恩诺沙星纳米混悬注射剂的制备及在猪体内药动学研究  

Preparation of enrofloxacin nanosuspension injection and its pharmacokinetics in swine

作　　者：余鹏灵 陈良柱 潘志坤 周巧仪[1] 王琴[1] 方炳虎[1] 

机构地区：[1]华南农业大学国家残留基准实验室,广东广州510642 [2]广东温氏大华农生物科技有限公司,广东新兴527400

出　　处：《中国兽医学报》2017年第8期1534-1539,共6页Chinese Journal of Veterinary Science

基　　金：国家自然科学基金资助项目(31372479)

摘　　要：采用高压均质法制备恩诺沙星纳米混悬注射剂并对其制备工艺和质量进行考察、评价;采用高效液相色谱法测定猪血浆中恩诺沙星的浓度,以拜有利注射剂为参照考察恩诺沙星纳米混悬注射剂在猪体内的药动学。结果显示:制备的恩诺沙星纳米混悬注射剂,恩诺沙星的含量为97.9%,平均粒径为(613.21±5.78)nm、PDI(0.22±0.02)、Zeta电位为-2.02mV。恩诺沙星纳米混悬注射剂和拜有利注射剂在猪体内的达峰浓度(Cmax)分别为(0.32±0.12)、(0.67±0.09)mg/L,达峰时间(Tmax)分别为(2.88±0.96)、(0.79±0.26)h,消除半衰期(t1/2ke)分别为(5.99±1.37)、(4.49±1.25)h,AUClast分别为每小时(4.63±1.30)、(4.40±0.45)mg/L,MRTlast分别为(9.59±2.34)、(5.41±1.10)h;与拜有利注射剂相比,恩诺沙星纳米混悬注射剂相对生物利用度为105.2%。结论:高压均质法制备的恩诺沙星纳米混悬注射剂操作简单、不易沉降、再分散性好,理化性质较稳定;与拜有利注射剂相比其Tmax、t1/2k明显增加(P<0.01),MRT显著延长(P<0.01)表明恩诺沙星纳米混悬注射剂具有明显缓释作用且消除缓慢。The aim of the study was to prepare enrofloxacin nanosuspension injection and evaluate its pharmacokinetics after giving a single intramuscular injection. The high pressure homogeneous technique was used to prepare enrofloxacin nanosuspension injection and preliminary evaluation of the quality was done. The high performance liquid chromatography （HPLC） method was used to determinate content of enrofloxacin in pig plasma. And the pharmacokinetic characteristics of enro- floxacin nanosuspension injection were compared with Baytril injection. The content of enrofloxacin in this preparation is 97.9 %. The average particle size of enrofloxaein nanosuspension injection was （613.21±5.78） nm,PDI was （0.22±0.02） and the potential was -2.02 mV. Maximal plasma concentrations were （0.32±0.12） and （0.67±0.09） mg/L after i. m administration with enro- floxacin nanosuspension injection and Baytril injection. The peak times were （2.88±0. 96） and （0.79±0.26） hours,respectively. Mean elimination half-lifes were （5. 99±1. 37） and （4. 49±1.25） hours,respectively. Areas under concentration-time curve were （4.63±1.30） and （4.40±0.45） mg/L·h,respectively. Mean residence times were （9.59±2.34） and （5.41±1.10） hours, respectively. The relative bioavailability of enrofloxacin nanosuspension injection was 105.2 %. The preparation method of high pressure homogeneous was simple and good reproducibility. Enrofloxacin nanosuspension injection was characterized by non-sedimentation, easy-redispersion, relatively stable. Comparing with Baytril injection,enrofloxacin nanosuspension injection had a certain slow- release effect,showing slower elimination than enrofloxacin injection.

关 键 词：高压均质法 恩诺沙星 纳米混悬注射液 药动学 

分 类 号：S859.79[农业科学—临床兽医学]