两种伊维菌素注射液在家兔体内的生物等效性研究

Bioequivalence of two different ivermectin injection in rabbits

关键词:  伊维菌素  生物等效性  家兔

Key words:  ivermectin  Bioequivalence  rabbits

摘要:

为评价两种伊维菌素注射液在家兔体内的生物等效性，采用双周期交叉给药方式，将16 只健康家兔随机分成2 组，按5 mg/kg体重皮下单剂量注射两种伊维菌素注射液，使用高效液相色谱法(HPLC)测定血浆中的伊维菌素，利用3P97药动软件计算主要药动学参数，以此来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(26.45±8.62) h，(22.33±11.72) h；Cmax分别为(182.73±59.27) ng/mL，(166.77±65.25) ng/mL；AUC0-t分别为(21122±9999)ng?h?L-1，(19475±7009)ng?h?L-1；AUC0-∞分别为(27390±12197)ng?h?L-1，(31559±13412)ng?h?L-1。伊维菌素注射液受试制剂与参比制剂的AUC0-t、AUC0-∞、Cmax、Tmax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，试验给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 two kinds of Ivermectin Injection in rabbits. In a randomized two-way self-crossover study, 16 healthy rabbits were randomly divided into two groups, and were given respectively a single dose of two kinds of Ivermectin Injection by subcutaneous injection(5mg/kg). Plasma concentrations of ivermectin were measured by HPLC. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic software, and the bioequivalence were evaluated. The main pharmacokinetic parameters of the test and reference prearations were as follows: Tmax were (26.45±8.62) h，(22.33±11.72) h；Cmax were (182.73±59.27) ng/mL，(166.77±65.25) ng/mL；AUC0-t were(21122±9999)ng?h?L-1，(19475±7009)ng?h?L-1；AUC0-∞were(27390±12197)ng?h?L-1，(31559±13412)ng?h?L-1. The pharmacokinetic parameters (AUC0-t、AUC0-∞、Cmax、Tmax) showed no significant difference between test and reference preparations of ivermectin injections. The test and reference formulations were bioequivalent after two one-side t-test. This study provided theoretical basis for making of veterinary clinical dosage regimen and clinical rational administration.