefficiencies of the GI tract. By delivering magnesium through the skin directly to the cells,topical magnesium products bypass many of the problems associated with low magnesium absorption.
In older adults, reduced gastric acid levels in the digestive system may be a factor in reduced mineral availability. Hydrochloric acid supplements may be combined with magnesium to combat this dilemma; however a simpler and less expensive option is the use of magnesium chloride supplements. Magnesium chloride has been proven to have a high bioavailability, while simultaneously providing the chloride necessary for healthy digestion and vitamin and mineral absorption.
Magnesium researcher Mildred Seelig has called magnesium “the silent guardian of our hearts and arteries” and “necessary for life”. And Dr. Carolyn Dean calls it “the missing link to total health”.
If you haven’t heard much about magnesium and its importance to good health, now is the time to learn. And if it’s something you’ve always meant to look into, now is the time to take action!
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I've been trying to develop Metformin 500 mg SR + Sitagliptin 50 mg IR bilayer tablets but the assay of sitagliptin drops by almost 10% in 1 month accelerated stability. Metformin is quite stable but the problem is only with the sitagliptin layer. Please give your valuable suggestions.
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 Dear Dhakshna,
Thanks a lot for your answer. I've developed this product now which is stable.
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Many works have been reported so far on various drugs belonging to many categories like anihypetensives, anti-lipidemia, etc etc. But i want to know if any of the drugs have been marketed?
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THANK YOU SIR.
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Dear All,
We have tried some essential oil in some of our solid dosage forms as a natural ingredient. But on analysis, content of essential oil is decreasing significantly.
We have adsorbed essential oil onto Sio2 then added to the compression mix to formulate tablets.
Open for Suggestions please?
Thanks for your time.
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Many essential oils are volatile even at room temperatures. Thermal degradation and loss of low boiling components in known in several essential oils. You may contact Essential Oil Association of India with a large number of manufacturers for sharing their practical experiences.
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We want to improve bioavailability of plant based lipophilic compound. Please let me know various pharmacological mechanism to improve kinetics.
Regards,
Shankar
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Micro-encapsulation technique we use.
Thanks,
Shankar
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The objective is a composition for a continuous few days i.v. infusion for short term tox studies in rat. The formulation should be well tolerated but still able to solubilize 5-20 mg/ml of the drug, which is a poorly water soluble weak base with intrinsic solubility of 0.01mg/ml, pKa ~4, and logP ~3. The vehicle or components should not have any major effects on hemodynamics of the rat.
Several standard formulation options based on e.g. co-solvents, surface active agents, and lipid systems have already been tested but  a well-functioning and tolerated formulation has not been achieved so far. Non-conventional lipid vehicles would be fine also if there’s any prior experience on suitability for tox use.
Any insight and ideas related to composition, formulation technology, infusion system, devices etc. will be highly appreciated. Thank You!
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oil in water emulsion is the most likely approach. The poorly soluble drug can be dissolved in the oil phase.
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we are developing a formula for drug with very poor solubility, we are using MCC and lactose as diluent sodium starch glycolate as super disintegrant,sodium lauryl sulphate as solubilizing agent and magnesium stearate as lubricant.
the dose is low so we are using wet granulation as preparation technique,
dissolution results are always come very low, we are using official dissolution method from USP:
media : 0.01 HCL, 900 ml
apparatus 2 : 50 RPM
time : 30 min
is there any method to enhance solubility of this product ??
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Mohammed, micronizing a drug does no increase its solubility. It only increase it dissolution kinetic (cd Noyes and Whitney equation). Solubility is only enhance when the size gets lower than 100 nm which is quite hard to get.
A simple method to improve the solubility is to form the amorphous form or use lipid-based formulations. I guess that lipid based formulation would bring you a wide latitude to find out the right composition (cf articles from Pouton, Charman and Porter from Monash university).
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Paracetamol suppositories made with PEG 4000 and PEG 6000 as suppository bases undergo dissolution test. After 45 minutes, both batches have mean % of drug release that is higher than 100%.
