国产与进口拉西地平片剂人体药动学研究

 目的：测定国产与进口拉西地平片剂的血药浓度，进行药动学参数比较。方法：8名健康志愿者，随机交叉，单剂量口服国产和进口拉西地平片12 mg,用HPLC测定不同时间的血药浓度，用MCPKP软件进行拟合处理，并计算药动学参数。结果：国产和进口片均符合开放一室模型，T_max,c_max,AUC_0～∞,Ka,K,T_1/2K,Vd,Cl分别为1.68±0.26 h和1.38±0.33 h,1.41±0.58 ng/ml和2.90±0.69 ng/ml，10.32±1.33 (μg·h)/L和12.03±2.29 (μg·h)/L，2.01±0.81/h和2.06±1.19/h,0.19±0.11/h和0.40±0.10 h,4.39±1.84 h和1.86±0.51 h,7.23±2.85 L和2.71±0.65 L,1.18±0.13 L/h和1.04±0.20 L/h。结论：药动学参数经统计学分析，两者之间的T_1/2K、T_max、c_max、Vd有显著性差异(P＜0.05)，而AUC_0～∞和Cl无显著差异(P＞0.05)。

Pharmacokinetics of domestic and foreign lacidipine tablets

OBJECTIVE:To determine the blood concentration of domestic and foreign lacidipine tablets,and compare their pharmacokinetic parameters.METHOD:A randomized crossover study on the pharmacokinetics of lacidipine tablets at a single oral dose of 12 mg was conducted in 8 healthy volunteers.The data of plasma levels determined by HPLC were fitted with MCPKP program on computer.RESULTS:The pharmacokinetics of the two kinds of tablets were all in accord with single compartment model,and T_max,c_max,AUC_0～∞,Ka,K,T_1/2K,Vd,Cl averaged respectively 1.68±0.26 h and 1.38±0.33 h,1.41±0.58 ng/ml and 2.90±0.69 ng/ml,10.32±1.33 (μg·h)/L and 12.03±2.29 (μg·h)/L,2.01±0.81/h and 2.01±1.19/h,0.19±0.11/h and 0.40±0.10/h,4.39±1.84 h and 1.86±0.51 h,7.23±2.85 L and 2.71±0.65 L,1.18±0.13 L/h and 1.04±0.20 L/h.CONCLUSION:Statistical analysis showed significant difference between domestic and foreign tablets for T_max,T_1/2K,c_max and Vd(P＜0.05),but no significant difference between AUC_0～∞ and Cl(P＞0.05).