双氯芬酸钾双层片与普通片在兔体内的生物等效性

 目的：研究双氯芬酸钾（DP）双层片在兔体内的药动学特征。方法：8只家兔分别单剂量口服DP双层片（Ⅰ）和普通片凯扶兰（Ⅱ）各50 mg，采用高效液相色谱法测定不同时间的血药浓度。经TOPFIT程序拟合，求算药动学参数。结果：Ⅰ和Ⅱ的药动力学参数MRT分别为（19.7±3.0）h和（7.7±0.9）h，t_1/2为（10.6±1.1）h和（3.2±1.0）h，T_max为（8.5±3.0）h和（5.0±1.2）h，C_max为(16.6±3.7) μg·ml^-1和(26.6±4.1) μg·ml^-1，AUC为(266.4±45.1) μg·h·ml^-1和（9237.0±19.1）μg·h·ml^-1。DP双层片和普通片的MRT、t_1/2、T_max、C_max差异有显著性，AUC、CL差异无显著性。体内吸收分数与体外释放度之间线性关系良好，r=0.9885。结论：双层片具有明显的缓释特征，吸收程度与普通片等效。

Pharmacokinetics of diclofenac potassium double-layer tablets in rabbits and in vitro/in vivo correlations

OBJECTIVE To study the pharmacokinetcs of diclofenac potassium double-layer tablet （Ⅰ） in rabbits .METHODS A single oral dose of 50mg （Ⅰ）and 50mg odinary tablet kaifulan（Ⅱ） was given to 8 rabbits respectively,drug concentration in plasma was determined by HPLC method.The pharmacokinetics parameters were fitted and caculated by Topfit program.RESULTS The pharmacokinetic parameters of （Ⅰ）and （Ⅱ）were respectively as follows: MRT (19.7±3.0) and (7.7±0.9) h，t_1/2 (10.6±1.1) h and (3.2±1.0) h，T_max (8.5±3.0) h and (5.0±1.2) h，C_max(16.6±3.7) μg·ml^-1 and (26.6±4.1) μg·ml^-1，AUC (266.4±45.1) μg·h·ml^-1 and (237.0±19.1) μg·h·ml^-1. MRT、t_1/2、T_max、C_max of （Ⅰ）were different from （Ⅱ） significantly. AUC and CL of （Ⅰ） and （Ⅱ） had no significant difference.Correlation between absorption rate in vivo and dissolution rate in vitro was fine(r=0.9885).CONCLUSIONS （Ⅰ） had marked characteristics of sustained release.