PEG 4000- 150% and PEG 6000- 120%
Why does the cumulative drug release exceed 100%? Is there error during measuring of absorbance or is it some form of degradation or hydrolysis of the medicine during manufacture/storage?
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Dear Ahmed,
Polymorphs are solid state-of-matter crystal forms? But, for an assay you're dealing with a solution. So the specific absorbance (in solution) will be identical, no matter which polymorph dissolved. You may be thinking of mutorotation, but the assay is by absorbance, not optical rotation.
Rachel, paracetamol is stable in the body until metabolized, which processes usually don't involve attack at the phenol group. So it's likely to be comparably stable once in solution in a dissolution test. As to the possible attack by PEG impurities, you might see http://www.spectra-analysis.com/documents/AppNote016Polyethyleneglycol.pdf , with the caveat that the sample had been "vigorously air oxidized" (hot?). Consider that PEG is used in many preparations, and that it may block chemical carcinogenesis, both of which wouldn't be practical if it generated large amounts of peroxides. I do note that sonication (to disperse or dissolve solids in a solution or semisolid) may degrade PEG, see https://en.wikipedia.org/wiki/Polyethylene_glycol . So don't do that!
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How do we perform optical resolution of Orphenadrine drug?
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Dear Rami,
The following paper covers the answer to your question:
Arzneimittelforschung. 1969 Dec;19(12):2010-2.
The resolution in optical isomers of orphenadrine, 4-methyldiphenhydramine and their N-demethyl derivatives.
van der Stelt C, Heus WJ, Nauta WT.
PMID: 5395894 [PubMed - indexed for MEDLINE]
Sorry I do not have an electronic copy of the paper but you can get from your library or other sources.
Hoping this will be helpful,
Rafik
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I am looking for development of topical formulation, including preformulation and stability studies. Is there any GLP certified lab which can perform the development and clinical manufacturing. 
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links provides GLP; may be useful
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Hello Everyone,
We are facing disintegration issue in one of our product development. Its an ODT (orally disintegrating tablets) dosage form with a target DT of less than 30 sec. We are not able to achieve a DT of 30 sec with a hardness of 30 N with wet granulation. If we lessen the hardness DT would be around 25 sec but that's not preferable as the hardness is very low and chances of friability will increase. 
Though the solution seems easy by using disintegrant like Croscarmellose and Crospovidone but we already tried with many of them .As the extracts are very hygroscopic tablets are not able to disintegrate within 30 sec. 
With MCC its giving good results but the mouth feel is unpleasant.
Any suggestions?
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Preferably use silicifed microcrystalline cellulose or Avicel pH 112 with syloid or Aerosil 200 according to the target active density. Regarding the disintegrants, AcDisol with Crospovidone Xl 10 upto 20% of tablet weight as previously mentioned  Pearlitol Flash Mannitol
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i need a review article that gather all possible excipients involved in solid dosage form  manufacturing?
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you can get some of relevant information focusing on granulation & capsule excipients on 
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if so how it is prevented? 
thanks in advance 
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For sure you have to proceed for an efficient phase separation method with a good control of temperature (centrifuge).
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Placebo pills are needed to form a matrix for pharmaceutical formulations. If my company does not have budget for it, is it possible to use sugar-free pills and/or panadol tablets to compensate for its use? Can they meet the minimum requirement? In my humble knowledge, they have some although not all of the characteristics of the placebo pills.
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Hi Kar-Weng Chan,
I would not recommend you to do that so. Herein, I give you an explanation.
As Vikram Shenoy mentioned, you can use panadol and sugar free matrices only you prove, it is similar excepients both in the type and amount of excepients. Because excepient can affect on drug release (in case of drug dissolution) or trap the active ingredient within the matrix. This is the example "Allwood MC. The adsorption of esters of p-hydroxybenzoic acid by magnesium trisilicate. Int J Pharm 1982; 11: 101–107." 
For pharmaceutical excepients, we normally use "Handbook of Pharmaceutical excepients 6th ed" as a bible of our study. I hope it is very useful. In case of magnesium stearate, please see attachment in page 405, item "18 comment". It states the problem of magnesium stearate used, in amount used and even mixing time can affect to drug release. It also forms physical interaction with hydrophobic drug. For further information, please look at specific reference. (I send you the file by RG message.)
