液相色谱/质谱联用法测定国产辛伐他汀胶囊人体相对生物利用度

Study on Relative Bioavailability of Simvastain Capsule by LC /MS in Healthy Volunteers

目的:建立辛伐他汀血浆中药物浓度的液质联用测定方法,研究其在人体的药代动力学及生物等效性。方法:18名健康男性受试者随机自身交叉给药,分别口服单剂量国产辛伐他汀胶囊剂和进口片剂20mg。用液相色谱/质谱联用测定血浆中辛伐他汀在人体内的浓度。结果;国产辛伐他汀胶囊剂和进口片剂主要药代动力学参数为:t_(max)分别为2.09±0.41h和2.13±0.47h,C_(max)分别为4.66±2.23μg·L^(-1)和4.71±2.45μg·L^(-1),AUC_(0-t)分别为19.42±3.99μg·h·^(-1)和19.76±4.13μg·h·L^(-1)。国产辛伐他汀胶囊剂的相对生物利用度为(98.3±10.8)％。结论:经统计学分析,国产辛伐他订胶囊剂和进口片剂具有生物等效性。

OBJECTIVE: To develop a LC/MS method for determining simvastain in human plasma and to study pharmacokinetics and relative bioavailability of simvastain in healthy Chinese volunteers . METHODS: A single oral dose of 20mg domestic capsule and imported tablet were given to 18 healthy volunteers in a randomized crossover study. Simvatatin concentration in plasma were determined by LC/MS method. The pharmacokintics and bioavailability were studied. RESULTES: The pharmacokinetics parameters of domestic capsule and imported tablet: tmax were 2.09 ± 0.41 h and 2.13 ± 0.47 h ; Cmax were 4.66 ± 2.23μg.L-1 and 4.71± 2.45 μg.L-1, AUC0-t were 19.42 ± 3.99 μg.h.L-1 and 19.76 ± 4.13 μg.h.L-1, The relative bioavailability of domestic to imported tablets was (98.3 ± 10.8)%. CONCLUSION: There were no statistically significant difference between the two parameters. The results demonstrated that two preparations were bioequivalent.