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The following message was posted to: PharmPK
It appears that formulation scientist do not like DMSO
that much; at least they prefer DMA over DMSO. But I
have not heard any convincing reason yet. One study
showed that DMSO causes more hemolysis than DMA. This
may be true but DMSO is far less toxic than DMA. Even
in ICH guideline, DMSO is classified as class 3,
whereas DMA is classified as class 2. I remember even
once someone said DMSO is never used in human
formulations. Is this true? And if, why? I appreciate
if someone can clear this for me.
Rostam
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Dear Rostam,
one reason might be, that DMSO is a known and unusual strong permeation
enhancer. It might override a transporter or intestinal metabolic enzyme
recognition leading to a higher F%. Especially in early PK studies (when
the compound in a program can still be changed) , you don=B4t want to be
misled in this respect. In in vitro metabolic setups, DMSO (in contrast to
MeOH or AcN) also strongly inhibits the turnover rate of microsomal
preparations, recombinant CYPs etc. (see: Easterbrook et al., DMD, 2002,
Vol. 29 No. 2, 141ff).
best regards,
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
DMSO was used recently to formulate 17-AAG. However, the offensive
taste killed the formulation and Kosan went to Cremophor El instead.
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Copyright 1995-2010 David W. A. Bourne (david@boomer.org)