盐酸贝那普利咀嚼片在犬体内的生物等效性研究  

Study on Bioequivalence of Benazeptil Hydrochloride Tablets in Dogs

作　　者：刘欣[1,2] 魏丽娟 宋婷婷[1,2] 瞿红颖 贾兴[1,2] 耿智霞 魏占勇 邹明[3] 陈杰 

机构地区：[1]河北远征药业有限公司,石家庄050041 [2]河北省兽药工程技术研究中心,石家庄050041 [3]青岛农业大学,山东青岛266000 [4]浙江省余桃市梨洲街道办事处,浙江余桃315400

出　　处：《中国兽药杂志》2017年第11期20-27,共8页Chinese Journal of Veterinary Drug

摘　　要：为研究国产和进口盐酸贝那普利片在犬体内的药代动力学和生物等效性,将20只健康比格犬随机分成2组,采用双周期交叉试验设计,按0.5 mg/kg体重分别单剂量口服受试产品和参比产品。采用UPLC-MS/MS法测定血浆中盐酸贝那普利及贝那普利拉的浓度,利用Win Nonlin5.2.1软件计算主要药动学参数,并评价两种产品的生物等效性。结果显示,受试产品和参比产品中盐酸贝那普利T_(max)分别为0.85±0.36和0.98±0.40 h;C_(max)分别为65.85±31.14和52.02±25.79 ng/m L;AUC_(0-t)分别为46.98±29.77和40.54±20.76 h·ng·m L^(-1);AUC_(0-∞)分别为48.28±30.05和41.54±20.85 h·ng·m L^(-1);受试产品和参比产品的贝那普利拉T_(max)分别为1.78±0.55和1.90±0.72 h;C_(max)分别为63.05±28.44和55.29±36.01 ng/m L;AUC_(0-t)分别为249.09±87.90和212.50±90.03h·ng·m L^(-1);AUC_(0-∞)分别为274.15±93.86和264.42±161.86 h·ng·m L^(-1)。受试产品和参比产品的T_(max)、C_(max)、AUC_(0-t)和AUC_(0-∞)均无显著性差异(P>0.05)。双单侧t检验及90%置信区间结果均提示两种制剂生物等效,临床上可相互替代。该试验可为兽医临床安全使用该药提供科学依据。To study the pharmacokinetics and bioequivalence dogs, 20 healthy Beagle dogs were randomly divided into two batches the tested product and reference product at a single of domestic and imported benazepril hydrochloride in groups. A two-period crossover trial was designed to dose of 0.5 mg/ kg body weight, respectively. The plasma concentrations of benazepril and benazeprilat was analysed by UPLC- MS/MS. The pharmacokinetic parameters were calculated by WinNonlin5.2.1 software and the bioequivalence of the two products was evaluated. The results showed that the Tmax of benazepril hydrochloride in the tested and reference products were 0.85±0.36 and 0.98±0.40 h,respectively, Cmax were 65.85±31.14 and 52.02±25.79 ng/mL;AUCot were 46.98±29.77 and 40.54±20.76 h·ng·m L^-1 ;AUC0-∞ were 48.28±30.05 and 41.54±20.85 h·ng·m L^-1. The Tmax of benazeprila and the reference product were 1.78±0.55 and 1.90±0.72 h, respectively, Cmax were 63.05±28.44 and 55.29± 36.01 ng/mL;AUC0-t were 249.09±87.90 and 212.50±90.03 h ·ng·m L^-1 ; AUC0-∞ were 274.15±93.86 and 264.42±161.86 h·ng·m L^-1. There was no significant difference in Tmax, C AUC0-t and AUC0-∞ between the two formulations （P〉0.05）. Double unilateral two one-side t-test and 90% confidence interval results suggest that the two formulations are bioequivalent and clinically interchangeable. The trial provides a scientific basis for veterinary clinical use of the drug.

关 键 词：盐酸贝那普利 贝那普利拉 生物等效性 超高效液相色谱串联质谱 

分 类 号：S829.2[农业科学—畜牧学]