马来酸氯苯那敏片健康人体药动学和相对生物利用度

Study of relative bioavailability of chlorpheniramine maleate tablets in healthy volunteers

目的研究马来酸氯苯那敏片剂在健康人体内的相对生物利用度。方法采用HPLC法测定18名男性健康志愿者单剂量交叉口服马来酸氯苯那敏片参比制剂和被试制剂8mg后不同时间血浆药物浓度。用3P97药动学软件进行药动学参数计算及生物等效性评价。结果参比和被试制剂的药-时曲线均符合一房室模型,两制剂的主要药动学参数如下Cmax分别为(15.74±7.06)μg·L-1和(14.88±4.40)μg·L-1;tmax分别为(3.9±1.2)h和(4.5±0.8)h;t1/2ke分别为(15.54±3.76)h和(14.49±3.24)h;AUC0-t分别为(248.86±78.52)μg·h·L-1和(245.09±90.77)μg·h·L-1,AUC0-∞分别为(292.64±99.21)μg·h·L-1和(282.04±98.64)μg·h·L-1。与标准参比制剂相比,被试制剂的相对生物利用度F0-t为(104.1±36.1)%,F0-∞为(103.2±35.6)%。结论方差分析与双单侧t检验证明,两种制剂具有生物等效性。

AIM： To study pharmacokinetics and bioavailability of chlorpheniramine maleate tablets in young healthy volunteers. METHODS： The chlorpheniramine concentrations in plasma were determined by HPLC method with UV detector after a single oral dose 8 mg of the reference formulation and the tested formulation were respectively given to 18 volunteers in randomized cross-over test. The pharmacokinetics parameters were calculated by 3P97 software. RESULTS AND CONCLUSION： The concentration-time curves of two formulations fitted to a one-compartment open model. The Cmax, was 15.74 ± 7.06 μg·L^-1 and 14.88 ± 4.40 μg·L^-1, tmax was 3.9 ± 1.2 h and 4.5 ± 0.8 h, t1/2ke was 15.54 ± 3.76 h and 14.49 ± 3.24 h, AUCo-t was 248.86 ± 78.52 μg·h·L^-1 and 245.09 ± 90.77 μg·h·L^-1, AUC0-∞ was 292.64 ± 99.21 μg·h·L^-1 and 282.04 ± 98.64 μg·h·L^-1, respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between two formulations （P 〉 0.05 ）. The relative bioavailability of F0-t and F0-∞ of tested formulation were （104.1 ±36.1）% and （103.2±35.6）%, respectively. The two formulations are bioequivalent.