This is just an example of excepient affected on drug release (both in dissolution or drug extraction). Now I also work on %recovery. I still have a problem. Even I used drug finish product and spiked known amount of standard. I extracted with 50%methanol, 100%methanol and also acetonitrile. The percent recovery of 1 compound is about 93-95%, while the rest is around 100%. Fortunately, the %recovery is very precise.
From your last question, the used of panadol or sugar-free tablets, we cannot ensure that there is no excepient effect on drug extraction. If I were reviewer (for publication) or drug registration agency (drug registration process), I would question on this. I understand your situation. Is it possible to get information regarding the excepients used in buprenorphine tablet? What I know in Germany, they have so called "Red book" that you can find it (only name of excepients not in amount). I also found some article that they just added the most common excepient in different amount based on normal range in formulation. Then they extracted and compared (This increases a lot of work). Is it possible to ask for a gift of placebo from the manufacturer (sometime it works)?
This is what I know and try to answer with solid references (as we, scientists, have to do). :-)
I hope I answer your question. 
Good luck!
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Regarding official monographs; every single API can be analyzed by titration methods. Is it possible to analyze each API alone with its own official method with the presence of the other APIs or this may lead to error in the analysis.
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I agree with you Subrata, Thank you very much. But kindly suggest the type of masking agent that can be used for the complexometric titration.
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Retinyl palmitate is a pre-formed version of Vitamin A, is a synthetic supplement available in dry or oily form. It can be taken orally or by injection to treat Vitamin A deficiency. It will get converted to an alcohol in the small intestine when ingested. Overdosing preformed Vitamin A forms such as retinyl palmitate leads to adverse physiological reactions known as: hypervitaminosis A, which can be harmful to liver, bones and skin, causing weakness and brittleness, even leading to fatigue and vomiting.
Can anybody have reference paper or official document on dose of vitamin A palmitate and its effect?
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In 2005 the UK Scientific Advisory Committee on Nutrition published the "SACN Review of Dietary Advice on Vitamin A" . This might contain some information which would help you and enable you to follow more recent reports. In contrast to India where it A deficiency is widespread, the interest in the UK was excessive exposure to vitamin A. I hope that the SACN report will be of some help, it is available online; just google Vitamin A and SACN.
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How Can I calculate stability constant between drugs and cyclodextrin.
 if the stability constant have a value of negative sign what is the reason for this?
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Through Phase solubility studies as per the method reported by Higuchi and Connors (1965).
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Hi everyone,
I'm working on the SB334867 (Cat. No. 1960; orexin 1 receptor antagonist). We tried to dissolve it with pure DMSO, but the DMSO is harmful to neurons. Could you please tell me a better method to dissolve it ? Thank you~
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You could perform an experimental design (mix design) using concentration of DMSO, HP-beta-cyclodextrin and a third vehicle (maybe isotonic NaCl) as variables, and solubility of SB 334867 as the response, trying to minimise the amount of DMSO. An useful program you can use to define and analyse the DOE is Design Expert, or any statistical program you have available. Hope you find this useful.
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is that tablet which is produce with B type punch have better dissolution compare to tablet which is produce with D type punch?
how about tablet porosity between the type of tooling (type B and type D)?
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2. Mostly the type of tooling (BB, B or D) is selected to improve the productivity during commercial manufacturing. For ex the productivity will be 20 to 25% more in B tooling compared to D, assuming same speed & diameter of turret of machine as number of stations will be higher
2. The maximum dimention possible in B and D are 19 and 25 mm respectively
3. Hardness which can be achieved might be more in case of D tooling due to larger dual time. It can lead to slower dissolution if dissolution is hardness dependent
4. you can ask specific question if you are facing any problem
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is there any method to complex natural drugs with anionic or cationic liposomes
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Provide an example of bioreducible liposomes.
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Please help me with the detail method for the dissolution of clotrimazole extended release vaginal tablets.
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Dear Pierre,
Thanks a lot for the method. I'll try out this method soon.
