硝苯地平控释胶囊在Beagle犬体内的药动学研究  

Pharmacokinetics of nifedipine controlled-release capsules in Beagle dogs

作　　者：张杰[1] 左飞[1] 柯清华[1] 丁劲松[2] 

机构地区：[1]荆门市第一人民医院,湖北荆门448000 [2]中南大学药学院,长沙410013

出　　处：《中南药学》2014年第9期873-875,共3页Central South Pharmacy

摘　　要：目的评价自制硝苯地平（NF）控释胶囊在Beagle犬体内的药动学,并对其体内外相关性进行研究。方法 6只健康Beagle犬随机分成2组,分别单剂量服用实验制剂（硝苯地平控释胶囊）和参比制剂（拜新同渗透泵片）各30 mg,一周后交叉给药。采用HPLC法,以尼群地平（NT）为内标测定犬给药后不同时间的血药浓度,用以估算药动学参数和相对生物利用度。结果实验制剂与参比制剂的主要药动学参数分别为：Cmax（21.79±8.11）、（21.99±3.97）ng·mL-1;tmax（8.32±1.51）、（9.31±1.02）h;AUC0～t（337.42±84.44）、（348.65±56.25）ng·h·mL-1;t1/2（9.27±1.75）、（8.96±1.73）h;相对生物利用度为（96.8±7.34）%;体内外相关性r=0.944。结论自制硝苯地平控释胶囊具有明显的控释特性,体内外相关性良好。Objective To evaluate the relative bioavailability and bioequivalence of nifedipine controlled-release capsules in Beagle dogs. Methods Six healthy dogs were orally given a single dose of 30 mg of test formulation and reference formulation （Adalat GITS ） after being randomly divided into 2 groups. The crossover dose was taken in one week. The blood samples of the dogs were collected to measure the drug concentration in the blood by HPLC with nitrendipine as the internal standard. The pharmacokinetic parameters and relative bioavailability were deter- mined. Results The pharmacokinetics parameters of test and reference samples were as follows： Cmax （21.79±8.11）、（21.99±3.97）ng·mL-1;tmax（8.32±1.51）、（9.31±1.02）h;AUC0～t（337.42±84.44）、（348.65±56.25）ng·h·mL-1;t1/2（9.27±1.75）、（8.96±1.73）h; The relative bioavailability of the test formulation was （96.8 ±7.34）%, Suggest- ing an excellent in vitro and in vivo correlation （r = 0.944）. Conclusion Nifedipine controlled-release capsules fea- ture a superior controlled-release profile, and are bioequivalent to the reference formulation.

关 键 词：硝苯地平 控释胶囊 药动学 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学]