托芬那酸注射液在犬体内的生物等效性研究

Bioequivalence of Tolfenamic Acid Injection in Dogs

关键词:  托芬那酸注射液  药代动力学  生物等效性  高效液相色谱

Key words:  HPLC  Tolfenamic acid injection  Pharmacokinetic  Bioequivalence

摘要:

为了研究国产和进口托芬那酸注射液在犬体内的药代动力学和生物等效性,采用双处理、双周期随机交叉试验设计,将20头健康比格犬随机分成2组,按 0.1 ml/kg 体重肌肉分别单剂量注射受试制剂和参比制剂,采用高效液相色谱法测定血浆中托芬那酸的浓度,利用 WinNonlin6.3 软件计算主要药动学参数,并评价两种制剂的生物等效性。结果显示,受试制剂和参比制剂的 Tmax 分别为(0.2±0.1)h和(0.3±0.2)h; Cmax 分别为(5.12±1.55) μg/ml和(5.38±2.04) μg/ml; AUC0－t分别为(12.1±2.97) μg.h.mL－1和(12.28±3.24) μg.h.mL－1; AUC0－∞分别为(13.38±3.10)μg.h.mL－1和(13.85±3.40) μg.h.mL－1 。托芬那酸注射液受试制剂和参比制剂的AUC0－t、AUC0－∞、C max、T max 均无显著性差异,(p>0.05)。双单侧 t 检验结果显示两种制剂生物等效,临床上可相互替代。试验为兽医临床给药方案的制定以及合理用药提供参考。

Abstract:

To evaluate the pharmacokinetics and bioequivalence of amoxicillin suspension injection in dogs. In arandomized two-way self-crossover study, 20 healthy dogs were randomly divided into two groups, and were given respectively a single dose of test or reference preparations by intramuscular injection(0.1ml/kg). Plasma concentrations of Tolfenamic Acid were measured by HPLC. The pharmacokinetic parameters were calculated by WinNonlin6.3 software, and the bioequivalence were evaluated. The main pharmacokinetic parameters of the test and reference preparations were asfollows: Tmax were(0.2±0.1) , (0.3±0.2) h; Cmax were (5.12±1.55) μg/ml, (5.38±2.04) μg/ml; AUC0－t were(12.1±2.97) μg.h.mL－1, (12.28±3.24) μg.h.mL－1 ; AUC0－∞ were (13.38±3.10)μg.h.mL－1, (13.85±3.40) μg.h.mL－1. The pharmacokinetic parameters (AUC0－t, AUC0－∞, Cmax, Tmax) showed no significant difference between test and reference preparations of Tolfenamic Acid suspension injections, (p>0.05). The test and reference formulations are bioequivalent after two one-side t-test. Clinically can replace each other; This study will provide theoretical basis for making of veterinary clinical dosage regimen and clinical rational administration.