Dear All,Back to the Top
Does anyone know of any appropriate method to see if the drug X is
metabolised in say, intestine? Also is anyone aware of any commercial
source for deuterated Digoxin and Midazolam?
All the best,
Dear AhmadBack to the Top
If you wanted the D-Midazolam for a MS standard I believe Ultrafine in
the UK do a 13C, M+5 standard. Regards Digoxin if you cannot find a
source it may be possible do a simple (preliminary) exchange experiment
with D20 to see if enough exchange occurrs. This can be quite compound
dependant and will lead to a cluster of isotope masses on the MS. My
company, BioDynamics in the UK, does a lot of radiosynthetic work and in
our experience it often represents a suitable and quick way forward.
Regards the intestinal metabolism query, I would suggest an incubation
of Drug-X with intestinal microsomes (+ enzyme cofactors) in the first
instance. These are commercially available and I believe are available
from several common laboratory species in addition to man.
Head of In Vitro Metabolism
Back to the Top
to synthesize d3-digoxin H/D exchange in etOD + D2O (best solubility in
80% ethanol) using triethylamine
is suitable. You may need to repeat the exchange procedure to obtain
Dr. rer. nat. Thomas E. M\0xB8rdter
Dr. Margarete Fischer-Bosch-Institut fuer Klinische Pharmakologie
Auerbachstr. 112, D-70376 Stuttgart, Germany
Tel. +49 (0) 711 8101-3707 FAX +49 (0)711 85 92 95
With thanks to people who got back to me on Isotopes;Back to the Top
About the second issue (testing the drug X for metabolism); What I'm
looking for is an experiment that can check for microsomal and
cytosolic metabolism at the same time if there is such an experiment.
(Not just Microsomal enzymes).
All the best
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