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The following message was posted to: PharmPK
Dear group,
Due to toxicological considerations of `inert' excipients such as
Hydroxypropyl-b-Cyclodextrin, I wonder if there is any literature which
is
looking for the absorbance / bioavailability of this formulation
ingredient
itself (not considering drug substances being absorbed from a HPbCD
solution).
Does anyone have a reference for this question in any species or an
educated guess?
best regards and have a nice christmas break!
Philip
Philip Lienau
Schering AG
Research Pharmacokinetics
Tel.: +49 - 30 - 468 - 18507
Fax: +49 - 30 - 468 - 12238
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The following message was posted to: PharmPK
dear Philip,
as far as I know the trouble with the use of cyclodextrin P.O. is that
they are not absorbed orally which is responsible for non-absorption of
some drugs relatively to their cyclodextrin affinity.
I hope this helps,
Frederic DOC
ACRITER CONSULTING
7 rue montespan
91024 Evry cedex
France
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Dear Frederick,
By saying so do you mean that cyclodextrin should not/ cannot be used
for oral formulation of highly water insoluble drugs?
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The following message was posted to: PharmPK
As we cannot be sure that the total drug is released from the
cyclodextrin we cannot ensure the max absorption. This is the main
reason for which I would not suggest to use HPBCD in oral dosage forms.
Hope this answers your question.
Best regards,
Frederic Doc
ACRITER CONSULTING
7 rue montespan
91024 Evry cedex
FRANCE
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The following message was posted to: PharmPK
Dear Frederic
As you told that cyclodextrin reduces
absorption
but we observed vice versa that it increses the absorption of NCEs. Is
this have any relation to lipophilicty of compounds because our NCEs
are
lipophilic and highly insoluble in water with a mol. wt. less than 500
or
some thing else?
Also we observed cyclodextrin absorption in
rodent pk studies ( obseved on HPLC )
Rahul Patil
Senior Research Associate
Wockhardt Research Centre
Aurangabad
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The following message was posted to: PharmPK
Dear All
Maybe this might be of interest to your discussion: Goran Westerberg,
Lars Wiklund, Beta-cyclodextrin reduces bioavailability of orally
administered [3H]benzo[a]pyrene in the rat, J.Pharm.Sci 94(1), 2005, (p
114-119)
Kim Kristensen, PhD
Research scientist
Pharmacokinetics
Novo Nordisk A/S
Denmark
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