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We are looking for a suitable dosing vehicle to try for our insoluble compounds. I have been looking to use NMP. Can anyone tell me what are the acceptable levels for use in both oral dosing and iv dosing? From what I can find out it looks like I can go up to about 25 % in water. I've no experience with this as a vehicle, any help would be gratefully received!
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The following message was posted to: PharmPK
I suggest you go to archives of PharmPK of yesteryears and you will find threads where this has been discussed at length.
I would rather go with a relatively safer approach before using NMP for either IV or oral use. In brief, preferred is to make use of the ionization constant of the compound by manipulating the pH with or without a complexing agent, use of co-solvents and/or surfactant <40% (make sure that the super-saturation does not lead to massive ppt, and you do not exceed surfactants>10%), or (if the POC stages of developments and if oral) micronization/ nanosizing in presence of stabilizer(s) or an amorphonization of the compound. Generally used co-solvents/surfactants could be PEG400, PG, Cremophor ELP, Solutol HS15, Ethanol, or a combination of these. Make sure that your formulation does not crash out after dilution with relevant bio-media, and the osmolality is not too high to cause untoward reactions at the site (if IV). Kindly note that most of these algorithms are not platforms and are being worked out on a case by case basis.
Still if you want to use NMP, DMA, DMSO or similar, better use it as low (<5%) as possible and run a vehicle control prior to your main study.
Hope this will help.
Vaibhav Sihorkar, Ph.D.
[Head, Pharmaceutical Development]
Aurigene Discovery Technologies Limited
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