磷酸苯丙哌林人体药代动力学及其制剂的相对生物利用度研究

Pharmacokinetics of Benproperine Phosphate and Relative Bioavailability of Its Preparations in Healthy Volunteers

本文首次报道了测定苯丙哌林血浆浓度的高效液相色谱法及该药在人体内的药代动力学行为。绘制了10名健康男性受试者服用磷酸苯丙哌两种制剂60mg（以苯丙哌林计）后的血浆浓度-时间曲线，用TopFit2．0软件进行房室模型拟合，结果表明苯丙哌林体内药代动力学过程符合二室模型。磷酸苯丙哌林分散片和胶囊的Tmax分别为1.76±0.29h和1.80±0.41h，Cmax分别为479.4±171.5和456.4±173.9μg·L－1；AUC0-t；为4309.4±1549.9和4119.5±2018.8μg·L-1·h。统计检验表明，10名受试者服用两种制剂后的药代动力学参数无显著性差异，具有生物等效性。

A HPLC method was developed to determine benproperine in human plasmaand the pharmacokinetic behavior of benproperine was reported for the first time. Theplasma concentrations of benproperine in ten healthy volunteers after an oral dose of 60mg of two benproperine preparations were determined and concentration-time profileswere shown to fit a two compartment model. Pharmacokinetic parameters were calculatedwith the aid of TopFit 2.0 programme. Parameters of benproperine phosphate dispersibletablet and capsule were obtained as follows: Tmax were 1 .76±0.29 and 1.80±0.41 h,Cmax were 479.4±171 .5 and 456.4±173.9μg·L'-1 AUC0-t were 4309.4±1549.9and 4119.5±2018.8μg· L-1·h, respectively. There was no statistically significantdifference for benproperine between the two formulations on pharmacokinetic parameters.