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Formulation Development of Pharmaceuticals - Science topic

Formulation development of various dosage forms
Questions related to Formulation Development of Pharmaceuticals
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I am looking for a plain/empty gel system, which we can directly buy and load the drug for the purpose of transdermal delivery. Your kind help will be appreciated.
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generally, based on the nature of the drug we have to select the polymers to prepare any formulation .
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For a drug that is practically insoluble in water and sparingly soluble in ethanol and DMSO, how may each of the following factors be manipulated to maximize the drug exposure when applied into a sustained-release injection (parenteral or IV) formulation?
  • particle size distribution
  • API crystal form (anhydrous/monohydrate) -> any effect?
  • suspension solution (aqueous/oil)
  • route of administration (SC/IV/IM)
  • metabolizing enzyme induction/inhibition (CYP/UGT)
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There's probably no one recipe for all drugs. I think it's pretty consistent that an amorphous form, if you can obtain it, is more rapidly soluble, and that smaller particles dissolve more quickly (due to the larger surface area), but the other factors will vary from one drug to the next. You don't specify if you're relying on low (slow) solubility for the sustained release effect.
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Some inhibitors act on protein active sites and inhibit protein action. Does anyone know of any software or database which provide the list of all inhibitors including biological, chemical and physical inhibitors?
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I was making a dilution and there was a mention of using 'concentrated water'.
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Anyone considering "concentrated water" should return to basic chemistry and physics! You can have higher concentrations of soluble and insoluble compounds in water but the water is the solvent. Many compounds can be concentrated in water; but, the water cannot be concentrated without combining the water with another compound.
The only thing that causes a change in the number of molecules per unit volume is the density associated with the temperature of the water and the physical form of the water.
Sounds like a ridiculous
marketing claim that is not supported by good science!
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With acceptable hardness and friability.
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Dear sir,
for paracetamol tablet you need 2.5-3.5% moisture in granules and optimized granules fine ratio. if higher % of fines present in blend, tablet will fail in friability test.
in paracetamol tablets optimal LOD is 2.5-3.5%, when we take batch with starch and pvp k-30 paste. if you take gelatin and starch as a binder then optimal LOD will change from 2-3%.
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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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Hi,
I was thinking of why should one prefer lyophilization over dry powder filling. All the APIs are manufactured in solid form and solid excipients like mannitol, trehalose, etc. Can the API and solid excipients not be filled into a vial, with carrier solvent and liquid excipients in another container? Reconstitution can be performed at the point of requirement, right?
PS: I am new to this area, so please apologise if the question sounds stupid!
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Liophilization is the choice process when a) the powder has flowability problems or adhesive properties that clog the dosage screw b) when the dose is critical (little difference between the toxic dose and the therapeutical dose).
The a) case is obvious, an aqueous liquid usually has little - if any - flowability problem and a solution overcomes these; the b) case, using a suitable dilution of the toxic API, overcomes the problem of a very small and very precise dosage of the API, since the dosage of a liquid can be precise at 0,1 microliter. Stability of the API can get a good boost too, since mannitol and glycine - the most common supports for liophilized API - act as stabilizer too.
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Guys,
I have been freeze-drying Vancomycin for some studies. But since the last three batches, the number of vials breaking during lyophilization are too much!
I haven't changed the material vendor, nor the cycle parameters. Even the lyophilizer is the same. Can anyone please help me out?
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Dear Vemparala,
OD = outer diameter of the vial. Note, this may vary up the height of the vial, it is often bigger where the base of the vial joins the side, there may be a bulge.
Tray band = ring surrounding the tray of vials. This has a fixed size. If you have a full tray and need "force" the vials to fit in the band, not uncommon, it is ideal to have a tight pack of vials, just not "too" tight. However much "too" tight is!
Heterogenity = unless you control ice nucleation, all the vials will freeze at a different time. You will then have different ice crystal structures in each vial. The vial that cools more before freezing will have small ice crystals and the vial that cools less will have larger ice crystals ... you then do not have the same condition across your vials, they are different.
