新型兽用纳米乳载药系统在大鼠体内的药代动力学研究

doi:10.16431/j.cnki.1671-7236.2019.04.033

摘要/Abstract

摘要：

为了解氟苯尼考纳米乳（FFNE）在大鼠体内药代动力学行为，本试验以氟苯尼考溶液（FFSol）为参比制剂，以30 mg/kg剂量给大鼠灌胃和肌内注射给药，分别于给药后0.5、1、2、4、8、12、24、36、48、72 h采血，利用高效液相色谱法测定血浆中氟苯尼考含量，利用DAS 2.0软件计算房室模型与非房室模型条件下药代动力学参数。结果显示，在两种给药方式下，FFNE与FFSol在大鼠体内均符合二室模型。灌胃给药后，FFNE与FFSol在房室模型条件下AUC_（0-∞）分别为1 085.047和2 176.490 mg/L·h，半衰期分别为10.566和13.687 h，FFNE的相对生物利用度为187.4%。肌内注射给药后，FFNE与FFSol在房室模型条件下AUC_（0-∞）分别为1 530.55和3 243.338 mg/L·h，半衰期分别为7.533和13.335 h，FFNE的相对生物利用度为211.9%。结果表明，FFNE通过灌胃和肌内注射给药在大鼠体内分布较广，灌胃相对肌内注射吸收差，消除快。将氟苯尼考制成纳米乳剂后促进了氟苯尼考的吸收，氟苯尼考的生物利用度显著提高。

关键词: 氟苯尼考; 纳米乳; 药代动力学; 生物利用度

Abstract:

To study the pharmacokinetics behavior of florfenicol nanoemulsion in rats,florfenicol solution was chosen as the contrast medicine,the medicine was taken oral and intramuscular dose of 30 mg/kg body weight,and sampled at 0.5,1,2,4,8,12,24,36,48 and 72 h.The concentrations of florfenicol in plasma samples were detected by a high performance liquid chromatography (HPLC) method.The data were analyzed with the pharmacokinetic program DAS 2.0.The results showed that the concentration-time course of florfenicol solution and florfenicol nanoemulsion in plasma fitted a 2-compartment open model.The parameters of FFNE and FFSol under compartmental model after oral administration,AUC_(0-∞) were 1 085.047 and 2 176.490 mg/L·h,half-life were 10.566 and 13.687 h,the relative bioavailability of florfenicol nanoemulsion was 187.4%.The parameters of FFNE and FFSol under compartmental model after intravenous administration,AUC_(0-∞) were 1 530.55 and 3 243.338 mg/L·h respectively,the half-life were 7.533 and 13.335 h,respectively,and the relative bioavailability of florfenicol nanoemulsion was 211.9%.The results indicated that FFNE had an adequate distribution in rats after intramscular and oral administration,however,elimination rate was faster by oral administration than by intramuscular of most rats.The prepared florfenicol nanoemulsion promoted absorption of florfenicol,and the bioavailability of florfenicol nanoemulsion was significantly improved.

Key words: florfenicol; nanoemulsion; pharmacokinetic; bioavailability

中图分类号:

S859.79

时菲菲, 王婧, 秦枫, 陈晓兰, 高建如, 魏宇, 张龙. 新型兽用纳米乳载药系统在大鼠体内的药代动力学研究[J]. 《中国畜牧兽医》, 2019, 46(4): 1236-1243.

SHI Feifei, WANG Jing, QIN Feng, CHEN Xiaolan, GAO Jianru, WEI Yu, ZHANG Long. Study on Pharmacokinetics of a Novel Veterinary Nanoemulsion Drug Loading System in Rats[J]. , 2019, 46(4): 1236-1243.

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