HPLC法测定阿仑膦酸钠的尿药浓度及其生物等效性研究

Urine Drug Level Determined by HPLC and the Bioequivalence of Alendronate Sodium Tablets in Healthy Volunteers

目的:研究阿仑膦酸钠片的人体生物等效性。方法:采用双制剂、双周期、自身交叉对照的方法,同时进行阿仑膦酸钠片10mg(第1组)和70mg(第2组)2种规格的生物等效试验,每个规格再随机分为2组,口服受试制剂和参比制剂。采用高效液相色谱法测定48h内不同时间段尿药排泄量,绘制平均尿药排泄率-时间曲线,用DAS软件计算药动学参数及相对生物利用度。结果:尿药累积排泄量90%置信区间为参比制剂的相应参数:第1组为82.4%～122.6%,第2组为85.4%～124.6%;最大排泄率90%置信区间为参比制剂的相应参数:第1组为80.3%～131.5%,第2组为82.3%～136.5%。结论:2种规格的受试制剂与参比制剂在体内生物等效。

OBJECTIVE： To study the bioequivalence of Alendronate Sodium Tablets in healthy volunteers. METHODS： According to a paired and cross-over design, a bioequivalence test was performed on two different alendronate sodium tablets, 10 mg （Group 1） and 70 mg （Group 2）. Then each group was subdivided into two groups, i.e. test preparation and reference preparation. The urine concentrations of alendronate at different time point within 48 h were determined by HPLC and the urine excretion rate - time curve was drawn, and the DAS software was used to compute the pharmacokinetic parameters and the relative bioavailability of the tested formulation. RESULTS： The 90% confidence intervals of urine excretion rate of the tested formulations were 82.4% -122.6% （Group 1） and 85.4% -124.6% （Group 2）, respectively and the maximum excretory rates were 80.3% -131.5% （Group 1） and 82.3-136.5% （Group 2）, respectively, compared with the reference formulations. CONCLUSION： The two different Alendronate Sodium Tablets and their respective reference formulations were proved to be bioequivalent in healthy volunteers.