西洛他唑片人体生物等效性研究

 目的对国产和进口西洛他唑进行生物等效性研究。方法20例健康志愿者按标准的2×2交叉试验方案设计,分别口服参比制剂或受试制剂各200mg,并采集60h内动态血标本;采用高效液相色谱法测定血清中药物浓度,计算药动学参数,并判定两制剂是否生物等效。结果参比制剂及受试制剂中西洛他唑的主要药动学数据t_max分别为(3.350±1.137)和(3.350±1.089)h,c_max分别为(745.2±208.7)和(732.6±212.9)ng·mL^-1,AUC_0～1分别为(8777±2158)和(8813±2526)ng·h·mL^-1,AUC_0～∞分别为(9366±2038)和(9259±2595)ng·h·mL^-1,t_1/2(ke)分别为(14.251±6.174)和(11.864±3.447)h,Ke分别为(0.05908±0.02871)和(0.06261±0.01566)h^-1;两种制剂的主要药动学参数c_max,AUC_0～t经对数转换后进行方差分析及双单侧检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂西洛他唑片的人体相对生物利用度为(100.52±15.52)%。结论两种制剂生物等效。

Study on bioequivalence of cilostazol table in healthy volunteers

OBJECTIVE To study the bioequivalence of cilostazol tables in healthy volunteers.METHODS 200 mg Test preparation and reference preparation were given to 20 healthy male volunteers in randomized two-way crossover design for the pharmacokinetic and relative bioavailability study. Serum concentrations of cilostazol were determined by RP-HPLC.RESULTS The main pharmacokinetic parameters of the two preparation were: t_max(3.350±1.137) and (3.350±1.089) h, c_max(745.2 ± 208.7) and (732.6±212.9)ng· mL^-1, AUC_0～t (8777±2158) and (8813±2526)ng·h·mL^-1,AUC_0～∞(9366±2038)and(9259±2595)ng·h·mL^-1, t_1/2(Ke)(14.251±6.174) and (11.864±3.447)h, Ke(0.059 08 ± 0.028 71) and (0.062 61 ± 0.015 66)h^-1,respectively. The mean relative bioavailability of test preparation vs reference preparation were (100.52± 15.52)%.CONCLUSION The statistical analysis shows that the two preparations are bioequivlent.