硝苯地平缓释微丸在Beagle犬体内的药动学及生物等效性  

Pharmacokinetics and bioequivalence of Nifedipine Sustained-release Pellets in Beagle dogs

作　　者：肖正林 丁劲松[2] XIAO Zhenglin;DING Jinsong(Department of Pharmacy,Xiangtan Central Hospital,Xiangtan 411100,China;College of Pharmaceutical Sciences,Central South University,Changsha 410013,China)

机构地区：[1]湘潭市中心医院药学部,湘潭411100 [2]中南大学药学院,长沙410013

出　　处：《西北药学杂志》2018年第1期67-71,共5页Northwest Pharmaceutical Journal

摘　　要：目的研究硝苯地平缓释微丸在犬体内的药动学,并评价其生物等效性。方法 6只Beagle犬随机分为2组,采用自身交叉单剂量口服硝苯地平缓释微丸和上市产品硝苯地平缓释胶囊(Coracen~),剂量均为20mg,采用LC-MS/MS法,以地西泮为内标,测定血药浓度,并对其药动学参数和生物等效性进行研究。结果硝苯地平缓释微丸和Coracen~的t1/2为5.03±1.16和4.67±1.02h,tmax为3.83±0.41和3.67±0.52h,AUC0~24h为164.99±20.32和155.41±23.43ng·h·mL^(-1),Cmax为27.11±2.87和28.72±4.88ng·mL^(-1)。与Coracen~相比,硝苯地平缓释微丸主要药动学参数差异均无统计学意义(P>0.05),双单侧t检验显示,硝苯地平缓释微丸的lnAUC0~24h和lnCmax的t1和t2均大于临界值t0.95(4);(1-2α)置信区间分别为88.3%~121.6%和79.6%~133.5%,两制剂生物等效。结论硝苯地平微丸缓释效果良好,与上市产品Coracen~生物等效。To assess the relative bioavailability and bioequivalence of Nifedipine Sustained-release Pellets in beagle dogs.6 beagle dogs were orally administrated a single dose of 20 mg of Nifedipine Sustained-release Pellets and Coracen R after randomly divided into 2 groups.The crossover dose was given after 1 week wash-out.The blood samples were determined by an LC-M S/M S method with diazepam as internal standard,and the pharmacokinetic parameters and bioequivalence were studied.The main pharmacokinetic parameters of Nifedipine Sustained-release Pellets and Coracen R were as follows:t1/2 5.03土1.16 and 4.67士1.02 h;tmax 3.83±0.41 and 3.67士0.52 h;AUC0-2h 164.9 9±2 0.32 and 155.41士23.43 ng.h.mL1;Cmax 27.11土2.87 and 28.72土4.88 ng.mL 1.Compared with Coracen R,the main pharmacokinetic parameters of Nifedipine Sustained-release Pellets showed no different significantly(P>0.05),two one-sided test and(l-2 a)confidence intervals demonstrated both formulations were bioequivalence.The release and adsorption in vivo of Nifedipine Sustained-release Pellets were similar to Coracen R,and they were bioequivalent.

关 键 词：硝苯地平 缓释微丸 药动学 生物等效性 LC-MS/MS 

分 类 号：R945[医药卫生—微生物与生化药学]