西洛他唑片在健康志愿者体内的药动学及生物等效性

Study on the pharmacokinetics and bioequivalence of cilostazol tablets in healthy volunteers

目的:研究国产西洛他唑片在人体的药动学和生物等效性。方法:20名男性健康志愿者随机交叉单剂量口服西洛他唑受试和参比制剂(P letaal)100mg,采用反相高效液相色谱法测定其血药浓度,计算其药动学参数和相对生物利用度,评价两种制剂的生物等效性。结果:西洛他唑受试和参比制剂的主要药动学参数:t1/2分别为(11.9±4.6)h和(11.2±3.0)h,Tm ax分别为(3.7±1.2)h和(4.0±1.2)h,Cm ax分别为(749.2±348.7)μg.L-1和(655.2±222.1)μg.L-1,AUC0-48分别为(10 088.5±4 606.1)μg.L-1.h和(9 259.0±3 511.8)μg.L-1.h,AUC0-∞分别为(10 926.3±4 713.6)μg.L-1.h和(10 183.4±3 540.7)μg.L-1.h,西洛他唑受试制剂的相对生物利用度为(107.5±14.9)%。结论:经统计学分析,两种制剂具有生物等效性。

OBJECTIVE To evaluate the pharmacokinetic profiles and bioequivalence of cilostazol tablets in healthy volunteers. METHOBS A single oral dose of 100 mg cilostazol test and reference tablets was given to 20 male healthy volunteers in a randomized crossover design. Cilostazol plasma concentrations were determined by the reversed-phase high performance liquid chromatography （HPLC） . The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations. RESULTS The main pharmacokinetic parameters of cilostazol test and reference tablets were as follow： t1/2 were （11.9±4.6） h and （11.2±3.0） h, T.Tmax were（3.7 ± 1.2）h and （4.0± 1.2）h , Cmax, were（749.2 ±348. 7）μg·L^-1 and （655. 2±222. 1）μg· L6-1 , AUC0-48 were（10 088. 5 ± 4 606. 1）μg. L^-1 ·h and（9 259. 0 ± 3 511.8） μg. L^-1 ·h, AUC0-∞ were （10 926. 3 ± 4 713.6） μg· L^-1· h and （ 10 183. 4 ± 3 540. 7） μg· L^-1. h, respectively. The relative bioavailability of test tablets was （107. 5 ± 14. 9） %. CONCLUSION The statistical analysis of the results shows that the two preparations are bioequivalent.