丙戊酸镁缓释片体外释药特性及体内相对生物利用度的研究  

Studies on dissolution and relative bioavailability of sustained-release magnesium valproate tablet

作　　者：钟硕宇[1] 唐敦立 胡良红[1] 唐铁军 邓英波[1] 尹文乐 

机构地区：[1]湖南医药工业研究所,长沙410014 [2]湖南湘中制药有限公司,邵阳422000

出　　处：《中国医学生物技术应用》2004年第2期17-21,共5页The Chinese Academic Medical Magazine of Organisms

摘　　要：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 prepare sustained-release magnesium valproate tablet (test drug)and evaluate its in vitro drug release property and bioequivalence in human . METHODS:Selected an optimal formulation and technology by dissolution experiment and studied on relative bioavailability in 12 healthy male volunteers by be given single dose of test drug and reference drug(magnesium valproate tablet). RESULTS :The release rate of the prepared tablet conformed to Higuchi equation and was not affected by the pH of the solution, drug was sustained released in vitro over 8h . the pharmacokinetic parameters were as follow : Cmax,30.0±4.6ug · ml-1; Tmax , 11.5±4.8h ; T1/2,17.8±4.6h; F , 95±8% .CONCLUSION:The test drug had sustained -release property and relative bioavailability 95±8%.

关 键 词：丙戊酸镁 缓释片 释放度 释药动力学 生物利用度 

分 类 号：R969[医药卫生—药理学]