左乙拉西坦缓释片的制备与体内外相关性研究  

Preparation and in vitro-in vivo correlation in Beagle dogs of levetiracetam sustained-release tablets

作　　者：伍衢[1] 王悦[1] 王永禄[1] 李学明[1] 毛利娟[1] 

机构地区：[1]南京工业大学药学院,南京211816

出　　处：《中国新药杂志》2011年第16期1573-1576,1586,共5页Chinese Journal of New Drugs

基　　金：江苏省高校自然科学基金(09JKB350001);南京工业大学学科基金(39728007)

摘　　要：目的:研制左乙拉西坦缓释片并考察其体外释放及犬体内药动学。方法:以羟丙甲基纤维素,乙基纤维素为混合骨架材料制备日服一次的缓释片,测定其体外释放度和Beagle犬口服单剂量缓释片后血浆中药物的浓度,推算药动学参数。结果:自制缓释片体外释放符合Higuchi模型。左乙拉西坦普通片,上市缓释片和自制缓释片的有关药动学参数如下:t1/2分别为(2.09±0.45),(5.35±0.76),(7.44±1.48)h,T(peak)分别为(1.184±0.38),(3.87±0.37),(4.07±0.56)h,AUC分别为为(175.40±15.47),(240.93±19.73),(251.47±13.22)μg.h.mL-1。结论:自制缓释片具体良好的缓释特性。体外释放和体内吸收有良好的相关性。Objective：To prepare levetiracetam sustained release tablets,and investigate in vitro-in vivo correlation in Beagle dogs.Methods：Mixed HPMC and EC matrix was used to prepare levetiracetam sustained release tablets.The in vitro release characteristics and in vivo pharmacokinetics in dogs of the tablets were investigated.Results：Higuchi model was optimal for the description of drug release profile.The mean elimination half-lives（t1/2） after administration of conventional tablets,reference sustained release tablets and our sustained release tablets were（2.09±0.45）,（5.35±0.76） and（7.44±1.48）h,respectively.The peak levels were（1.184±0.38）,（3.87±0.37） and（4.07±0.56）h;AUCs were calculated to be（175.40±15.47）,（240.93±19.73） and（251.47±13.22）μg·h·mL-1,respectively.Conclusion：The levetiracetam sustained release tablets exhibit the sustained release characteristics in vitro,and show a good correction in vitro release and in vivo absorption.

关 键 词：左乙拉西坦 缓释片 体外释放 体内外相关性 

分 类 号：R943.41[医药卫生—药剂学] R971.6[医药卫生—药学]