坎地沙坦酯自微乳软胶囊和普通胶囊在家兔中相对生物利用度研究  

Relative bioavailability of candesartan cilexetile self-microemulsifying soft capsules and common capsules in rabbits

作　　者：李蓉蓉[1] 李小莉[1] 祝红达[1] 刘明星[1] 

机构地区：[1]湖北工业大学生物工程学院制药工程系,武汉430068

出　　处：《中南药学》2012年第11期808-811,共4页Central South Pharmacy

基　　金：武汉市科技局攻关项目(No.200960323126)

摘　　要：目的研究坎地沙坦酯自微乳软胶囊和普通胶囊在家兔体内的药动学及相对生物利用度。方法以家兔为实验动物,采用高效液相色谱法测定坎地沙坦酯自微乳软胶囊和普通胶囊单剂量口服给药后家兔的血药浓度变化。用3P97软件统计计算药动学相关参数和相对生物利用度。结果坎地沙坦酯自微乳软胶囊:AUC0～24为735.005μg.h L-1,Cmax为90.68μg.mL-1,tmax为3.5h;普通胶囊:AUC0～24为542.839μg.h.L-1,Cmax为60.72μg.mL-1,tmax为4.5h。软胶囊相对生物利用度为135.4%。结论坎地沙坦酯自微乳软胶囊和普通胶囊均符合二室模型,自微乳软胶囊较普通胶囊具有较高的生物利用度。Objective To investigate the pharmacokinetics and relative bioavailability of candesartan cilexetile self-microemulsifying soft capsules and common capsules in rabbits.Methods Rabbits were respectively treated with single dose candesartan cilexetile self-microemulsifying soft capsules and common capsules.The concentration of candesartan in rabbit serum was determined by HPLC.Pharmacokinetic data were processed with 3P97 software.The pharmacokinetic parameters and relative bioavailability were calculated.Results For candesartan cilexetile self-microemulsifying soft capsules： AUC0～24=735.005 μg ？ h ？ L-1,Cmax=90.68 μg ？ mL-1,tmax=3.5 h;for common capsules： AUC0～24 =542.839 μg ？ h ？ L-1,Cmax=60.72 μg ？ mL-1,tmax=4.5 h.The relative bioavailability of soft capsules as compared to common capsules was 135.4%.Conclusion The pharmacokinetics of candesartan cilexetile self-microemulsifying soft capsules and common capsules are in accordance with 2 compartment models,and the relative bioavailability of capsules is higher than that of common capsules.

关 键 词：坎地沙坦酯 自微乳 软胶囊 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学] R944.5[医药卫生—药学]