Back to the Top
Dear group,
Can anybody suggest that which is the ideal formulation for IV without using Captisol and Cyclodextrin. I tried with 6% solutol:ethanol (1:1), 6% DMSO and make up with normal saline, but it is getting precipitated.
Suresh
Jubilant Discovery centre
Bangalore.
Back to the Top
A simple solution which worked for me once, try diluting with Mannitol solution rather than saline (nonionic solution instead of ionic solution).
Thanks
Maninder
Back to the Top
The following message was posted to: PharmPK
Dear suresh,
Initially dissolve the compound in ethanol.
Later you can choose in between
DMSO/Dimethylacetamide/n-Methyl-2-pyrrolidone. Try using PEG 200
(around 40%) and make up with normal saline (not exceeding 35%). You
can try using probe sonicator instead of water bath sonicator. I dont
know why you dont want to use cyclodextrins, becoz they are very good
complexing agents?
(or)
Depending upon the pka value of the compound, try using buffer at a
particular pH instead of normal saline for enhancing the solubility.
With regards,
Vijaya Bhaskar Veeravalli,
GVK BIO
Back to the Top
40% PEG, 10% EtOH and 50% saline works for most of the compounds.
Back to the Top
15EtOH,15Cremophor EL,70dextrose is work
Back to the Top
Try 15 % Pharmasolve + 15 % Ethanol + top up with 6 % PEG 400. We have solubilised most of the water insoluble compounds in this cosolvant mixture
Hope this will help you.
Dr. Amol A Raje
Vimta Labs Limited
5, S. P. Biotech Park, Genome Valley
Turkapally, Shameerpe
Back to the Top
Dear suresh,
The following article will through some light on your query. An intravenous formulation decision tree for discovery compound formulation development by Yung-chi leeInternational Journal of Pharmaceutics, Volume 253, Issues 1-2, 6 March 2003, Pages 111-119.
note: There is no wonder in precipitation when you are attempting to formulate insoluble drug and there is no strict rule for selecting appropriate vehicle for IV administration, It all depends on physico chemical property of your compound and of course it may require couple of trials.
Regards
Devarajan,
Formulation Research.
Back to the Top
The following message was posted to: PharmPK
Dear Mr. Suresh,
Please find the artilce reference for your perusal, which will answer
all your questions. As per my experience every NCE has different
solubilty, so just based on any ones experience you cant decide the
solubility of your compound. Please kindly read this article and
choose the different solvent system as suggested for IV route.
I hope you will be confident and satisfied after reading the nicely
written article as below.
Thanks and regards,
Aslam Burhan
Piramal Life Sciences Ltd., Mumbai
Preclinical formulations for discovery and toxicology: physicochemical
challenges
Seshadri Neervannan
Amgen, Inc., Mail Stop 8-2-D, One Amgen Center Drive, Thousand Oaks,
CA 91320, USA
Expert Opin. Drug Metab. Toxicol. (2006) 2(5):715-731
Want to post a follow-up message on this topic?
If this link does not work with your browser send a follow-up message to PharmPK@boomer.org with "IV vehicle in rat PK study" as the subject | Support PharmPK by using the |
Copyright 1995-2011 David W. A. Bourne (david@boomer.org)