两种盐酸多西环素注射液在猪体内的药代动力学研究

Pharmacokinetics of Two Kinds of Doxycycline Hydrochloride Injections in Swine

关键词:  盐酸多西环素注射液  猪  药代动力学

Key words:  doxycycline hydrochloride injection  swine  pharmacokinetics

摘要:

研究制备了两种稳定的20%盐酸多西环素注射液，按10 mg/kg的剂量分别给猪肌肉注射，观察两个制剂在猪体内单剂量肌注的药代动力学特征。结果表明，多西环素在猪体内的药物动力学特征均符合一级吸收二室开放模型，其主要的药物代谢动力学参数：消除半衰期（T1/2β）分别为（3.246?1.04）和（9.631?1.12） h，药时曲线下面积（AUC）为（10.462?0.28）和（17.525?0.14） (μg/mL)*h，达峰时间（Tpeak）及达峰浓度（Cmax）分别为（1.427?0.16） h、（1.465?0.20）μg/mL和（1.694?0.15） h、(1.058?0.09)μg/mL。其中制剂一的血药浓度在给药2 h后迅速降低，为普通注射液；与制剂一相比，制剂二能够缓慢释放药物，为长效缓释盐酸多西环素注射液。

Abstract:

Two kinds of doxycycline hydrochloride injections（20%）were prepared， the swines were injected intramuscularly at the dose of 10 mg/kg body weight. The pharmacokinetics of two preparations in swines were characterized. The results showed that the kinetics of two doxycycline hydrochloride injections were fitted to two compartment open model with first-order absorption. The main pharmacokinetic parameters were as follows: the half life of elimination (T_1/2β) were（3.246?1.04）,（9.631?1.12） h，and the area under the plama drug concentration-time curve (AUC) were（10.462?0.28）,（17.525?0.14） (μg/mL)*h，and the peaking time(Tpeak) and the peak plama concentration (Cmax) were（1.427?0.16） h,（1.465?0.20） μg/mL and（1.694?0.15） h, (1.058?0.09) μg/mL, respectively. The concentration of doxycycline of prescription one decreased rapidly after 2 h, which was a common injection. Compared with the prescription one, the prescription two released the drug slowly, which was the sustain released doxycycline hydrochloride injection.