苯磺酸左旋氨氯地平氯沙坦钾控释片的研制及体内外评价  

Preparation and in vitro/in vivo Evaluation of Levamlodipine Besylate and Losartan Potassium Controlled-release Tablets

作　　者：石其德 冯中 

机构地区：[1]鲁南制药集团新药研发中心,山东临沂273400

出　　处：《中国医药工业杂志》2014年第4期344-348,共5页Chinese Journal of Pharmaceuticals

基　　金：国家火炬计划项目(2010GH021182)

摘　　要：制备了苯磺酸左旋氨氯地平(1)氯沙坦钾(2)控释片,并建立了HPLC法测定制品中的1和2。考察了制品在不同介质中的体外释药行为及在Beagle犬体内的药动学。不同介质中的体外释放数据拟合结果表明,自制控释片在24 h内两种药物均呈零级释放特征。体内结果表明,自制控释片中1和2的相对生物利用度为95.2%和90.6%;1的半衰期由(8.3±2.8)h延长至(15.3±4.7)h,2的半衰期由(3.1±1.8)h延长至(5.1±2.3)h,达到了控释效果。The levamlodipine besylate （1） and losartan potassium （2） controlled-release tablets were prepared. An HPLC method was established for the determination of both drugs in the self-made product. The in vitro release behaviors in different media and the pharmacokinetics in Beagle dogs of the product were also investigated. The fitting results of drug release in vitro showed that both 1 and 2 released from the product within 24 h in different media exhibited a zero-order release profile. The relative bioavailabilities of 1 and 2 were 95.2% and 90.6%, respectively. The t1/2 of 1 and 2 of the self-made product were prolonged to （15.3±4.7） h and （5.1±2.3） h, while those of common prescribed tablets of 1 and 2 were （8.3±2.8）h and （3.1±1.8）h, respectively. It indicated that the self-made product had a controlled-release profile.

关 键 词：苯磺酸左旋氨氯地平 氯沙坦钾 控释片 体内外评价 

分 类 号：R944.9[医药卫生—药剂学]