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目的：比较单次口服两种阿尼西坦制剂在健康人体内的药代动力学过程，并对两制剂的生物等效性做出评价。方法：１８名健康受试者交叉口服单剂量阿尼西坦颗粒剂（Ｔ）和阿尼西坦胶囊（Ｒ）４００ｍｇ后，用ＨＰＬＣ法测定其主要活性代谢物对甲氧基苯甲酰氨基丁酸（ＡＢＡ）的经时血药浓度，进行药代动力学和生物利用度研究。结果：试验结果表明，两制剂的ＡＢＡ血药浓度时间曲线符合一级吸收一级消除的一房室动力学模型，主要药代动力学参数ｔｍａｘ。分别为２２．７２± １１．７８、２８．５０± ７．７４ｍｉｎ；Ｃｍａｘ分别为 １５．０９± ３．４４，１２．２０± ３．６３ｍｇ·Ｌ－１；ｔ１／２ｋｅ分别为２２．８８±６．５４，３４．８４± １３．５０ｍｉｎ。ＡＵＣ０ｔ 分别为７５５．２１± １２４．３０、７７８．４５± １０６．０９ｍｇ·ｍｉｎ·Ｌ－１（Ｔ和 Ｒ）。相对生物利用度为 ９７．８３％± １５．９６％。结论：两种阿尼西坦制剂具有生物等效。
OBJECTIVE: To compare the pharmacokinetics of two single-dose aniracetam preparations in healthy volunteers and to evaluate the bioequivalence of the two preparations. Methods: Eighteen healthy volunteers were given oral administration of aniracetam granule (T) and aniracetam capsule (R) 400 mg. The main active metabolites p-methoxybenzamido Butyric acid (ABA) over time plasma concentration, pharmacokinetics and bioavailability studies. Results: The experimental results showed that the ABA blood concentration time curves of two preparations accord with the one-compartment kinetic model of first-order absorption elimination and the main pharmacokinetic parameter tmax. Respectively, 22.72 ± 11.78,28.50 ± 7.74min; Cmax were 15.09 ± 3.44,12.20 ± 3.63mg · L-1; t1 / 2ke were 22.88 ± 6.54, 34.84 ± 13.50 min. AUC0t was 755.21 ± 124.30, 788.45 ± 106.09 mg · min · L-1 (T and R), respectively. The relative bioavailability was 97.83% ± 15.96%. Conclusions: Two aniracetam formulations are bioequivalent.