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Hello - I am trying to formulate a compound in 25% b-cyclodextrin for a
PK
study. I haven't worked with this excipient before and upon mixing it
with
water, as has been suggested in other publications, it becomes a
non-homogenous sludge. Is there some trick I am missing? I appreciate
your
experience with this excipient. Thanks- Maralee
Maralee McVean, Ph.D.
Senior Scientist, Absorption and Pharmacokinetics
Cerep, Inc.
15318 NE 95th St.
Redmond, WA 98052 USA
Phone: 425.895.8666 x 286
Fax: 425.895.8668
m.mcvean.-a-.cerep.com
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I suggest you use Hydroxy Propyl Betacyclodextrin instead of beta
cyclodextrin. HP b-cyclodextrin has more aqueous solubility
Sunil Vandse
Able Labs
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Hai
If you are using to formulate with beta cyclodextrin. First solubilize
the compound in DMSO (Permissible limits) then add the aqueous
solubilized 25% beta cyclodextrin to it while stirring. Hope this will
solve your problem.
Regards
Ansar Ali Khan, M.Sc.,
Research Scientist,
Drug Metabolism and Pharmacokinetics,
Glenmark Research Centre,
Plot No.-A-607, TTC, Industrial Area,
Mahape, Navi Mumbai-400 709,
India.
Phone No: 91-22-5590 2491/92 Extn.308
Fax No.: 91-22-5590 2318
Dear MaraleeBack to the Top
as such the B-Cyclodextrin is sparingly soluble in water, it is better
to use the solution of 5% cyclodextrin. it is better to warm the
solution to get clear solution of cyclodextrin. if the drug is not
soluble in 5% B-cyclodextrin, it is better to opt water soluble
derivative of Hydroxy propyl B cyclodextrin or sulfa butyl ethrer
cyclodextrin. if still drug is not soluble it is prefered to use
cosolvent along with Hydroxy propyl B cyclodextrin.
Basavaraj
Senior pharmacologist
Formulation research Dept
Dr.Reddys labarotaries
India
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Hello,
It is better to use hydroxy propyl beta cyclodextrin over simple
cyclodextrin as the former is having more aqueous solubility over the
latter. Comming to the point of method of preparing, you can try the
following procedure:
First take the required quantity of dextrin and add water to it.
Sonicate till the time dextrin gets into solution. Weigh aliquot
quantity of the drug dissolve in minimum quantity of DMSO. Then add
drug solution drop by drop to the cyclodextrin solution while
vortexing.
Note: While preparing the formulation please consider the volume
expansion factor which is generally seen with cyclidextrin formulation
In case of doubt please feel free to contact me.
Regards,
Ravi Kanth
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dear maralee,
what we usually use is not \0xFB02-Cyclodextrine but
Hydroxypropyl-\0xFB02-Cyclodextrine which does a good solubility enhancing
job on
most of our compounds. We use it up to 30% and the rough procedure is a
simple solubilizing process of mixing/(slightly heatin, if necessary and
NCE is ok)/and sterile filtering (also for iv administartion).
all the best,
Philip
Dr. Philip Lienau
Schering AG
Research Pharmacokinetics
Tel.: +49 - 30 - 468 - 18507
Fax: +49 - 30 - 468 - 12238
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I would agree with most of the contributors here that HPCD is
definitely a preferably choice over the CD. I have worked with HPCD in
a semisolid formulation (an ointment like formulation) to enhance the
solubility of the poorly soluble steroidal drugs in the transdermal
absorption. We have used polyethylene glycol as an vehicle. I believe
if you are conducting PK clinical studies then incorportaing DMSO is
not an good option, however if your studies are animal specific then it
could be an viable option.
Good luck!!!
Naushad
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Dear Mr. Naushad,
I do agree that DMSO is not an ideal solvent that can be used. We can
select a suitable solvent depending on the nature of the NCE under
question. It is preferable to keep DMSO percentage below 10 % in the
final formulation if it is meant for rodent studies.
Regards,
Ravi Kanth
Ravi Kanth Bhamidipati
Senior Pharmacologist
Dept.of Drug Metabolism and Pharmacokinetics
Discovery Research Division
Dr.Reddy's Laboratories Ltd.
Bollaram Road , Miyapur
Hyderabad - 500 050
Andhra Pradesh
India
Hello,Back to the Top
Does anyone know if hydroxypropyl-b-cyclodextrin is soluble in
propylene glycol? If it is, and anyone out there has ever used both in
their formulation, what amounts did you use? Is it possible to get up
to 40% of each?
Andy
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