氟苯尼考原料药及制剂在大鼠体内的药代动力学及绝对生物利用度研究  

Pharmacokinetics and Absolute Bioavailability Study of Florfenicol Raw Materials and Preparations in Rats

作　　者：戴银娣 孙少辉 马小平 胡娟 孙莹 万进 马妮妮 杨秋实 张少南 王聪 DAI Yin-di;SUN Shao-hui;MA Xiao-ping;HU Juan;SUN Ying;WAN Jin;MA Ni-ni;YANG Qiu-shi;ZHANG Shao-nan;WANG Cong(China Animal Husbandry Nanjing Veterinary Drugs Co.,Ltd.,Nanjing,Jiangsu,210012,China;China Animal Husbandry Industry Co.,Ltd,Beijing,100070,China)

机构地区：[1]中牧南京动物药业有限公司,江苏南京210012 [2]中牧实业股份有限公司,北京100070

出　　处：《动物医学进展》2024年第7期82-87,共6页Progress In Veterinary Medicine

摘　　要：对氟苯尼考制剂不同给药方式在大鼠体内的药动学特征和体内生物利用度进行了研究,以评价β-环糊精包合工艺对氟苯尼考体内生物利用度的影响。选取15只健康大鼠平行随机分为3组,分别静脉注射氟苯尼考原药,口服灌胃氟苯尼考物理混合物,口服灌胃包合工艺氟苯尼考粉,采用高效液相色谱法测定大鼠血浆中氟苯尼考的浓度,利用药代动力学软件PKSovler软件中非房室统计矩分析模型,计算药动学参数并进行药动学数据分析。结果显示,静脉注射组药物消除为半衰期(t_(1/2))为(367.04±159.85)min、平均药时曲线下面积AUC_(0-)为6622.16±927.55。包合工艺氟苯尼考组达峰时间(T max)为(40.00±14.14)min、达峰浓度(C_(max))为(28.82±4.00)μg/mL、半衰期(t_(1/2))为(378.40±226.34)min,平均药时曲线下面积AUC_(0-)为5627.60±1442.41。物理混合物组达峰时间(T max)为(68.00±30.33)min、达峰浓度(C_(max))为(15.64±4.40)μg/mL、半衰期(t_(1/2))为(288.29±52.25)时曲线下面积AUC_(0-)为4543.56±761.34。氟苯尼考粉物理混合组体内绝对生物利用度为68.6%,包合工艺氟苯尼考组在体内绝对生物利用度为85.0%。综上可判定包合工艺法氟苯尼考组能显著提高氟苯尼考达峰浓度和氟苯尼考体内吸收程度,生物利用度高。The present study was conducted to investigate the pharmacokinetic profiles and bioavailability of florfenicol preparations in rats by different means of administration,and to evaluate the effect ofβ-cyclodextrin inclusion technology on the in vivo bioavailability of florfenicol.In this experiment,15 healthy rats were selected and randomly divided into three groups:Florfenicol raw material intravenous injection group,oral administration of a physical mixture of florfenicol group,and oral administration of florfenicol group by inclusion technology alone.The concentration of florfenicol in rat plasma was determined by high-performance liquid chromatography(HPLC).Pharmacokinetic data analysis was conducted using non-compartmental model-dependent statistical moment analysis model in PKSolver software.Pharmacokinetic parameters were calculated to investigate the pharmacokinetic characteristics and bioavailability of florfenicol group by inclusion technology after intravenous injection and oral administration.The results showed that the peak time(T max)of the florfenicol group by inclusion technology was 40.00±14.14 min,the peak concentration(C_(max))was 28.82±4.00μg/mL,the half-life(t_(1/2))was 378.40±226.34 min,and the average area under the concentration-time curve(AUC)was 5627.60±1442.41.The peak time(T max)of the physical mixture group was 68.00±30.33 min,the peak concentration(C_(max))was 15.64±4.40μg/mL,the half-life(t_(1/2))was 288.29±52.25 min,and the average AUC was 3319.22±733.59.The absolute bio-availability of florfenicol powder physical mixture group was 68.8%,while that of the florfenicol group by inclusion technology was 85.0%.In conclusion,the inclusion complex technology of florfenicol product significantly improved the absorption extent of florfenicol in vivo,resulting in a higher bioavailability.

关 键 词：氟苯尼考 包合工艺 药代动力学 大鼠 

分 类 号：S859.796[农业科学—临床兽医学]