A lipophilic prodrug of Danshensu：preparation, characterization, and in vitro and in vivo evaluation-中国期刊网

摘要 Danshensu[3-(3,4-dihydroxyphenyl)lacticacid,DSS],oneofthesignificantcardioprotectivecomponents,isextractedfromtherootofSalviamiltiorrhiza.Inthepresentstudy,anesterprodrugofDanshensu(DSS),palmitoylDanshensu(PDSS),wassynthesizedwiththeaimtoimproveitsoralbioavailabilityandprolongitshalf-life.TheinvitroexperimentswerecarriedouttoevaluatethephysicochemicalpropertiesandstabilityofPDSS.AlthoughthesolubilityofPDSSinwaterwasonly0.055mg·mL~(-1),itssolubilityinFaSSIFandFeSSIFreached4.68and9.08mg·mL~(-1),respectively.Octanol-waterpartitioncoefficient(logP)wasincreasedfrom-2.48ofDSSto1.90ofPDSS.PDSSwasrelativelystableintheaqueoussolutioninpHrangefrom5.6to7.4.Furthermore,thepharmacokineticsinratswasevaluatedafteroraladministrationofPDSSandDSS.AUCandt1/2ofPDSSwereenhancedupto9.8-foldand2.2-fold,respectively,comparedtothatofDSS.Cmaxwas1.67±0.11μg·mL~(-1)forPDSSand0.81±0.06μg·mL-1forDSS.Thus,theseresultsdemonstratedthatPDSShadmuchhigheroralbioavailabilityandlongercirculationtimethanitsparentdrug.

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A lipophilic prodrug of Danshensu：preparation, characterization, and in vitro and in vivo evaluation

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A lipophilic prodrug of Danshensu：preparation, characterization, and in vitro and in vivo evaluation

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