A full webinar on freezing from a true expert can be viewed here:
Look for the 2018 webinar by Dr Margit Giesler;
The Freezing Stage in Freeze Drying: Fundamental Concepts 2.0
You will have to register to view, but there is no charge.
Kind regards
Rob
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There is a multivitamin capsule I'm working on that ended up being too big, I'm thinking of changing the excipients as a way to make the capsule smaller and more convenient to take. the capsule contains omega three and other vitamins, that's why it's a soft gelatin capsule. so, I would also like to know if there are other options for the final dosage form.
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there is the book of the handbook of pharmaceutical excipients
as a galenist, I suppose:
soft capsule shaping contains omega 3 plus other vitamins causes a large capsule therefore it is possible just to administer the liquid contents and discard the gelatinous capsule.
otherwise you have to think about the form:
* separate omega 3 and vitamins (soft capsule + tablets)
* otherwise you will perform tests reducing vitamins to reduce the size of the capsule.
* if possible, try to incorporate some vitamins into the gelatin mass
Good luck
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Drug release study requires taking absorbance of samples at absorption maxima (Lambda max) of drug. What should be the approach in case of poly herbal formulation (nanogel). There are atleast 5 active components in the nanogel with different absorption maxima.
In this case, at what lambda max should the absorbance be taken?
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you can use HPLC with program sequence of diffrent lamda maxima & can anlyze the release quantity of drug.In primary stage you have to validate your method.
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-What are the latest techniques used for masking of the bitter taste in drugs how stable are they? Can we mask the bitterness of API's /drug's only with using Flavors? mostly in Orally Disintegrating Strip / Tablet. Could anyone suggest me?.
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Thank you to All.........
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I am having a hard time establishing a Tg'. I have sent this to other colleagues who give me a value at ~ -23*C. However, I am unsure how to establish a baseline to calculate this from.
My initial thoughts were to integrate peak linear and trying to establish a baseline across the melt region. Then I measured Tg' from the beginning of the transition to the point at which the graph crosses my baseline. This gives me my expected value, but I am unsure if this logically works or if I just got lucky.
Using FDM my collapse temperature was about -21*C. Any help would be appreciated.
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I think that there is no clear evidence to properly assign a glass transition temperature (Tg) to the plot presented at the enunciate. Maybe you want to check the signalled discussions ― on the relationship between Tg and the melting temperature for polymers: https://www.researchgate.net/post/What_is_the_best_correlation_between_glass_transition_and_melting_temperature https://www.researchgate.net/post/What_is_the_correlation_of_Tg_Tm_values_with_Hot_Melt_Extrusion
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In dissolution study of gastro retentive tablet , How to select dissolution fluid and their volume if drug's formulation is not official in pharmacopoeia.
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For gastro retentive preferable medium is acetate buffer pH 1.2 or 0.1 N HCl as gastro retentive we assume to be used in the empty stomach conditions. Volume of dissolution medium you can select on the basis of drug content of your formulation means the concentration of drug in each collected sample should be sufficient enough for the detection thorough your analytical method. Secondly, we should try to correlate with the empty stomach conditions (specially volume). 
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In dissolution test for Abilify 5mg (aripiprazole) Results show high results about 110%, while maximum result should not exceed 104%(max. result in content uniformity test).
This problem does not happened in Abilify 10 or 15 or 30mg.the different in Abilify 5mg is the colorant which is indigo carmine aluminum lake (E132).
When i run the dissolution test with placebo tablets (without active) it give results about 6%.
Dissolution medium contain KCL and 0.2N HCL. PH 1.2
The same method used for all types of Abilify tablets
UV- visible at 249nm , rpm 60 for 30 min.
So, if the reason is the colorant, how to avoid it?
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Determine absorbance of your samples using a blank solution made with the placebo of the formulation containing the lake colorant, to substract the effect of such colorant.
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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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How to increase the viscosity of the herbal shampoos?
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You can check some publications here: http://www.rheosense.com/publications
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Other than commercial drugs, what chemicals/reagents can be used to visualize drug delivery?
