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1、雷帕霉素缓释涂层支架在模拟心脏泵血状态下的体外释药研究213324陈玉成,熊素彬,幸浩洋,曾智,齐民(11浙江工业大学药学院,杭州310000;21四川大学华西医院心内科,成都610041;31四川大学物理学院应用物理系,成都610041;41大连理工大学材料工程系,辽宁大连116023)摘要:目的利用体外模拟血循环装置,评价自制雷帕霉素乳酸2羟基乙酸共聚物(PLGA)涂层支架的体外药物释放规律,探讨释药机制,为涂层支架的应用提供药动学参数。方法以316L不锈钢为支架,采用高压多层电喷技术制备含雷
2、帕霉素的PL2GA涂层。采用自制体外模拟循环装置,定时取样,RP2HPLC检测残留于支架的药物,评价流体循环冲刷状态下雷帕霉素涂层支架的药物释放度。结果自制雷帕霉素PLGA涂层支架的涂层厚度平均为5～10μm,雷帕霉素的平均含量为14139μg。在模拟流体循环冲刷状态下,雷帕霉素涂层支架的体外药物释放呈先快后慢的趋势,12和30d药物累积释放百分率分别为(58148±5167)%和(60166±5175)%,释药机制以溶蚀为主。结论体外模拟血循环装置适于药物涂层支架体外释药的研究;自制雷帕霉素PL
3、GA涂层支架的体外释药符合内皮细胞增殖规律,与动物体内疗效一致。关键词:雷帕霉素;雷帕霉素缓释涂层支架;模拟血循环装置;体外释放中图分类号:R94411文献标识码:A文章编号:1001-2494(2008)09-0688-05InVitroReleaseofRapamycinSustainedElutingStentDetectedbyaNewDesignedCirculatingDevice213324CHENYu2cheng,XIONGSu2bin,XINGHao2yang,ZENGZhi,Q
4、IMin(11CollegeofPharmaceuticalScience,ZhejiangUniversityofTechnology,Hangzhou310000,China;21CardiovascularDepartment,WestChinaHospital,SichuanUniversity,Chengdu610041,China;31AppliedPhysicsDepartment,CollegeofPhysicalScience,SichuanUniversity,Chengdu6
5、10041,China;41MaterialDepartment,DalianUniversityofTechnology,Dalian116023,China)ABSTRACT:OBJECTIVETodetectinvitroreleasepropertiesofrapamycinsustainedelutingstentandtoprovidepharmacokineticprofileforclinicalapplication1METHODSRapamycinandPLGAwerecoat
6、edonthe316Lstainlessmetalstentbythehighpressuremultilayerelectronicsprayingtechnique1Theinvitroreleasekineticsofrapamycinsustainedelutingstentwerestudiedbyaself2de2signedmimiccardiacpumpingdevice1Attheinterval,theconcentrationofrapamycinontheremaineds
7、tentwasdetectedbyRP2HPLCmethod1RESULTSTheaveragethicknessofrapamycinandPLGAcoatingwas5～10μmandtheaveragecontentofrapamycinwas14139μg1Theinvitroreleaseprofileshowedthatrapamycinreleasedslowlyfromthecoatingwiththefastspeedattheearlystageandslowspeedatth
8、elaterstage1Thecumulativereleasepercentageswere(58148±5167)%for12dand(60166±5175)%for30d1ThereleasemechanismaccordedtoHixson2Crowellerosionmodel1CONCLUSIONTheself2designeddeviceformimiccardiacpum2pingissuitabletostudytheinvitroreleaseofdrugelu
