Bialer M, Hussein Z, Dubrovsky J, Raz I, Abramsky O
Isr J Med Sci. 1984 Jan;20(1):46-9.
The pharmacokinetics and bioavailability of valproic acid (VPA) were compared in six healthy volunteers after oral administration of the drug as follows: 1 g in standard tablet form, 1 g in enteric-coated tablet form, and 0.8 g in gelatin-capsule form. Following the administration of standard tablets, VPA concentrations reached a peak mean +/- SD of 105.4 +/- 9.0 micrograms/ml at 1 h and declined monoexponentially, with a terminal half-life of 14.9 +/- 2.4 h. Following the administration of the capsule, the serum concentration reached a peak of 82.1 +/- 14.8 micrograms/ml at 4 h. Following the administration of an enteric-coated tablet, there was an average time lag of 2 h with a delayed peak serum concentration of 93.5 +/- 13.1 micrograms/ml at 6 h. An identical terminal half-life of VPA was obtained for the three oral formulations. The bioavailability of the three VPA formulations was not significantly different, and it may be concluded that these formulations are bioequivalent.
在六名健康志愿者口服以下形式的丙戊酸（VPA）后，对其药代动力学和生物利用度进行了比较：标准片剂形式的1 g、肠溶片剂形式的1 g以及明胶胶囊形式的0.8 g。服用标准片剂后，VPA浓度在1小时时达到峰值，平均±标准差为105.4±9.0微克/毫升，随后呈单指数下降，终末半衰期为14.9±2.4小时。服用胶囊后，血清浓度在4小时时达到峰值82.1±14.8微克/毫升。服用肠溶片剂后，平均有2小时的时间延迟，血清浓度在6小时时出现延迟峰值，为93.5±13.1微克/毫升。三种口服制剂的VPA终末半衰期相同。三种VPA制剂的生物利用度无显著差异，可以得出结论，这些制剂具有生物等效性。