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Benzoic acid, Salicylic acid are stable and commonly employed as standard test drugs in formulation.
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I am doing reserch on the preparation of PLGA microsphere by phase seperation,and i have made many trials to accelerate the release ,but it doesn't work.  Does anyone who do related researches can share some experiences with me, for your help, i really appreciate.
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you can use lower mw PLGA or PGA itself. Vit E TPGS used in previous paper also work. Not sure about your main intention as PLG is hydrophobic by nature to slow release esp. as MP unless size reduction, too many articles on this aspect. 
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Chemical synthesis of Amoxicillin trihydrate
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Paclitaxel IV solution is commercially available which contains Cremophor EL and ethanol at 50:50 ratio.
As Cremophor EL has several drawbacks and side effects.
So, Why Tween 80 and Ethanol combination was not selected for the formulation?
What was the drawbacks of tween 80 over Cremophor EL?
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Thank you sir for the valuable information.
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Drug to be incorporated is water insoluble.
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either ur compound is water soluble or partially water insoluble drugs can form gel with pluronic F, actually pluronic F can make the insoluble drugs to be solubilized in low temperature before micelle formation .
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We have a salt and it's in powder form. We need to coat it to make it resistant to moisture. How can we coat this powder (salt)?  Considering it's water soluble and it should be coated in powder form.
Thanks in advance.
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What Calistus said is one option-making a solid dispersion of the powder in an inert polymer like PEG or waxes / acrylic polymers. 
The other method is Microencapsulation of the water-sensitive powder by suitable methods  like solvent evaporation, Wurster process, Spray drying. Check out the suitable polymer and method to be used. 
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Manufacturing process is wet granulation where API, Pregelatinized Starch & MCC PH 101 are used in dry mixing stage; whereas PVP k 30, PEG 400, Tween 80, Cremophore RH 40 are used as granulating aid with Purified Waster. And Ac-di-sol, MCC PH102, Sweetener, Flavors, lubricant are used in blending followed by lubrication stage. Drug load is 60% of total tablet weight.
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Thank you both Mr. Himangshu Bhatt Mr. Ahmed Agiba for reply.
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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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I've been preparing an oral dispersible film of Meclizine HCL (25 mg) that has to be solubilized in water. Unfortunately, it is almost insoluble in water (0.1 mg/ml). I tried using complexation method with cyclodextrins, solid dispersion method taking PEG 4000 as a carrier, used sodium citrate to shift the pH to an upper range so that drug ionization takes place aiding in enhanced solubility; however, the result has not been as promising as I would have liked. I would be grateful to get your inputs. Thank you.
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You can make trial by using surfactant micellization. Use some type of surfactants like Spans or Tweens to get your drug solubilized.
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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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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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If drug loaded micro-spheres are compressed into Tablet, will the compression affect the drug release behavior or not?
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Dear Athar
Yes, If drug loaded microspheres are compressed into tablet then compression will affect the drug release pattern so I will suggest you that if you want to check the drug release pattern of your microspheres encapsulated with the drug then use Dialysis Tube Method to check drug release pattern. Because in dialysis tube method, it is not necessary to make a tablet of drug loaded microspheres to check drug release pattern
If you have more question then I will be happy to answer it.
Cheers
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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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I'm developing transdermal patches with eudragit polymers using the solvent casting method onto glass petridish. The resulting films always get stuck on the glass surface and cannot be taken out. I have tried applying a little bit of silicon oil or glycerin on the glass surface to grease it to no avail. 
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You may also use silicone oil to prevent it, as silicone oil is almost insoluble in any solvent. 
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What size of batch should be studied under process optimisation during process qualification in pharmaceutical industry?
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As per FDA:
For Solid Dosage:Two Pilot Scale batches of 100,000 units or at least 10% of proposed production whichever is greater, Third batch can be smaller than 10% of proposed  production but NLT 25% of the pilot scale
For Parenteral: Two batches at least 10% of proposed commercial size (i.e. pilot scale size) or 50 L whichever is larger. Third batch can be smaller than 10% of proposed production but NLT 25% of the pilot scale
All submission batches manufactured under CGMP with same formulation, same specifications, and at the commercial site
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can any one help me with live example, how to protect pellets from cracking while compression in an ER product.