Regards,
Abhishek
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Dear Researchers,
We developed one product with wet granulation process and the IPA is used in binder preparation, so after the wet granulation, we were dried the wet mass in FBD but we observed the case hardning as well as even after dried the granules i.e. upto the LOD 1.5 % .. and moreover after that we kept the milling step, and also after that the two steps are ahead i.e. compression and followed by coating but still after final formulation we got the IPA more than 5000 PPM..
So could you suggest any solution for the drying like humidity or dew point control...
Awaited for your responses....
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Yes this exercise we did at drying stage where RH we control ..
Initially keep the drying temp as low as possible with high fuidization .....
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Is there any effect of temperature generation during compression?
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Sounds like a capping problem. This can occur when compressing particles which are plate like in shape. Can also be caused by too high compression forces.
If permitted you could reduce particle size of the drug, or increase amount of binder.
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Dear sir,
We are in to manufacturing of pharmaceutical oral dosage forms. We develop thin oral medicated films of size 32 x 25 mm of 50 micron thickness. Our idea is to fill such 30 films in to small cassettes. A cassette is made with food grade HDPE material ( silica desiccant preferably) with self locking mechanism.
For this, we have two requirements.
1. Food grade HDPE cassettes (silica desiccant preferably).
2. A machine which fill the films into cassettes.
I request you to look in to this requirement and give us you possibilities.
Waiting for the reply.
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Thanks a lots Sandeepji.
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siRNA delivery in Bilosomes
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It has been used for oral vaccine delivery but not encapsulated siRNA
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I would appreciate some advice on how to encapsulate an amphiphilic small molecule into a liposome.
My small molecule is amphiphilic – it has a hydrophobic aromatic core, to which two alkyl linkers are attached. These linkers have a basic nitrogen atom each, so these constitute hydrophilic groups. The salts of this small molecule are water soluble, while the neutral form is poorly soluble in virtually everything (except acids and DMSO).
Unfortunately, the only lipids I have on disposal to prepare the liposomes are standard, 99% pure Sigma Aldrich egg yolk phosphatidylcholine and cholesterol. I have tried the standard approach: made a thin film out of the lipids + compound salt, suspended the film in water and sonicated the suspension. I extruded through 0.2 µm filters, precipitated the liposomes via centrifugation and had only about 9% encapsulation (which is to be expected, since the compound salt is water soluble, only 9% could statistically be “captured” by the forming liposome, the rest remained in solution, out of the liposome). How can I increase this yield? On the other side, when I took the neutral form, which is poorly water soluble, I had a higher encapsulation % (which is to be expected) but the precipitate after centrifugation could not be resuspended in water, and had a very high compound to lipids ratio (meaning these are not “good” liposomes).
The additional problem is that I have a really small amount of both my compound and the pure egg yolk phosphatidylcholine, so I can’t afford “throwing them away” on too many different experimental approaches. Also, this is a completely new area of work for me, and I have no experience in liposome preparation. Any piece of advice would be helpful. Thank you!
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For water-soluble drugs which do not interact with the bilayer, the encapsulation efficiency is proportional to the aqueous volume enclosed by the vesicles which itself depends on the morphology/lamellarity of vesicles and phospholipid concentration. The encapsulation capacity (not efficiency) can be improved by using per example higher ratio. Additional strategies have been also described but I never tried: freeze/thawing in presence of TEAP or freeze-drying followed rehydration.
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I have dissolved limonoid aglycone in 100 % DMSO at a concentration 10mg/ml. It completely dissolved. But when i add the stock to serum free media [ 10-200ug/ml] for treating cancer cells. Media becomes turbid and when viewed under microscope it looks like crystal clusters. No toxicity is seen even in higher concentration.
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Try to lower the conectration in starting solution, that means that you have highly insoluble compound. :(  Try Tween, or Ethanol...
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Currently we dissolve it in minimal DMSO then add cremophore-EL. This mixture is then diluted in buffer immediately before injecting. It’s a struggle to keep the compound in solution it readily precipitates out. Any suggestions would be appreciated.
