Study on the enzymatic reaction kinetics of epimeric isomers of budesonide in rat liver microsomes by HPLC

doi:10.3969/j.issn.10073205.2016.05.016

Abstract

Abstract: [
Abstract ] Objective Toidentifythedifferencesoftheenzymaticreactionkineticsoftwo
epimericisomersofbudesonideinratliver microsomes.Methods Theratliver microsomes
( RLM ) wasprepared by ultracentrifugation , andtheconcentration ofepimericisomersof
budesonideco-incubatedwithRLM weredeterminedbyhighperformanceliquidchromatography.
Results Themetabolicdifferencesoftwoisomersofbudesonidewereobservedafterbudesonide
incubatedwithRLM.Themetabolismof22R-budesonidewasfasterthanthatof22S-isomerin
theearlystageofincubationsoratlowconcentrationofmicrosomalenzymeused.However , with
theprolongation ofincubationtimeorincreasedconcentration of microsomalenzyme , the
metabolismof22S-budesonidewasobviouslyfasterthan22R-isomer.ThevaluesforK m andV max
of22R-budesonidewereabout2timesgreaterthanthoseoftheepimer ( 22S ) .Conclusion The
higheraffinityfor22R-budesonideandwithasmallvalueofV max , wasthemainreasonforthe
presentedmetabolicprofileofepimericisomersofbudesonide.

Key words: budesonide, microsomes, liver, rats

LIU Yan-shuang1, GUO Wei2. Study on the enzymatic reaction kinetics of epimeric isomers of budesonide in rat liver microsomes by HPLC[J]. Journal of Hebei Medical University, doi: 10.3969/j.issn.10073205.2016.05.016.

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Study on the enzymatic reaction kinetics of epimeric isomers of budesonide in rat liver microsomes by HPLC

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