吲哚美辛口服自微乳化给药系统的大鼠体内药动学研究  

Study on the pharmacokinetics of indomethacin oral self-microemulifying drug delivery system( SMEDDS) in rats

作　　者：滕希峰[1] 李钟[1] 方壬德[1] 李国全[2] 黄诗莹[1] 何洋[3] 何琳[3] 

机构地区：[1]广东药科大学国家中医药管理局岭南药材生产与开发重点研究室,广东广州510006 [2]广东药科大学广州市医疗救助服务中心,广东广州510630 [3]广东药科大学医药化工学院,广东中山528458

出　　处：《广东药学院学报》2016年第4期406-409,424,共5页Academic Journal of Guangdong College of Pharmacy

基　　金：广东药学院"创新强校工程"医药化工省级实验教学示范中心资助项目;广东省医学科学技术研究基金项目(A2015345);广东省科技计划项目(2016A020226018)

摘　　要：目的研究吲哚美辛口服自微乳化给药系统(IDM-SMEDDS)在大鼠体内的药动学特征。方法大鼠灌胃给予IDM-SMEDDS(给药剂量按IDM计为8.0 mg/kg),采用HPLC法测定IDM在大鼠血浆中的药物浓度,以IDM原料药制备混悬液作为参比,绘制两者血药浓度-时间曲线,DAS Ver2.0药动学软件计算药动学参数。结果 IDM-SMEDDS的药动学过程符合二室模型,权重因子为1/C2,IDM混悬液的药动学过程符合一室模型,权重因子为1/C^2;大鼠口服IDM-SMEDDS的C_(max)为42.56μg/m L、T_(max)为1 h、AUC0-48 h为814.25(μg·h)/m L,口服IDM混悬液的C_(max)为9.72μg/m L、T_(max)为6 h、AUC0-48 h为134.57(μg·h)/m L。结论自微乳化给药系统可以提高吲哚美辛的口服生物利用度。Objective To study the pharmacokinetics of indomethacin oral self-microemulsifying drug delivery system（ IDM-SMEDDS） in rats.Methods IDM-SMEDDS was given to rats by oral administration（ 8.0 mg/kg）.HPLC method was used to determine the plasma concentration of IDM.The plasma concentration-time profiles were obtained in contrast with indomethacin suspension.The pharmacokinetic parameters were calculated by using DAS ver2.0 as pharmacokinetic software.Results Pharmacokinetics of IDM-SMEDDS was accord with two-compartment model with the weight factor of 1/C2.IDM suspension was accord with one-compartment model with the weight factor of 1/C2.After given IDM-SMEDDS,the Cmaxwas42.56 μg/m L,Tmax was 1 h,and AUC0-48 hwas 814.25（ μg·h）/m L.After given self-made IDM suspension,the Cmax was 9.72 μg/m L,Tmaxwas 6 h,and AUC0-48 hwas 134.57（ μg·h）/m L.Conclusion The selfmicroemulsifying drug delivery system can increase the oral bioavailability of indomethacin.

关 键 词：吲哚美辛 自微乳化给药系统 药动学参数 

分 类 号：R965[医药卫生—药理学]