Please do not suggest what is in the litrature. I went through them and tried them but of no use.
please suggest me from industrial prospective.
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sir use cushning agent and special turret.
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In the Sasol Excipients for pharmaceuticals, the Emulsifiers are separated from Partial Glycerides. What is the reason for it? Why should Imwitor 372 and Imwitor 948 be separated, whereas both of them can be used as emulsifier? 
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Dear Zahra,
Partial glycerides are esters of glycerol with fatty acids, where not all the hydroxyl groups are esterified. Since some of their hydroxyl groups are free their molecules are polar. Partial glycerides may be monoglycerides (two hydroxyl groups free) or diglycerides (one hydroxyl group free). Short chain partial glycerides are more strongly polar than long chain partial glycerides, and have excellent solvent properties for many hard-to-solubilize drugs, making them valuable as excipients in improving the formulation of certain pharmaceuticals.
An emulsifier consists of a water-loving hydrophilic head and an oil-loving hydrophobic tail. The hydrophilic head is directed to the aqueous phase and the hydrophobic tail to the oil phase. The emulsifier positions itself at the oil/water or air/water interface and, by reducing the surface tension, has a stabilising effect on the emulsion. In addition to their ability to form an emulsion, emulsifiers have the ability to interact with other food ingredients. In this way, various functionalities can be obtained, for example interaction with proteins or carbohydrates. The emulsifier may be an aerating agent, starch complexing agent and/or crystallisation inhibitor.
The classification if a compound is an emulsifier or not is determined on its HLB value (Hydrophilic Lipophilic Balance). Generally, the HLB values of partial glycerides are very high and are not within the acceptable HLB range of emulsifiers as a result this class of compounds is not classified as emulsifiers.
Please note, that the HLB value reflects the ability of the emulsifier to interact with water and organic phase (oil). If the HLB is too high, the interaction with the oily phase is negligible, thus affecting the ability of the agent to stabilize a system of two phases: water & organic phase.
Hoping this will be helpful,
Rafik
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As per ICH, Quality by Design is nowadays mandatory requirement for regulatory procedures.
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QbD can be applied via step by step analysis of each step involved in your formulation design. If you are woking on nanoparticles or liposomes and you want to explore QbD for their optimization then you need to use step as following:
1.Selection of critical quality attribute of your final product.
2.Failure mode effect analysis. (it includes selection of factors using knowledge space and ishikawa diagram followed by risk priority numbering of the factors, selection of high risk factor)
3. Preliminary study of high risk factors.
4. Selection of upper and lower limit of factors at which you re getting desired response.
5. Use of PB screening design for screening factors having significant effect on response.
6. Use of RSM for optimization of screened factors.
7. Design space establishment.
8. Assessment of design space robustness.
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The dose is standardised in animals in mg/kg.
i just wanna extend the same treatment to cell lines and was trying to find a way to convert Drug dose from mg/kg to mg/ml ?
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Thank you Tushar for this discussion. Thanks to Rafik too for sharing valuable article. It is helpful for all. Thank you Alain and Sagar.
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I have prepared cationic niosomes composed of surfactants and DC-Cholesterol but i found these niosomes were not stable and tend to agregates in a couple of days although the ZP was around 75mV, so does any one has an explaination of that and how can i increase their stability?
thanks
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The stability of niosomes could be altered by surfactant to cholesterol ratio. selection of surfactant type, span 60  has been to be the best of its congers.
  • prepare them in a freeze dryed formf or longer term stability.
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Synovial fluid is normally a thick, straw-colored liquid found in small amounts in joints, bursae (fluid-filled sacs in the joints), and tendon sheaths.
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I don't think it is practical to replace synovial fluid. Connective tissue spaces generate their own fluid constantly. If you put anything in it will diffuse out very rapidly. I guess the question is why one would want to replace the natural fluid?
