格列吡嗪口崩片的人体生物等效性试验

Bioequivalence of glipizide orally disintegrating tablets in healthy volunteers

目的研究格列吡嗪口崩片的人体相对生物利用度和生物等效性。方法健康志愿者20名，随机双交叉单剂量口服格列吡嗪口崩片和格列吡嗪片，剂量均为10mg。分别于服药后24h内多点抽取静脉血；用HPLC法测定血浆中格列吡嗪的浓度。用DAS药动学程序计算相对生物利用度并评价2种制剂生物等效性。结果单剂量口服试验和参比制剂后血浆中的格列吡嗪的ρmax分别为（930．16±171．63）和（915．12±126．11）μg·L^-1；tmax分别为（3．05±0．94）和（3．85±1．39）h；AUC0→24分别为（8220．93±1162．94）和（7927．13±1158．82）μg·h·L^-1；AUC0→∞分别为（8821．76±1323．28）和（8303．96±1239．24）μg·h·L^-1。ρmax、AUC0→24和AUC0→∞的90％可信区间分别为94．82％～107．46％、99．76％～108．10％和101．93％～110．84％。结论试验与参比制剂的人体相对生物利用度为（104．5±12．0）％，两制剂具有生物学等效性。

AIM To study the relative bioavailability and bioequivalenee of glipizide orally disintegrating tablets in healthy volunteers. METHODS A single oral doses （10 mg of tested and reference formulations） were given to 20 healthy volunteers in a randomised crossover study. The concentrations of glipizide in plasma were determined by HPLC. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS After a single dose, the pharmacokinetic parameters for glipizide were as follows： ρmax were （930.16 ± 171.63）μg·L^-1 and （915.12 ± 126.11）μg·L^-1; tmax were （3.05 ± 0.94）h and （3.85 ± 1.39） h; AUC0→24 were （8 220.93 ± 1 162.94）μg·h·L^-1 and （7 927.13 ± 1 158.82）μg·h·L^-1; AUC0→∞ were （8 821.76 ± 1 323.28）μg·h·L^-1 and （8 303.96 ± 1 239.24） μg·h·L^-1 for tested and reference formulations respectively. The 90% confidence interval of ρmax、AUC0→24 and AUC0→∞ of tested formulation were 94.82% - 107.46%、99.76% - 108.10% and 101.93% - 110.84% respectively. CONCLUSION The relative bioavailability is （104.5 ± 12.0） % .The results of the statistic analysis show that the two formulations are bioequivalence.