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 Wysłany: Czw 21:06, 17 Mar 2011 Temat postu: 地塞米松前 |
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地塞米松前体药结肠定位释放的药代动力学
ksV，TriggerDJ，ThomsonAG．Prednlsolonelevelsintheplasmaandurine：astudyoftwopreparationsinman[J]BrJClinPharmacol，1975，2(4)：327—332．[73FedorakRN，HaeberlinB，EmpeyLR．CuiN，No]enH3rd，JewellLD。etalColonicdeliveryofdexamethasonefromaprodrugaccelerateshealingofcolitisinratswithoutadrenalsuppression[J]．Gas-troenterology，1995。108(6)：1688—1699．Pharmacokineticsofcolon—specificdeliveryofdexamethasoneprodrugZHOUSi—Yuan，MEIQi—Bing，ZHOUJin，ZHAODe—Hua(DepartmentofPharmacology，theFourthMilitaryMedicalUniversity，Xia717100322，China)Abstract：Toevaluatecolon-specificdeliveryofdextran—dexamethasone，whichwassyn—thesizedbyusingdextran(．averagenlolecu—larweight一20000)asadrugcarrier，andtheprodrugwasgivenbyoraladminstrationatdosageof5t~mol·kg～．Thedistributionofreleaseddexamethasoneincontentofdif—ferentpartsofratgastrointestinaltractandinplasmawasdeterminedbyHPLC。andcomparedwithfreedexamethasone，Wefoundthatdexamethasoneanddexametha—sone—hemisuccinateweremainlyreleasedincecumandcoloncontentsafteroraladminis—trationofdexamethasoneprodrug．Thepeaktimeofdruginplasmawas6．3h，andthepeakconcentration110g·L．How—ever，freedexamethasonewasmainlydis—tributednstomach，proximalsmal1ntes—tineanddista1smallintestinewhenfreedexamethasonewasadministeredatthesamedosage．Itspeaktimeinplasmawas2．2h，andthepeakconcentration2．12mg·L～．Theresultsshowthatdexametha—sonecanbedeliveredtolargeintestinebydexamethasoneprodrug，andtheprodrughasapotentialintreatmentofcolitis．Keywords：prodrug；dexamethasone；kinetics，pharmaco(车文编辑石涛)-
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