左乙拉西坦缓释片的制备及其Beagle犬体内药动学研究  

Study on Preparation of Levetiracetam Sodium Extended-release Tablet and It's Pharmacokinetics in Beagle Dogs

作　　者：徐兵勇 潘迎锋 平丽[3] 

机构地区：[1]浙江省药品化妆品审评中心,杭州310012 [2]正大青春宝药业有限公司,杭州310012 [3]浙江大学药物安全评价研究中心,杭州310058

出　　处：《中国现代应用药学》2017年第9期1266-1271,共6页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的制备左乙拉西坦缓释片,进行体外释放特性以及Beagle犬体内药动学研究。方法按照筛选处方制备左乙拉西坦缓释片,以市售左乙拉西坦缓释片(Keppra-XR)为参比制剂,采用相似因子(f2)法进行体外释放行为相似度评价;并将自制左乙拉西坦缓释片与市售普通片进行Beagle犬体内药动学参数比较。结果自制左乙拉西坦缓释片与市售左乙拉西坦缓释片体外释放行为相似。市售左乙拉西坦普通片和自制左乙拉西坦缓释片的药动学参数Tmax分别为(1.75±0.50)和(5.50±1.00)h,Cmax分别为(30.33±2.00)和(17.29±3.56)mg·L-1,AUC0-t分别为(186.88±8.83)和(202.50±34.20)mg·L^(-1)·h。结论自制的左乙拉西坦缓释片具有缓释效果。OBJECTIVE To prepare the Levetiracetam extended-release tablet and investigate its pharmacokinetics in Beagle dogs and in vitro release. METHODS Prearation of Levetiracetam extended-release tablet according to optimized prescription, choosed sell products（Keppra-XR） as reference products, evaluation of in vitro release behavior similarity by the similar factor（f_2）. The pharmacokinetic parameters were compared between the self-made extended-release tablet and the sell tablet. RESULTS The self-made extended-release tablet was similar to the reference products in vitro release, Tmax of reference products and self-made extended-release tablet were（1.75±0.50） and（5.50±1.00） h, C_（max） were（30.33±2.00） and（17.29±3.56） mg·L-1, AUC0-t were（186.88±8.83） and（202.50±34.20） mg·L^（-1）·h. CONCLUSION The self-made Levetiracetam extended-release tablet exhibits the sustained release characteristics in vitro.

关 键 词：左乙拉西坦 缓释片 药动学 

分 类 号：R943[医药卫生—药剂学] R969.1[医药卫生—药学]