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Dear all,
I would like to prepare a solution for iv administration of a poor soluble compound . I have tried with beta-cyclodextrine withouth success. Has anyone experienced with gamma-cyclodextrine?. Would it be a better option than beta-cyclodextrin?
I would appreciate your comments.
Thans in adance for all
joan
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Dear Joan
For iv administration of poor soluble drugs, you can try to use some inorganic solvent, such as PEG100-400. I have tried to use PEG200 before.
--
Best Regards, Alec H YU
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Dear Joan,
Regarding choice of beta- versus gamma cyclodextrin (or other cyclodextrins), it first depends on how well the compound binds into the central cavity of the specific cyclodextrin. Gamma cyclodextrin has a larger cavity and can accommodate larger molecules. Cyclodextrin binding affinities tend to be relatively low (e.g., compared to antibodies), cyclodextrins themselves have specific aqueous solubilities. There are also derivatized cyclodextrins that have higher aqueous solubilities. The best approach is to obtain samples of cyclodextrins and test them in vitro. Note also that use of organic co-solvents with cyclodextrins will compete with the compound for the cyclodextrin binding site.
-Tom
Thomas L. Tarnowski, Ph.D.
CMC and Bioanalytics
Department Head, Biopharmaceutical Development
Elan Pharmaceuticals, Inc.
800 Gateway Boulevard
South San Francisco, CA 94080
thomas.tarnowski.at.elan.com
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The following message was posted to: PharmPK
Hi Joan,
I think you can try with hydroxypropyl beta cyclodextrin, along with
changing the pH if it does not affect the stability of your drug. Also
you can try with solvents like PEG 400.
TRY IT.
thanks,
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