恩诺沙星纳米混悬注射剂的制备及在猪体内药动学研究

发布时间：2018-03-15 18:26

本文选题：高压均质法　切入点：恩诺沙星　出处：《中国兽医学报》2017年08期 　论文类型：期刊论文

【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(P0.01),MRT显著延长(P0.01)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。
[Abstract]:High pressure homogenization method was used to prepare enrofloxacin nano-suspension injection and its preparation technology and quality were investigated and evaluated, and the concentration of enrofloxacin in pig plasma was determined by HPLC. The pharmacokinetics of enrofloxacin nano-suspension injection in pigs was investigated by using Baiyi injection as a reference. The results showed that the prepared enrofloxacin nano-suspension injection was prepared. The content of enrofloxacin is 97.9, the average particle size is 613.21 卤5.78nmmg / L, the Zeta potential is -2.02mV. the peak concentration of enrofloxacin nano-suspension injection and benazepam injection in pigs is 0.32 卤0.1212ng / L, and the peak time is 2.88 卤0.96nmg / L and 0.79 卤0.26hrespectively, and the elimination of half-life is 5.99 卤1.37hAUClast, respectively. The MRTlast was 4.63 卤1.30 mg / h, 4.40 卤0.45 mg / L MRTlast was 9.59 卤2.34 mg-1 / h and 5.41 卤1.10 / h, respectively. The relative bioavailability of enrofloxacin nano-suspension injection was 105.2. Conclusion: the preparation of enrofloxacin nano-suspension injection by high pressure homogenization method is easy to operate, easy to settle, good dispersion and stable physical and chemical properties. Compared with the injection, its Tmax1 / 2k increased significantly (P 0.01) and MRT significantly prolonged (P 0.01). The results showed that enrofloxacin nano-suspension injection had obvious slow-release and slow elimination.
【作者单位】：华南农业大学国家残留基准实验室;广东温氏大华农生物科技有限公司;
【基金】：国家自然科学基金资助项目(31372479)
【分类号】：S859.5;S859.7

【相似文献】