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Hi all,
I have a novel compound for Pre-clinical screening by I.V. and sub-cutaneous route. The
compound is non-polar, it is not soluble in Ethanol, soluble in DMSO. Can anyone suggest
for suitable co-solvents and their limits for dosing in animals by these route.
Nagsen Gautam
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The following message was posted to: PharmPK
Hello,
I found this paper to be exceptionally helpful when I was developing
formulations for our lab.
Int J Pharm. 2007 Aug 16;341(1-2):1-19. Epub 2007 May 26.
Developing early formulations: practice and perspective. Li P , Zhao L
AJ Beaupre
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Hi gautam,
There are some excellent review articles which talk about this. Usually for preclinical
studies, use either cosolvency or pH adjustment or use of buffers for making solution.
The order of cosolvents for making solution also makes the difference. I suggest, use
PEG400 or PEG200 (20%). I usually found N-methylpyrrolidene (around 10%) to be a good
cosolvent for highly lipophilic compounds. Try changing the pH and if you still have
problems, use buffers instead of saline.
Regards
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Hi..
total cosolvent content should be <15% in SC formulation. SC route has the highest constraints in using cosolvents because of the very slow rate of diffusion from the administration site and rich nerve supply. here is another article which very useful..
Solubilizing Excipients in Oral and Injectable Formulations; Robert G. Strickley; Pharmaceutical Research, Vol. 21, No. 2, February 2004
Jay
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Hi,
The use of 10% NMP is not documented, can you please give us the
reference in which you found the information!
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