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As you know Lanolin is yellow substance and produce yellow eucerin . How can I bleach lanolin or eucerin?
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There is a bleached Lanolin available from "Parachem" 415 Huguenot Street, new Rochelle, New York 10801, 1-800-282-3982..
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I am trying to couple my compound with terminal carboxamide amine to lysine amine. Is there any prodrug for carboxamide so that the Lysine-compound conjugate breaks down to give carboxamide?
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Might help!
Recent Trends in Targeted Anticancer Prodrug and ...
www.ncbi.nlm.nih.gov › NCBI › Literature › PubMed Central (PMC)
by Y Singh - ‎2008 - 
Prodrug and conjugate design involves the synthesis of inactive drug .... Tegafur is a slow-releasing prodrug of 5-FU, which avoids the rapid breakdown of drug in ...... FUDR to aliphatic carboxylic acid chains to improve drug permeability [134]. ... greatest in the prodrugs with lysine and arginine residues giving IC50 values ..
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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 have a water extract of Withania somnifera and Curcumin (soluble in alcohol and acetic acid). I want to use them for disc diffusion assay for which I need a complete solution.I am unable to dissolve them in their respective solvents. I cannot use acetic acid as I am doing antibacterial study. I tried DMSO for both but they are not soluble. 
Thanks.
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Hi Adam, I tried with Acetic acid and even used as a control but in negative control as well I am getting inhibition zone. They should be completely soluble but I am seeing some visible particles of the extract in the solvents like Ethanol, DMSO,Water (for Withania somnifera).
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I am working on Curcumin Bioavailabilty improement.
My product (Test) have dose 25 mg and Reference product have dose 100 mg.
Test product have Cmax 1.46 mcg/ml and reference product have 1.16 mcg/ml Cmax.
How can i calculate Dose of test product to have same Cmax of reference?
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Thank you all friends
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I am trying to prepare cocrystals of one of the pharmaceutical API, from XRD results it shows formation of cocrystals.
1- I want to evaluate the same for it's all information about new single co-crystal for that i need to make a single crystal.
Please suggest me the best methods for single crystal preparation.
2- How can i confirm that, this is a single crystal?
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Dear Sir,
Thank you very much for the most useful information.
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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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I am trying to make a prodrug where it breaks down metabolically to give carboxamide. Is there any literature on carboxamide prodrug?
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I need small particles between 5 and 10 um.What material would be suitable? What encapsulation specific procedures would fit for such small particles? I manage to obtain encapsulation in alginate of both hydrophobic and hydrophilic agents but the particles are to big (240 um).
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One is spray-drying and another is emulsification-solvent evaporation method based on ionotropic gelation technique, provided high shearing overhead stirrer must be used.
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I have a small volume (<10ml) of viscous oil that I want to mix with a powder at high temperature. The mixture will be a tacky blend and viscous. So far I have been preparing the mixture using a mortar and pestle but this is not convenient and very messy. Does anyone have a suggestion for mixer or a mixer shaft (or any other type of blending device) that can be used to accomplish my objective?
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Once, you can try with tissue homogenizer..
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I need to dissolve Dronedarone-hydrochloride for intraperitoneal injections in mice. However, due to its hydrochloride form Dronedarone is quite differcult to dissolve in aqueous solutions. Phosphate buffers ranging from pH 3 to 5 with added cyclodextrin should increase the solubility of Dronedarone and be well tolerated at the injection site. I'm perparing a phosphate buffer (NaH2PO4, pH 4.5), but I'm not sure about what the cyclodextrin concentration should be? 
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Hi,
At pH 4.5 you might already some abdominal pain response in mice. I would suggest to increase the pH a little more ( close to 6). Using beta-cyclodextrin might help you in this regard.
I have used upto 30% Oral beta-Cyclodextrin in mice and it was tolerated well. But for IP, it would be wise to start from as low as 5% and observe if it improves solubility for the selected dose.
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I really need to know ASAP. Thank You!
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Thank you :)
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I would like to know how regulation on pharmceutical industry has affected its productitivy. Has anyone done something similar?
