国产与进口拉西地平片剂人体药动学研究

Pharmacokinetics of domestic and foreign lacidipine tablets

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１２ｍｇ，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±０．２６ｈ和１．３８±０．３３ｈ，１．４１±０．５８ｎｇ／ｍｌ和２．９０±０．６９ｎｇ／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±０．１０ｈ，４．３９±１．８４ｈ和１．８６±０．５１ｈ，７．２３±２．８５Ｌ和２．７１±０．６５Ｌ，１．１８±０．１３Ｌ／ｈ和１．０４±０．２０Ｌ／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）。

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 Tmax ,Cmax,AUC0～∞,Ka,K,T1/2K,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/hand 2.01±1.19/h,0.19±0.11/h and 0.40±0.10/h,4.39 ±1.84h and1.86±0.51h,7.23±2.85Land2.71±0.65L,1.18±0.13L/hand1.04±0.20L/h.CONCLUSION:Statistical analysis showed significant difference between domestic and foreign tablets for Tmax ,T1/2k,Cmax and Vd(P<0.05),but no significant difference between AUC0～∞and Cl(P>0. 05).