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.docx

编号：时间：2021年x月x日书山有路勤为径，学海无涯苦作舟页码：第页共NUMPAGES9页第PAGE\*MERGEFORMAT9页共NUMPAGES\*MERGEFORMAT9页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通讯作者:Tel:[phone],Fax:[phone]E-mail:[e-mail]（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，并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。采用一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%以上,平均粒径为212.1nm，稳定性好；药代动力学研究显示,与混悬剂相比川陈皮素脂质体在体内吸收较快,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，并具有一定的缓释作用。关键词：川陈皮素；自组装前体脂质体；药代动力学Preparationofself-assemblenobiletinproliposomesanditspharmacokineticsinratsLINWei,YAOJing，ZHOUJian-ping﹡(DepartmentofPharmaceutics,ChinaPharmaceuticalUniversity,Nanjing210009,China)Abstract：Toprepareself-assemblenobiletinproliposomesandstudythepharmacokineticbehaviorofnobiletininratsafterigadministrationofnobiletinpro-liposomesandnobiletinsuspension.Nobiletinproliposomeswerepreparedbyanewkindofproliposomepreparationmethod,thetestsofphysicochemicalpropertiesincludingencapsulationefficiency,particlesizeandstabilityofformedliposomeweredetermined.Nobiletinsuspensionandnobiletinproliposmeswereadministratedtoratsbyigadministration,respectively.PlasmaconcentrationofnobiletinwasdeterminedbyHPLCtakingnimodipineasinternalstandard.ThepharmacokineticparameterswerecalculatedbyKinetica4.4software.Theencapsulationefficiencyofnobiletinliposomeswasmorethan80%,withanaverageparticlesizeof212.1nmandverygoodstability.Comparedtonobiletinsuspension,nobiletinproliposomespossessedhigherabsorptiverateandlongerMRT,andtherelativebioavailabilitywas264.3%inrat.Itcouldbeconcludedthatnobiletinproliposomeswasasimpleandfeasiblepreparation,andshowedgreaterabsorptionandsustained-releasecharacteristics