Questions related to Formulation Development of Pharmaceuticals
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.
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)
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?
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.
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!
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?
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.
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?
-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?.
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.
In dissolution study of gastro retentive tablet , How to select dissolution fluid and their volume if drug's formulation is not official in pharmacopoeia.
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?
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.
Other than commercial drugs, what chemicals/reagents can be used to visualize drug delivery?
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.
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?
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.
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.
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?
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.
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.
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?
If drug loaded micro-spheres are compressed into Tablet, will the compression affect the drug release behavior or not?
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.
What size of batch should be studied under process optimisation during process qualification in pharmaceutical industry?
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?
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 ?
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?
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.
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.
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.
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.
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?
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?
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).
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?
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?
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.
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,
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?
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.
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"?
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
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?
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.
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
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??
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?
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?
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!
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
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.