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Dear David,
you could try a polymer we are working with and could prepare extremely highly loaded and stable formulations of a number of drugs which otherwise crystallize easily, for example Paclitaxel. 
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I have used PLGA:DCC:NHS in molar ratio of 1:10:10. after 12 hrs of reaction no precipitate of dicyclohexyl urea is seen. The reaction was carried out at room temp. Do I have to change the reaction condition in order to cause precipitation.
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Dear Vaseem,
So you have a Plolymer with a terminal functional carboxyl group (PLGA-COOH) and you want to activate its COOH with DCC/NHS in order to conjugate PLGA and an Amine containing moiety together. Dicyclohexyl urea is a possible byproduct of the reaction; Right??
1. But how are U sure that it certainly forms during the reaction?
2. And why do you insist on removing it absolutely via precipitation?! You can simply remove all the byproduct and excess DCC-NHS through filtration or dialysis.
Can you clearly explain the reason why U wanna do this??
Best of luck 
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I am currently working on PLGA nanoparticles and encapsulation of hydrophobic drug. What (among single emulsion, multiple emulsion and nanoprecipitation)is the best method  for enhanced encapsulation of hydrophobic  drug ?
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My opinion is that there is no such thing as "suitable" method. All methods have their pros and cons, and have to be tried out IF you have enough material to work with.
Having said that, my preference goes to the nanopreciptation method, but dropping water into the mixture of PLGA and drug in organic solvent. Even better if you first evaporate the organic solvent from the mixture and then re-dissolve it. If you can form any particles, they will have a relatively high encapsulation efficiency.
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I am interesting what can be adjunct for drugs for animals or for humans that would be enhance its effect, f.e. would help to better suck substance from intestine, if f.e. the drug is against worms in pigs or cow or against bacterial infection etc.
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Permeability enhancers may work.
We are working on the intestinal permeability enhancement of drugs in humans using colloidal carriers mostly polymeric nanoparticles. This is costly but yes it may work in animals too.
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I have my amount of drug in mg/mL and amt of drug+nanocapsule in mg/mL as I weighed the mass of my nanoparticles after freeze drying their solution forms.
I followed the equation Loading ratio= amt of drug (mg/ 1 mL)/amt of drug+nanocapsule (mg/1 mL).
However, I was asked to multiply this ratio by 1000 so that I can have a loading content of µg/mL.
How does this work? I thought the ratio would give units of mg/mg. But why does multiplying by 1000 give units of µg/mL? 
(It was mentioned that this concentration unit was needed when testing samples in vivo.)
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Hi. Unless I am missing something it is just a unit conversion...  1mg = 1000 ug. It is just a unit conversion.
Good luck!
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I would like to use aspartame in an orally disintegrating tablet. In literature there is lot of variation for the %age of aspartame so I would like to know the safe limit which I can use.
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The European Food Safety Authority (EFSA) recommends 40 milligrams aspartame per kilogram of body weight. Since aspartame is approximately 200 times sweeter than the sugar (sucrose), then its use will involve very small amounts & research has not found harmful side effects upon using it except when taken together with some schizophrenia medications.
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I want to micronize curcumin,and I would like to prove that after micronization the curcumin has already activity as a drug. How can I do? and what instrument can I use?
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1.micronization do by ball mill 2.pass through 100 mesh sieve
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Dear collagues. We planned a new study to evaluate effects of resveratrol ana CAPE on pregnant rats in endocrine disorder. However, because of low water solubility we cannot transffered all the LD50 dosage. could you answer please which solution is more preferrable for solving Resveratrol and also CAPE?
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Why would you be dosing them at LD50 anyway? It's a splendid way to induce liver CP450 detox routes that aren't biochemically relevant (and may be misleading, see controversy over safrole for example). But if you must, give by gavage in oil suspension (but see http://www.procedureswithcare.org.uk/oral-gavage-in-the-rat/ ), since most organic solvents for polyphenolics are toxic. You could also try topical DMSO solution -- e.g. under an occlusive patch on bare skin -- but the DMSO will significantly dampen your inflammatory pathways on its own, and your dosage would be uncertain (without confirmatory blood tests).