双醋瑞因在小鼠角膜中的药代动力学行为

发布时间：2018-06-06 09:06

本文选题：双醋瑞因 + 药代动力学　；参考：《中成药》2017年11期

【摘要】：目的考察双醋瑞因在小鼠角膜中的药代动力学行为。方法将2%双醋瑞因滴眼液单次滴入小鼠双眼结膜囊,分别于滴眼后5、15、30、45、60、90、120、150、180 min处死动物,取角膜,HPLC法测定角膜中双醋瑞因代谢产物大黄酸含有量。结果各个时间点小鼠角膜中均未检测到双醋瑞因,而是其活性产物大黄酸。给药后5 min,角膜中大黄酸含有量最高,为(143.59±2.37)μg/g,之后逐渐下降。角膜组织中药物浓度半衰期为(0.86±0.06)h,达到最大药物质量浓度所需时间为5 min(0.08 h),最大药物质量浓度为(143.59±19.61)μg/g。结论双醋瑞因滴眼液能够透过角膜上皮到达小鼠角膜,并完全转化为大黄酸,具有良好的药代动力学特征。
[Abstract]:Objective to investigate the pharmacokinetics of diacetate in the cornea of mice. Methods 2% diacetate eye drops were injected into the binocular conjunctival sac of mice, and the animals were killed at 51530U 45.60120150180 min after dropping, and the content of Rhein, the metabolite of diacetate, was determined by HPLC. Results Diacetate was not detected in the cornea of mice at all time points, but was the active product of Rhein. The content of Rhein in cornea was the highest (143.59 卤2.37) 渭 g / g at 5 min after administration, and then decreased gradually. The half-life of drug concentration in corneal tissue was 0.86 卤0.06h. the time to reach the maximum drug concentration was 5 min(0.08 hU, and the maximum drug concentration was 143.59 卤19.61 渭 g / g. Conclusion diacetate eye drops can reach the cornea of mice through corneal epithelium and be transformed into Rhein completely, which has good pharmacokinetic characteristics.
【作者单位】：郑州大学人民医院/河南省人民医院眼科河南省立眼科医院/河南省眼科研究所;河南省口岸食品检验检测所;新乡医学院;
【基金】：河南省科技创新人才计划项目(144100510015) 河南省医学科技攻关计划项目(201203171) 河南省自然科学基金项目(162300410163)
【分类号】：R965

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