格列吡嗪片剂对20名健康志愿者的人体相对生物利用度研究

The Relative Bioavailabity of Glipzide Tablets in 20 Healthy Volunteers

２０名健康志愿者随机交叉给药先后一次口服格列吡嗪（受试和参比）片剂进行人体相对生物利用度研究。方法：采用ＨＰＬＣ—ＵＶ法和内标法定时检测其血药浓度，进行药代动力学分析。结果：经ＣＡＰＰ软件拟合所得的药时曲线均符合一室开放模型。格列吡嗪受试片与参比片的主要药动学参数分别为：Ｔ１／２ｋ（ｈ）：２．６８±０．４６和２．７１± ０．４６； Ｃｍａｘ（μｇ·Ｌ－１）： ６２２．５３ ± １３６．９６和６２０．９５ ± １１７．３６； Ｔｍａｘ（ｈ）： １．９３±０．１８和１．９５±０．１５；ＭＲＴ（ｈ）：５．９４±０．３７和５．９６±０．４５； ＡＵＣ０－１６（μｇ·ｈ·Ｌ－１）：２８４８．２４±５５３．２４和２９６２．３８±５３０．１３；这些参数经方差分析证明无显著性差异（Ｐ＜０．０５）。受试片剂对参比片剂的相对生物利用度（Ｆ％）为： ９７．１１±１１．０６。结论：两者的ｌｎＡＵＣ、ｌｎＣｍａｘ、ｌｎＴｍａｘ经交叉试验下的方差分析法证明无显著性差异，经双单侧检验证明两种片剂具有生物等效性。

OBJECTIVE:A single dose of 10 mg glipizide test tablet or its reference tablet was given to 20 healthy male volunteers in a randomized cross-over study. METHODS: The pharmacokinetics and bioavailability of test glipizide tablets were compared with reference glipizide tablets. Plasma levels of glipizide were detected by HPLC-UV method. RESULTS: It was found that the plasma concentration-time curves of the two preparations were fitted to a one compartment model. The parameters of the two formulations for glipizide: Cmax(μg＠·ml-1) were 622.53 ± 139.96 and 620.95 ± 1 17.36, Tmax (h)1.93 ± 0.18and 1.95 ± 0.15; respectively. MRT(h).5.74 ± 0.37 and 5.96 ± 0.45, AUC0-16(μg· h· L-1): 2848.24 ± 553.24 and 2962.38 ± 530. 13; The relative bioavailability (%) of test tablets was 97. 11 ± 11 .06. CONCLUSION: There were no significant difference between pharmacokinetic parameters for test and reference tablets. It was demonstrated the two preparations were bioequivalent by one two-sided tests.