论文部分内容阅读
目的:研制丙戊酸镁缓释片,并评价其体外释药特性及体内生物等效性。方法:以释放度为主要指标筛选片剂处方及制备工艺,并对12名健康男性受试者进行体内生物利用度研究。结果:以优选的处方,工艺制备的片剂,体外释药性能良好,符合Higuchi方程,持续释药达8h以上。且释药性能稳定,不受溶出介质pH值的影响。其体内药代动力学参数为:Cmax,30.0±4.6ug·ml-1;Tmax,11.5±4.8h;T1/2。17.8±4.6h;F,95±8％。结论:丙戊酸镁缓释片与普通片相比具有缓释特性。相对生物利用度为95±8％。
OBJECTIVE: To develop magnesium valproate sustained release tablets and evaluate its in vitro release characteristics and in vivo bioequivalence. Methods: The drug release rate was taken as the main index to screen the tablet prescription and the preparation process. The bioavailability of 12 healthy male volunteers was studied in vivo. Results: The tablets prepared by the best prescription and technology had good in vitro release performance and conformed to Higuchi equation. The sustained-release tablets reached more than 8h. And drug release performance is stable, not affected by the dissolution medium pH value. The in vivo pharmacokinetic parameters were: Cmax, 30.0 ± 4.6 ug · ml-1; Tmax, 11.5 ± 4.8 h; T1 / 2.17.8 ± 4.6 h; F, 95 ± 8%. CONCLUSION: Magnesium valproate sustained release tablets have sustained release characteristics compared with ordinary tablets. The relative bioavailability was 95 ± 8%.