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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。
Twenty healthy volunteers were randomized to receive oral administration of glipizide (trial and reference) tablets for relative bioavailability in humans. Methods: HPLC-UV method and internal standard method were used to detect the plasma concentration and pharmacokinetic analysis. Results: The curves of the drugs obtained by the CAPP software fit the one-compartment open model. The main pharmacokinetic parameters of glipizide tablets and reference tablets were: T1 / 2k (h): 2.68 ± 0.46 and 2.71 ± 0.46; Cmax (μg · L-1 ): 622.53 ± 136.96 and 620.95 ± 117.36; Tmax (h): 1.93 ± 0.18 and 1.95 ± 0.15; MRT (h): 5.94 ± 0. 37 and 5.96 ± 0.45; AUC0-16 (μg · h · L-1): 2848.24 ± 553.24 and 2962.38 ± 530.13, respectively; these parameters were shown by ANOVA to be insignificant ( P <0.05). The relative bioavailability (F%) of the test tablets versus the reference tablets was: 97.11 ± 11.06. CONCLUSION: The lnAUC, lnCmax and lnTmax of the two groups showed no significant difference by ANOVA under cross-over test. The bioequivalence of the two tablets was proved by double unilateral test.