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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。
In order to study the pharmacokinetics and bioequivalence of domestic and imported benazepril tablets in dogs, 20 healthy beagle dogs were randomly divided into two groups. The rats were treated with 0.5 mg / kg body weight A single dose oral test products and reference products. The concentration of benazepril hydrochloride and benazepril hydrochloride in plasma was determined by UPLC-MS / MS. The main pharmacokinetic parameters were calculated by Win Nonlin 5.2.1 software and the bioequivalence of the two products was evaluated. The results showed that the T_ (max) of benazepril hydrochloride in the tested and reference products were 0.85 ± 0.36 and 0.98 ± 0.40 h, respectively, and the C max were 65.85 ± 31.14 and 52.02 ± 25.79 ng / m L, respectively. The AUC_ (0-t) were 46.98 ± 29.77 and 40.54 ± 20.76 h · ng · m L -1, respectively; AUC 0 -∞ were 48.28 ± 30.05 and 41.54 ± 20.85 h · ng · m L ~ (-1) 1). The T max of benazeprilat of the tested and reference products were 1.78 ± 0.55 and 1.90 ± 0.72 h, respectively. The C max values were 63.05 ± 28.44 and 55.29 ± 36.01 ng / m L, respectively. The AUC_ (0-t) were 249.09 ± 87.90 and 212.50 ± 90.03 ng · m L -1, respectively; AUC 0 -∞ were 274.15 ± 93.86 and 264.42 ± 161.86 h · ng · m L ~ (-1) 1). There was no significant difference in T max, C max, AUC 0-t and AUC 0 -∞ between the tested product and the reference product (P> 0.05). Both single-sided t-test and 90% confidence interval results suggest that the two preparations are bioequivalent and can be clinically substituted for each other. This test provides a scientific basis for the clinical use of this medicine in veterinary safety.