氟苯尼考论文：氟苯尼考、恩诺沙星及替米考星微囊在猪体内的药物动力学研究

氟苯尼考论文：氟苯尼考、恩诺沙星及替米考星微囊在猪体内的药物动力学研究

氟苯尼考论文：氟苯尼考、恩诺沙星及替米考星微囊在猪体内的药物动力学研究

【中文摘要】本试验旨在研究氟苯尼考、恩诺沙星及替米考星的新型制剂微囊,给猪灌服之后,在猪体内的药物动力学参数。比较微囊制剂与其原粉的优缺点,为兽医临床合理用药提供理论依据。1.氟苯尼考微囊在猪体内的药物动力学试验分析氟苯尼考微囊（Florfenicol Microcapsules,FM）和氟苯尼考原粉（Florfenicol,FF）在猪体内的药物代谢动力学过程。猪单剂量分别灌服FF和FM 30 mg·kg-1,36 h不同时间16次前腔静脉采血,高效液相色谱法（HPLC）测定血药中FF的浓度。结果表明,FM和FF在猪体内的药物动力学配置均符合有吸收因素一室开放模型,其药-时曲线最佳方程分别为:CFM=3.772 7(e﹣0.047t-e﹣0.8477t),CFF

=0.375 9 (e﹣0.2581t-e﹣4.670 9t)。微囊及原粉的主要药物动力学参数:吸收半衰期t1/2Ka分别为（0.944 6±0.507 5） h,（0.155 0±0.030 1） h;消除半衰期t1/2Ke分别为（15.214 0±3.024 9）h,（2.694 5±0.169 5） h;药-时曲线下面积AUC分别为（77.311 1±13.312 7）mg·L-1·h,（1.374 7±0.606 0） mg·L-1·h;峰质量浓度分别为（2.937 1±0.232 2） mg·L-1,（0.298 3±0.023 9）mg·L-1;达峰时间分别为（3.951 0±1.533 9） h,（0.675 3±0.104 6） h。通过比较,说明FM口服给药吸收较慢但完全,达峰时间较长,消除缓慢,能够发挥长效作用。2.恩诺沙星微囊在猪体内的药物动力

mg·L-1·h。表明TM在猪体内吸收缓慢完全,消除相对较慢,能较长时间发挥药效。

【英文摘要】The purpose of this study was to get the pharmacokinetic parameters of the new dosage forms of florfenicol, enrofloxacin, and tilmicosin, after a single oral administration in pigs. Compared with their original powder, then provided theoretical basis for rational drug use.1. Pharmacokinetic parameters of Florfenicol Microcapsules （FM）and Florfenicol in 6 pigs were calculated.Pigs were treated with a single dosage of FF (30 mg·kg-1) orally, while the blood samples were collected from precaval vein within 36 hour after giving drug. The concentrations of FF in serum were determined by high performance liquid chromatography （HPLC）. The result showed that the one-compartment open modle with first-order absorption factor adequately describes concentrations of FM and FF in serum disposition and best concentration-time equations are: CFM=3.772 7 (e﹣0.047t-e﹣0.8477t), CFF=0.375 9(e-0.258 1t-e-4.670 9t). The primary pharmacokinetic parameters of FM and FF are: t1/2Ka=（0.944 6±0.507 5） h and （0.155 0±0.030 1） h, t1/2Ke=（15.214 0±3.024 9） h and （2.694 5±0.169 5） h, AUC=（77.311 1±13.312 7） mg·L-1·h and（1.374 7±0.606 0） mg·L-1·h, Cmax=（2.937 1±0.232 2）

mg·L-1 and （0.298 3±0.023 9） mg·L-1·h, Tmax=（3.951 0±1.533 9） h and （0.675 3±0.104 6） h. It will be seen that Florfenicol microcapsules was completely absorbed with a slowly absorption rate, and which was eliminated slowly in the blood after single oral administration.2. Pharmacokinetic parameters of Enrofloxacin Microcapsules（EM） and Enrofloxacin （ENR） in 6 pigs were calculated.Pigs were treated with a single dosage of ENR (30 mg·kg-1) orally, while the blood samples were collected from precaval vein within 72 hour after giving drug. The concentrations of ENR in serum were determined by HPLC. The result showed that the two-compartment open modle with first-order absorption factor adequately describes concentrations of EM and ENR in serum disposition and best concentration-time equations are: CEM=11.326

3e-0.353 8t+5.420 6e-0.066 1t-16.746 9e-0.979 8t, CENR=11.251 1e-0.934 7t+5.330 1e-0.079 9t-16.581 2e-2.965 7t. The primary pharmacokinetic parameters of EM are: t1/2ka=（0.769 5±0.250 9） h; t1/2a=（2.160 3±0.704 1） h; t1/2β=（10.522 4±0.719 5） h; AUC=（92.924 3±5.308 4） mg·L-1·h. It will be seen that EM was completely absorbed with a slowly absorption rate, and which was eliminated slowly in the blood after single oral administration.3. Pharmacokinetic parameters of Tilmicosin