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The following message was posted to: PharmPK
Dear Sreekanth
Sources of cyclodextrins include: Wacker Chemie (www.wacker.com) and
Regis Technologies of Norton Grove, IL
You probably know this, but generally compounds with 'bi-aromatic'
moieties will be solubilized with beta-cyclodextrins, whereas compounds
with single aromatic rings are better solubilised using
alfa-cyclodextrins (a hydrogen-bonding group close to the ring also
helps). But I am not sure whether Oxazolidone is aromatic ?
Others ways of solubilising polar molecules is to use U.S. (Universal
Solvent) - otherwise known as DMSO ! A concentrated solution of your
compound can be diluted down with water etc to make the dosing solution
more bio-compatible. More often than not the compound will remain in
solution.
Hope this helps,
Dr Peter Clayton
petermc.-a-.wickhamlabs.co.uk
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Have you tried NN Dimethyl Acetamide. It might solve your problem.
Thanks
Mukesh Kumar
Principal Scientist
Dabur Research Foundation
India
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We got the 2 Hydroxypropyl Beta Cyclodextrin from Sigma for disolving
itraconazole. But it was in a weird place in the catelog because of
the "2"
at the beginning. Don't know if this would apply to the Sulfa butyl
compuound.
Regards-- John
John Mohr, Pharm.D.
Clinical Instructor
University of Texas Health Science Center
Division of Infectious Diseases
6431 Fannin, JFB 1.728
Houston, TX 77030
Phone: 713-500-6742
Fax: 713-500-5495
Email: john.mohr.at.uth.tmc.edu
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The following message was posted to: PharmPK
Sreekanth
Call Cydex and ask for their Captisol product line. They are located in
Kansas City (Overland Park), KS. Their information is
CyDex, Inc. * cdinfo.-at-.cydexinc.com
12980 Metcalf Ave., Suite 470 * Overland Park, KS 66213 USA
Ph: (913)-685-8850 * Fax: (913)-685-8856
Good Luck
Anup Zutshi
PDM, Pfizer
Kalamazoo, MI
(269) 833-8347
Anup.Zutshi.-at-.Pfizer.com
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Sreekanth, SBE cyclodextrins are sold under the commercial name of
Captisol
by CyDex in Kansas. You may obtain more information at www.cydexinc.com
Srinivasan Ramanathan, Ph.D.
Gilead Sciences
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You can buy SBECD in CTD inc (www.cyclodex.com).
J
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Thank you all for your kind responses regarding the solubility of my
Oxzolidinone family of compound. Some researchers raised some points.
So, i am just clarifying those issues.
1. Actually my compound is bi- aromatic and I should use Beta -
cyclodextrin to dissolve it. I found Cydex inc, the manufacturer of
CAPTISOL, the only approved formulation by FDA among cyclodextrins.
I will try first with Hydroxy propyl cyclodextrin ( HPCD) and then,
Captisol.
Sreekanth Gutala
sgutala.-at-.hotmail.com
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The following message was posted to: PharmPK
Hello Dr. Srikanth,
I feel, as far as oxazolidinone series is concerned, the best solvent
is DMSO. generally people will be using drug dissolved in pure DMSO for
intravenous administration to rodents. For initial screening of
oxazolidinone compounds in rodents DMSO solution can be used. But if
your DMSO concentration is greater than 5%, the formulation cannot be
used for intravenous administration in dogs because they are very
suseptible to it. So, I feel the best phenomenon that holds good with
oxazolidinone series is complexation using cyclo dextrins.
You mentioned in your mail that CAPTISOL is the only formualtion
recommended by FDA among cyclodextrins.Can you send me any further
details regarding this?
As far as my knowlwdge goes, HPBCD, according to literature, is
recommended for intravenous administration. So, for pre-clinical
evaluation it is the best option for oral and intravenous
administration.
Expecting your valuable comments on my points
Regards
Ravi Kanth Bhamidipati
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