缬沙坦分散片的人体药动学与生物等效性研究

Pharmacokinetics and Bioequivalence of Valsartan Dispersed Tablet in Healthy Volunteers

目的研究缬沙坦分散片在健康人体内的药动学,评价两种制剂的生物等效性。方法采用随机自身交叉双周期设计方法,将20例健康男性受试者随机分为2组,分别单次交叉口服缬沙坦受试制剂或参比制剂80mg,采用高效液相色谱-荧光检测法测定血浆中缬沙坦的浓度,计算其药动学参数和相对生物利用度,评价两制剂的生物等效性。结果受试制剂和参比制剂缬沙坦药代动力学参数:Cmax分别为(2536±1293)ng·mL-1和(2457±1413)ng·mL-1,tmax分别为(2.5±1.1)h和(2.3±0.7)h,t1/2分别为(5.9±1.8)h和(5.8±1.1)h,AUC0～30h分别为(14984±7155)ng.h.mL-1和(14390±7040)ng.h.mL-1。受试制剂的相对生物利用度为(115.6±52.5)%。结论缬沙坦的两制剂具有生物等效性。

OBJECTIVE To investigate pharmacokinetic and bioequivalence of valsartan dispersed tablet in healthy volunteers. METHODS Twenty volunteers were randomly divided into 2 groups. A single oral dose of 80 mg of test or reference tablets was delivered to each volunteer in an open crossover test. The plasma concentration of valsartan was determined by HPLC fluorescence detection. Based on the parameters of pharmacokinetic and relative bioavailability, the bioequivalence of valsartan was evaluated. RESULTS Cmax was （2 536 ±1293）ng·mL^-1 and （2 457 ±1 413）ng·mL^-1, tmax was （2.5 ±1.1） h and （2.3 ±0.7） h , t1/2 was （5.9±1.8） h and （5.8 ±1.1） h, AUC0-30h in 2 groups was （14 984±7 155） ng·h·mL^-1 and （14 390±7 040）ng·h·mL^-1 in 2 groups respectively. The relative bioavailability of valsartan dispersed tablet was （115.6±52.5）%. CONCLUSION The two preparations of valsartan dispersed tablet and reference tablets are bioequivalent.