辛伐他汀缓释片在比格犬体内的药动学及生物等效性研究  

Study on Pharmacokinetics and Bioequivalence of Simvastatin Sustained Release Tablets in Beagle Dogs

作　　者：赵丽华[1] 徐德琴[1] 王玉鹏[1] 

机构地区：[1]武警安徽省总队医院药剂科,合肥市230041

出　　处：《中国药房》2010年第25期2347-2349,共3页China Pharmacy

摘　　要：目的:研究辛伐他汀缓释片在比格犬体内的药动学和生物等效性。方法:将6只比格犬随机分成2组,分别单剂量灌服20 mg辛伐他汀缓释片(受试制剂)和市售辛伐他汀片(参比制剂),不同时间采集血样,采用液相- 质谱- 质谱联用法测定比格犬体内的血药浓度并计算药动学参数。结果:参比制剂与受试制剂的C_(max)分别为(23.461±6.043)、(13.942±3.236)ng.mL^(-1);t_(max)分别为(2.158±0.396)、(4.116±1.145 3)h;t_(1/2) 分别为(4.564±0.645)、(8.143±0.679)h;AUC_(0～24 h) 分别为(118.647±31.989)、(129.977±29.853)ng.h.mL^(-1)。结论:受试制剂与参比制剂在吸收速率方面具有显著差异,二者不具有生物等效性。OBJECTIVE：To study pharmacokinetics and bioequivalence of Simvastatin sustained release tablets in healthy beagle dogs.METHODS：6 beagle dogs were randomized into two groups.They received oral single dose of Simvastatin sustained release tablets 20 mg（test tablet） or Simvastatin tablets for sale（reference tablet）.Plasma samples were collected at different time points.Plasma concentration of simvastatin acid was determined by LC-MS/MS and pharmacokinetic parameters were calculated.RESULTS：The pharmacokinetic parameters of reference tablet vs.test tablet were as follows：Cmax：（23.461±6.043） ng·mL^-1 vs.（13.942±3.236） ng·mL^-1;tmax：（2.158±0.396） h vs.（4.116±1.145 3） h;t1/2：（4.564±0.645） h vs.（8.143±0.679） h;AUC0～24 h：（118.647±31.989） ng·h·mL^-1 vs.（129.977±29.853） ng·h·mL^-1.CONCLUSIONS：The absorption rate of test tablet is different from that of reference tablet.The two kinds of tablets are not bioequivalent.

关 键 词：辛伐他汀缓释片 药动学 生物等效性 液相-质谱-质谱联用法 

分 类 号：R969.1[医药卫生—药理学] R972.6[医药卫生—药学]