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Thanks a lot!!!
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 I am trying to read about this but I could not get a final answer and clear one 
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We used lissome to cleave chitosan in a nanoparticulate system in which chitosan contributed to the structure of the nanoparticle. It worked.
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Is anybody hahing the uv detection method for the lova, prava and atorvastatin?
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Contact me.....
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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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When we encapsulate oils in soft gelatin capsules, the capsules are getting coated with oil.
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Soft gel encapsulation is inherently messy, since your gelatin sheets are gloppy, the oil is filled under pressure, and the encapsulator isn't pressure-tight! (No way it could be, in continuous-movement mode.) So, don't fret. You could rinse the exterior of the capsules with a non-toxic volatile hydrocarbon (a couple dips in COLD butane should do it), before air-drying; don't know what solvent is commercially used for this, perhaps IPA?
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Do you know any example?
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compression force affects dissolution behavior of a drug, insignificantly. 
It mainly depends upon nature of the product and excipients included. 
If you are working on a water soluble drug, effect of compression will be negligible on dissolution rate. while working on water insoluble drug with low melting point (like Erythromycine stearate) effect of compression force will be more significant and even dissolution rate and disintegration tests can be failed. 
At high compression force material with low melting point forms an inclusion complex due to heat generated during compression which can reduce dissolution to large extent. Even physical appearance of tablets can indicate its nature change. For water insoluble and low melting point drugs compression force should be kept in an optimum range. 
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Oxaloacetate has been shown to be an effective glutamate scavenger.   Oral supplements have low bioavailability.   IV should be more effective, especially in crossing into the blood brain barrier.
Thank you in advance for your help,
Dr. Burtis
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Thank you!!
Scott
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I wonder if I can use it in topical drug delivery formulations as a permeation enhancer.
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Brief contact is essentially nonirritating to skin. Prolonged or repeated contact may cause moderate
skin irritation. Prolonged skin contact is unlikely to result in absorption of harmful amounts.
Similar materials have been shown to cause lung effects following contact with the skin.
ISO9001:2000 CertifiedMaterial Safety Data Sheet
Triton X-100*
*[Triton is a registered trademark of Dow Chemical Corporation]
Ingestion:
Low toxicity if swallowed. Small amounts swallowed incidentally as a result of normal handling
operations are not likely to cause injury; however, swallowing larger amounts may cause injury.
Aspiration into the lungs may occur during ingestion or vomiting, causing lung damage or even
death due to chemical pneumonia.
Inhalation:
At room temperature, exposure to vapor is minimal due to low volatility; single exposure is not
likely to be hazardous. Mist may cause irritation of upper respiratory tract.
Chronic:
May cause dermatitis and conjunctivitis.
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I mean , is there a methods that make it sweet ?
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Thanks Ashraf
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I am doing sustained release buccal drug delivery of statin having shorter half life (about 3 hrs), I am sustaining it for 12 hrs, will it require dose calculation?
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Sorry ur question isn't clear at all ! ......
U want to calculate in vitro release of sustain release formulation ? 
Or u r asking about is the half life of drug will be different for sustain release ? 
Please clarify ur question, paraphrase it ! 
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Commercial available biphenyl moiety containing drugs?  
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Oritavancin (LY333328)- analogue of eremomycin; 1000 times more potent than vancomycin
Read about this new antibiotic and I can send to you the structure, if needed:
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An intravenous (IV) formulation is desired for a high dose drug that needs to be delivered over a period of 8 to 10 hours. This sustained release approach would allow a bolus of drug (approximately 40 to 60%, burst release ) to be delivered quickly upon IV administration followed by the remaining dose  to be delivered in a near zero order fashion. 
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(tramadol HCl) Extended-Release Tablets
The volume of distribution of tramadol in small dosages, following intravenous dose. 
The binding of tramadol to human plasma proteins is approximately 20% and binding also appears to be independent of concentration up to 10 µg/mL. Saturation of plasma protein binding occurs only at concentrations outside the clinically relevant range.
