We are looking at the in-vitro PK profile of few ester prodrugs usingBack to the Top
mouse and human serum.
Our lab follows the standard procedure of spiking the prodrug
(dissolved either in water or DMSO)in freshly collected
serum,incubation at 37C,taking the samples at different time points and
estimating the parent prodrug and the converted active by LC/MS or
HPLC.
I was wondering - Do we need to run a control in serum inactivated
esterase system to show that prodrug remains intact under those
conditions. If yes than which is the preferred method of inactivation -
heat or chemical??. I would appreciate some references if some one can
guide me to that.
Sandeep.
Dear Sandeep, to check the stability of the ester prodrug under theBack to the Top
conditions you apply, you need not follow any complicated procedures like
inactivating enterases. you can run a control in pH 7.4 phosphate buffer
to
confirm that the prodrug is hydrolysed by the enterases and not the
incubation conditions. i hope i am clear in xpressing what you wanted to
know,bye and All the best,Jagannath Kota
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