（医疗药品管理）川陈皮素自组装前体脂质体的制备及其大鼠体内药动学研究.pdfVIP

（医疗药品管理）川陈皮素 自组装前体脂质体的制备 及其大鼠体内药动学研究 川陈皮素自组装前体脂质体的制备及其大鼠体内药动学研究 林薇，姚静，周建平 （中国药科大学药剂教研室，江苏南京210009） 摘要：本文研制川陈皮素自组装前体脂质体，且以混悬剂为对照考察其经大鼠灌 胃给药后的药代动力学行为。采用壹种新型前体脂质体法制备川陈皮素前体脂质 体，考察其水合后粒径、包封率、稳定性等理化性质；大鼠分别灌胃给予川陈皮 素混悬剂和水合后的脂质体后，以尼莫地平为内标，采用HPLC法测定血浆中药物 浓度，用Kinatica4.4程序计算药动学参数。制得的脂质体包封率可达80%之上, 平均粒径为212.1nm ，稳定性好；药代动力学研究显示,和混悬剂相比川陈皮素脂 质体于体内吸收较快,相对生物利用度264.3% ，MRT增加。结果表明，液态前体脂 质体制备工艺简单，可行性高；川陈皮素制成前体脂质体后，大鼠口服吸收显著 增加，且具有壹定的缓释作用。 关键词：川陈皮素；自组装前体脂质体；药代动力学 Preparationofself-assemblenobiletinproliposomesanditspharma cokineticsinrats LINWei,YAOJing ，ZHOUJian-ping ﹡ (DepartmentofPharmaceutics,ChinaPharmaceuticalUniversity,Nanjing210009,China) Abstract ： Toprepareself-assemblenobiletinproliposomesandstudythepharmacokinetic behaviorofnobiletininratsafterigadministrationofnobiletinpro-liposome 通讯作者: 　Tel: 86 - 25 - Fax: 86 - 25 - E-mail: zhoujianp60@163. com sandnobiletinsuspension.Nobiletinproliposomeswerepreparedbyanewkindof proliposomepreparationmethod,thetestsofphysicochemicalpropertiesinclu dingencapsulationefficiency,particlesizeandstabilityofformedliposomew eredetermined.Nobiletinsuspensionandnobiletinproliposmeswereadministr atedtoratsbyigadministration,respectively.Plasmaconcentrationofnobile tinwasdeterminedbyHPLCtakingnimodipineasinternalstandard.Thepharmacok ineticparameterswerecalculatedbyKinetica4.4software.Theencapsulatione fficiencyofnobiletinliposomeswasmorethan80%,withanaverageparticlesize of212.1nmandverygoodstability.Comparedtonobiletinsuspension,nobiletin proliposomespossessedhigherabsorptiverateandlongerMRT,andtherelativeb ioavailabilitywas264.3%inrat.Itcouldbeconcludedthatnobiletinproliposom eswasasimpleandfeasiblepreparation,andshowedgreaterabsorptionandsusta ined-releasecharacteristicscomparedwiththatofnobiletin. Keywords:nobiletin;self-assembleproliposome;pharmacokinetics 川陈皮素(nob