健康志愿者消糖灵丸中格列本脲的人体相对生物利用度研究

目的评价健康志愿者消糖灵丸中格列本脲的人体相对生物利用度并与胶囊剂比较其生物等效性。方法 18名男性健康志愿者随机分组、自身交叉对照单剂量口服消糖灵丸和胶囊,建立HPLC-荧光法测定血浆中格列本脲的质量浓度。结果含格列本脲4.2mg的受试制剂和参比制剂的主要药动学参数如下:达峰时间tmax分别为(2.56±0.38)和(2.50±0.32)h;血药质量浓度峰值Cmax分别为(84.68±27.27)和(88.93±17.58)ng·mL-1;药时曲线下面积AUC(0→10)分别为(360.45±101.18)和(364.26±82.39)ng·h·mL-1。2种制剂的药物动力学参数差异均无统计学意义(P>0.05),受试制剂的相对生物利用度(F)为98.30%±10.82%。结论受试制剂与参比制剂具有生物等效性,消糖灵丸作为迟效制剂进行等效性评价应考虑更多相关因素。

Study on the relative bioavailability of glibenclamide in Concentrated Pills of Xiaotangling in healthy volunteers

Objective To evaluate the relative bioavailability of glibenclamide in Concentrated Pills of Xiaotangling and to compare the reference bioequivalence with capsules in healthy volunteers.Methods 18 male healthy volunteers orally took a single dose of 4.2 mg glibenclamide in Concentrated Pills of Xiaotangling and Xiaotangling Capsules in randamized self-crossover ways.The plasma concentrations of glibenclamide determined by RP-HPLC with a fluorescent detector.Results The main pharmacokinetic parameters of reference and test drugs were as follows:tmax(2.56±0.38) and(2.50±0.32) h;Cmax(84.68±27.27) and(88.93±17.58) ng·mL-1;AUC(0→10)(360.45±101.18) and(364.26±82.39) ng·h·mL-1,respectively.There was no statistical difference between glibenclamide in Concentrated Pills of Xiaotangling and Capsules in pharmacokinetic parameters(P>0.05).The relative bioavailability of glibenclamide in Concentrated Pills of Xiaotangling was 98.30%±10.82%.Conclusion The two preparations of glibenclamide in reference and test drugs were bioequivalence.The characteristics of the delayed-action preparation should be paid much attention.