氟苯尼考环糊精包合物的药物代谢动力学研究

The Pharmacokinetics of Florfenicol Cyclodextrin Inclusion Complex

为研究氟苯尼考环糊精包合物的药代动力学及生物利用度,将健康白羽肉鸡24只,随机分为两组,每组12只,分别以20 mg/kg的剂量单次灌服20%普通氟苯尼考粉(A组)和20%氟苯尼考环糊精包合物(B组),并于给药后不同时间点从翅下静脉采血,采用已建立的UPLC-MS/MS测定血浆中的药物浓度,用WinNonlin 5.2.1药动学分析软件的非房室模型拟合血药浓度-时间数据。结果显示:A组达峰时间(T max)和达峰浓度(C max)分别为1.563±0.755 h、1043.15±391.42 ng/mL,平均消除半衰期(T 1/2λz)约为4.814±3.058 h,平均曲线下面积(AUC last)为4283.53±2406.81 h·ng/mL;B组T max、C max分别为1.417±1.683 h、4691.95±1597.28 ng/mL,T 1/2λz约为2.106±1.476 h,AUC last为14911.70±2976.22 h·ng/mL;相对生物利用度约为348.12%。试验表明,采用环糊精包合工艺的氟苯尼考粉的生物利用度显著高于普通工艺的氟苯尼考粉。

In order to study the pharmacokinetics and bioavailability of florfenicol cyclodextrin inclusion compound,twenty-four healthy broilers were randomly divided into two groups,and each group had twelve broilers.20%florfenicol powder without inclusion process(group A)and 20%cyclodextrin inclusion florfenicol powder(group B)were administrated in a single dose of 20 mg/kg,respectively.Plasma samples were collected from the subwing vein at different time points and tested using UPLC-MS/MS.The WinNonlin 5.2.1 pharmacokinetic analysis software was used to process the blood concentration time data.The peak time(T max)and peak concentration(C max)in group A were 1.563±0.755 h and 1043.15±391.42 ng/mL,respectively.The average elimination half-life(T 1/2λz)was 4.814±3.058 h,and the average area under the curve(AUC last)was 4283.53±2406.81 h·ng/mL.T max and C max in group B were 1.417±1.683 h and 4691.95±1597.28 ng/mL,respectively.T 1/2λz was about 2.106±1.476 h,and AUC last was 14911.70±2976.22 h·ng/mL.The relativ e bioavailability was about 348.12%.The results showed that the bioavailability of florfenicol powder by cyclodextrin inclusion was significantly higher than that of florfenicol powder without inclusion process.