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RELATED AREA- Cancer,Immunity,Plant Drug/Phytoanalysis,Pharmaceutical Sc.
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Eulalia vidal mam please write your e mail.
Thanks and regards.
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I am trying to prepare nanoparticles with alcoholic herbal extract. Suggest to me polymers that can be used?
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This article may help you even it does not answers your query 
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Subcutaneous formulations are developed based on the science of pharmaceutical drug formulations and empirically detected biological behavior. What are "golden rules" to develop a general "best in class approach for subcutaneous formulations to inject a new biologic (antibody, antibody-drug conjugates or vaccines) into the "biological compartment"?
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Broad variety of attributes:
• Molecular Weight (MW):
  1. small molecules
  2. medium molecules
  3. large molecules
• Chemistries and the level of structural complexity:
  1. biopolymers built from amino acids, nucleotides, saccharides
  2. Conjugates of large molecules with medium size (CovX) or small molecules (PEG)
• Manufacturing or source of the material:
  1. Small molecules are made by well understood and controlled chemical synthesis
  2. Proteins (including antibodies) are made by less controlled fermentation
  3. Cell components
  4. Cells or tissues
• Regulatory cutoff in the US (may be different in other countries):
  1. Peptides and oligonucleotides fall under NDA
  2. Proteins and antibodies
• Functional class
  1. Enzyme
  2.  Antibodies
  3. Hormones
• Others
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Hi there is a material called trolox using which we can perform the antioxidant capacity of a material. Any one aware about the analytical procedure along with calculation part kindly share. 
Thanks in advance 
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Follow this article:
If you have any question, do not hesitate to ask.
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What are the best phospholipids that can be used for topical drug delivery and manufacturers?
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Soyalecithin available in various grades can be used. You can get it from Lipoid who manufactures pure and quality grades. 
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Could the dialysis tubing concept in nanoparticle purification be used as in vitro dissolution tests for suppositories?
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yes you can use it .According to my exper. non membrane dissolution test for supp. was better correlated to the in vivo data.
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I would like to deliver in a cell specific manner an antisense in the colon
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Best and feasible way to target colon with colon specific micro or nano particles using different polymer or combination of polymeric material which are biodegradable or pH sensitive toward colonic area. Like chitosan 
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Stability study of pharmaceutical products
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From a RA standpoint the requested (to authorities) shelf-life must be based on real-time stability data and no extrapolation is allowed. According to WHO guidelines if accelerated stability was OK you could ask for extrapolation up to twice the real-time stability data (minimum of 12 mo real-time stability) but no more than 12 months extrapolation. Refer to Ali's attachments for details.
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Triton X-100 is nonionic surfactant which may be used for dispersing and encapsulation of poorly water soluble drugs. Is it justified and safe for enhancing the bioavailability of poorly water soluble drugs?
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USFDA has not not approved it for safe use for oral formulation.
So no toxic limit on same.
Kindly go through other reseach work to inquired oral toxic level or stage for same as reference 
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We are interested to screen molecules particularly peptides that can be delivered orally. Please write name of software or web server which we can use for predicting oral-delivery potential of a molecule. I will appreciate if you write free (open source software) for predicting bio availability of molecules particularly peptides and proteins. Please also write in vitro techniques (assays ) that correlate with in vivo bio availability of molecules.
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Thanks
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Dear All,
Can any one share me how to find A and B in Kopcha model of dissolution. Is there any software to do it? If so how to incorporate in it and get the results? Can we get it using excel sheet? Pls share your views as I want this details urgently. 
Thanks in advance 
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Kopcha kinetics
Qt = At1/2 + Bt
Kopcha kinetics model describes how to quanify contribution of diffusion & polymeric relaxation.(where A = diffusional constant and B = erosion constants) and Qt is the amount of drug dissolved in time t.,If you divide both side by t you will get                             Qt/t =A/t1/2+B.
 The above equation resembles Y=mx+C
By ploting Qt/t vs 1/t1/2, you will find slope means A ,  and intercept means B.
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When we perform dissolution studies of niosomal formulations how much volume of dissolution medium and how much quantity of niosomal formulation be added into dialysis bag, what consideration should be taken into account for this??
