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1、紫杉醇长循环脂质体制备及其药动学探究摘要：目的制备紫杉醇长循环脂质体并观察其在大鼠体内的药动学。方法用薄膜分散法制备紫杉醇长循环脂质体；HPLC法测定血浆中紫杉醇的药物浓度；用3P97程序计算药动学参数。结果脂质体粒径为(106.5±1.7)nm,包封率为(87.5±2.5)%,紫杉醇长循环脂质体和紫杉醇注射液的血药浓度-时间曲线均符合二室模型，药动参数tl/2B分别为(7.32±1.24)h和(0.32±0.06)h,AUC分别为(23.85±1.20)ug・h・mL-1和(5.08±0.45)ug•h•mL-lo结论与紫杉醇注射液相比，
2、紫杉醇长循环脂质体显著延长了紫杉醇在血液循环系统中的驻留时间，具有长效作用。关键词：紫杉醇；长循环脂质体；包封率；药动学中图分类号：R946文献标识码：A文章编号：1672-979X(2009)-01-0014-04PreparationofLong-circulatingPaclitaxel-containingLiposomesandItsPharmacokineticsZHANGZi-yul,JIALi-jun2,GONGJian-gang3,LIGuang-zhou4,KANGBail*(1.DepartmentofPharmaco
3、logy,WeifangMedicalUniversity,Weifang261042,China；2.BeijingTongrenHospitalaffiliatedtoCapitalMedicalUniversity,Beijing100730,China；3.CollegeOfTraditionalChineseVeterinaryMedicine,HebeiAgriculturalUniversity,Dingzhou073000,China；4.DepartmentofNuclearMedicine,AffiliatedHospi
4、talofWeifangMedicalUniversity,Weifang261042,China)Abstract:ObjectiveTopreparethelong-circulatingpaclitaxel-containingliposomesandevaluateitspharmacokineticsinrats.MethodsThelong-circulatingpaclitaxel-containingliposomeswerepreparedbyfilmdispersionmethod.Theconcentrationofp
5、aclitaxelinrats，plasmawasdeterminedbyHPLCmethodandtheparameterswerecalculatedwith3P97program.ResultsThemeandiameterofliposomeswas(106・5±1.7)nmandtheentrapmentefficiencywas(87.5±2.5)%.Theplasmaconcentration—timecurvesoflong-circulatingpaclitaxel-containingliposomesandpaclit
6、axelinjectionwerebothfittothetwo-compartmentmodelandthepharmacokineticparameterswere(7.32±1.24)hand(0.32±0.06)hfortl/2P,(23.85±1.20)ug•h•mL-1and(5.08±0.45)ug•h•mL-1forAUC,respective!y.ConclusionComparedwithpaditaxelinjection,thelong-circulatingpaclitaxel-containingliposome
7、scansignificantlyprolongtheresidenttimeofpaclitaxelinthebloodcirculatingsystem,andhasaprolongedaction.Keywords：paditaxel；long-circulatin£liposome；entrapmentefficiency；pharmacokinetics紫杉醇(paclitaxel,PTX)是从短叶红豆杉种属的树皮中提取的一种抗癌新药，它通过促进细胞微管聚合，抑制微管降解以及使纺锤体失去正常功能的机能异常方式抑制细胞的有丝分裂，阻
8、止细胞周期的G2及M期的修复，诱导多种癌细胞的凋亡［1,2］。临床上紫杉醇常作为治疗卵巢癌、乳腺癌、宫颈癌和非小细胞肺癌的一线用药［3］。目前市售的PTX注射液以无水乙醇和聚氧乙
