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目的 :研究阿尼西坦颗粒剂在正常人体内的药代动力学及相对于胶囊剂的生物利用度。方法 :采用反相高效液相色谱法 ,测定 8名健康男性志愿者自身交叉单剂量口服阿尼西坦颗粒剂和胶囊剂 (60 0mg)经时血药浓度。结果 :用 3p87程序拟和 ,符合一级吸收、单室模型。阿尼西坦胶囊剂和颗粒剂的药代动动力学参数 :Ka分别为(0 0 76± 0 1 9)min 1 、(0 348± 0 0 54)min 1 ;t1 / 2 分别为 (2 2 .69± 2 .45)min、(2 7.78± 1 .50 )min ;Cmax分别为 (61 .2 4±4 .1 5)ng·ml 1 、(76 .2 4± 3 .60 )ng·ml- 1 ;Tmax分别为 (2 2 .94± 1 .66)min、(1 1 .94± 0 .58)min ;AUC分别为 (3735 .78±1 92 .3)ng·min·ml- 1 、(3754 .98± 1 63 .58)ng·min·ml- 1 。经统计学处理 ,两制剂药代动力学参数t1 / 2 无显著性差异(P >0 .0 5) ,Ka、Cmax、Tmax有显著性差异 (P <0 .0 5) ;阿尼西坦颗粒剂相当于胶囊剂的生物利用度为 1 0 0 50 %±2 59%。结论 :经方差分析、配对双单侧t检验 ,两制剂具有生物等效性
OBJECTIVE: To study the pharmacokinetics of aniracetam granules in normal human and its bioavailability relative to capsules. Methods: The anti-phase high performance liquid chromatography (HPLC) was used to determine the serum concentration of Olyizon Granules and capsules (60 mg) administered orally in 8 healthy volunteers. Results: Fitting with 3p87 program, in line with the first-order absorption, single-compartment model. Pharmacokinetic parameters of aniracetam capsules and granules were as follows: Ka = (0 0 76 ± 0 1 9) min 1, (0 348 ± 0 544) min 1; t1 / 2 were 2 .69 ± 2.45) min, (2 7.78 ± 1.50) min, respectively; Cmax were (61.24 ± 4.15) ng · ml 1, (76.24 ± 3.60) ng · Ml-1; Tmax were (2 2 .94 ± 1. 66) min, (1 1 .94 ± 0. 58) min respectively; AUC were (3735.78 ± 1 92.3) ng · min · ml - 1, (3754 .98 ± 1 63 .58) ng · min · ml-1. Statistically, there was no significant difference in the pharmacokinetic parameters t1 / 2 between the two preparations (P> 0.05), Ka, Cmax and Tmax (P <0.05); Aniracetam The bioavailability of granules equivalent to capsules is 100% ± 2 59%. Conclusion: By means of ANOVA, paired double unilateral t test, the two preparations have bioequivalence