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The volume of dissolution medium and amount of formulation that is to be taken is based on the solubility of the drug in the medium.  Check the dissolution of the drug in the medium. The drug release from the niosomes at particular time interval should be quantifiable by the method used.
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My question does not just refer to their commercial use but also the R&D one… Let’s say I want to submit a Horizon 2020 project for a nano-functionalized cosmetic crème (not a medical grade one), would I still have to foresee clinical trials?
Does anyone have any experience on the EU’s ethics guidelines on this point?
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Hi Alexander
I suspect it depends upon what you expect to be able to claim for the product.  There are no clear guidelines in relation to "user" trials of cosmetics, although of course you need to have your biological safety assessments and other toxicology data completed before you should consider going ahead.
From a commercial point of view there may be advantages to conducting a properly constructed randomised trial.  Many Advertising Standards authorities now wish to see clear data in support of any claims made, especially if you are planning for marketing in countries like USA where the Federal Trade Commission will follow up on any claims - for example Lornamead were recently fined $500K for not being able to justify claims for a product (http://www.ftc.gov/news-events/press-releases/2014/05/company-settles-ftc-charges-head-lice-prevention-claims-were).
Also if the product is to be advertised through media like QVC they have a really quite strict code for what they want to see in terms of data (see attached).
So my advice is if you are confident of the effectiveness of the product, conducting a properly constructed randomised, controlled trial is not only the best way forward to give the product the best commercial start in life versus the opposition it could also save a lot of grief and money in the long term.
Good luck, Ian
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We  know that now a days,  the hollow core shell  materials are popular due to their applications in drug delivery system.  As they can separate molecules based on their pore size, can we call it as meso to macro molecular sieves?  However, I have not seen this material called a molecular sieve anywhere in literature? Why is this so?
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A sieve in the typical sense means a sheet of a porous material. A hollow core shell particle, in particular for the application of drug delivery, are independent particles, and thus I do not believe they can be used for the filtration of materials based on size.
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For example, gels.
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thiomers are chitosan , having thiol group attached to it. in case of topical application it is very possible to use it as a polymer for topical application. but its compatibility should be checked with Active pharmaceutical ingredient.
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Help! We don't have a speed vac and when I tried the freeze drier the solution was just spat out the ends of the tube. Solutions contain antibiotics so I need to watch the temperature. Any suggestions appreciated!
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For answers to a somewhat related question earlier posed at this forum, also dealing with gelatin coating: «Can anyone suggest a method to coat surgical grade titanium with a gelatin based film?» ─ you may check: https://www.researchgate.net/post/Can_anyone_suggest_a_method_to_coat_surgical_grade_titanium_with_a_gelatin_based_film
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The color of synthetic carbamazepine is cream, but in references it is white. how can i purify it to white crystalline.
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Thanks carlos for your answer. but in purification of this compound, after 3 times of re-crystallization, the color is pale cream, the solvent is EtOH and the anti-solvent is water.
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In Ionic Gelation Method Chitosan and TPP will be used to cross link and produce nanocapsules. Drug will be entrapped in the nanocapsules. 
My question is whether only the drug will be present within the entrapment of Chitosan Nanocapsules or it will be entrapped with some Chitosan with in the entrapment? 
Also let me know whether Poloxamer will help to reduce the aggregation of Nanocapsules in physiological fluids. 
Hope my question is clear. 
Thanks in advance
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I think it depends on the type of the drug (physico-chemical characteristics) and on the method of preparation. Release profile and scanning electron microscopy will give evidence about drug location.
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I need your help regarding a problem I faced during dissolving of a CGRP antagonist BIBN 4096 (10mg, Tocris).
I dissolved it in 1:1 ratio of 100% DMSO (500 micro liter) and water for inj. (500micro liter). but couldn't get success in doing so even after using ultra-sonicator. It would be a great help if you could suggest how to dissolve this drug at this stage (to make stock solution). We are planning to purchase the fresh drug and to use it again with new dilutions.
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