吲哚美辛缓释胶囊多剂量达稳态时人体药动学与相对生物利用度  

In steady state pharmacokinetics and relative biovailability of indomethacin sustained-release capsule in multiple dose

作　　者：赵语[1] 陈钧[2] 蒋学华[2] 

机构地区：[1]重庆医科大学附属第一医院药剂科,重庆400016 [2]四川大学药学院临床药学教研室,四川成都610041

出　　处：《医学信息（西安上半月）》2005年第3期241-243,共3页Medical Information

摘　　要：目的研究吲哚美辛缓释胶囊在正常人体内的药动学和相对生物利用度。方法采用随机交叉自身对照试验设计,对18名志愿受试者分别PO多剂量给予国产和进口吲哚美辛缓释胶囊,用反相高效液相色谱法测定吲哚美辛达稳态时的血药浓度,以3P97药动学程序进行数据处理。结果两种制剂的Cssmin分别是0.99mg·L-1和1.04 mg·L-1,Cssmin分别是3.69 mg·L-1和3.68mg·L-1,Tmax均为3.44h,AUCo→τ分别为23.49 mg·h·L-1和22.48 mg·h·L-1,波动度DF分别为138.21%±23.10% 和134.53%±28.14%,css分别是1.96 mg·L-1和1.85 mg·L-1;国产吲哚美辛缓释胶囊的相对生物利用度为102.45%;两种制剂的Cssmin、Cssmax、Tmax、AUCo→τ、DF、css、经方差分析和生物等效性检验,均无显著性差异(P>0.05)。结论:两种制剂为生物等效制剂。Objective: To study the pharmacokinetics and relative bioavailability of indomethacin sustained-release capsule(ISRC) in steady state. Methods: The indomethacin concentrations in plasma were determined by reversed-phase HPLC method following multiple oral dose of native and imported ISRC respectively given to 18 volunteers in an open randomized cross-over test. Results: The Cssmin of native and imported product was 0.99mg·L-1 and 1.04 mg·L-1, Cssmin was 3.69 mg·L-1 and 3.68mg·L-1,both of Tmax were 3.44h,AUCo→τ was 23.49 mg·h·L-1和22.48 mg·h·L-1,the degree of fluctuation(DF) was 138.21%±23.10% and 134.53%±28.14% , css was 1.96 mg·L-1和1.85 mg·L-1. The relative bioavailability of native produce was 102.45%. There was no significant difference between the two formulations in the Cssmin?Cssmax?Tmax?AUCo→τ?DF and css (P>0.05). Conclusion The two preparations are bioequivalent.

关 键 词：吲哚美辛缓释胶囊 用药剂量 人体药动学 生物利用度 血药浓度 解热镇痛药 

分 类 号：R971.1[医药卫生—药品] R96[医药卫生—药学]