关键词检索
按:
检索词:
  高级检索
引用:杨柯,陈世伟,窦新岩,张晊瑞,金鑫,张红敏.2%双醋瑞因滴眼液结膜囊多次与单次给药的角膜药代动力学差异.国际眼科杂志 2018;18(4):630-633,doi:10.3980/j.issn.1672-5123.2018.4.08
2%双醋瑞因滴眼液结膜囊多次与单次给药的角膜药代动力学差异
Corneal pharmacokinetics of the 2% diacerein eye drops between multiple administration and single administration
投稿时间:2017-10-19  修订日期:2018-03-12
Email this Article  Add to Favorite  Print
DOI:10.3980/j.issn.1672-5123.2018.4.08
关键词:  结膜囊给药  双醋瑞因  多次  单次  药物代谢动力学
Key Words:  conjunctival sac delivery  diacerein  multiple administration  single  pharmacokinetic
基金项目:河南省科技创新人才计划项目(No.144100510015); 河南省自然科学基金项目(No.162300410163)
Fund Project:Science and Technology Innovation Talent Project of Henan Province(No.144100510015); Natural Science Foundation of Henan Province(No.162300410163)
                 
作者单位
杨柯 中国河南省郑州市,河南省眼科研究所 河南省立眼科医院 河南省眼科学与视觉科学重点实验室 河南省人民医院 郑州大学人民医院眼科
陈世伟 中国河南省郑州市,河南省口岸食品检验检测所
窦新岩 中国河南省郑州市,河南省眼科研究所 河南省立眼科医院 河南省眼科学与视觉科学重点实验室 河南省人民医院 郑州大学人民医院眼科
张晊瑞 中国河南省新乡市,新乡医学院
金鑫 中国河南省郑州市,河南省眼科研究所 河南省立眼科医院 河南省眼科学与视觉科学重点实验室 河南省人民医院 郑州大学人民医院眼科
张红敏 中国河南省郑州市,河南省眼科研究所 河南省立眼科医院 河南省眼科学与视觉科学重点实验室 河南省人民医院 郑州大学人民医院眼科
                 
AuthorInstitution
Ke Yang Henan Eye Institute; Henan Eye Hospital; Henan Key Laboratory of Ophthalmology and Visual Science; Department of Ophthalmology, Henan Provincial Peoples Hospital; Peoples Hospital of Zhengzhou University, Zhengzhou , Henan Province, China
Shi-Wei Chen Henan Food Inspection and Testing Institute, Zhengzhou , Henan Province, China
Xin-Yan Dou Henan Eye Institute; Henan Eye Hospital; Henan Key Laboratory of Ophthalmology and Visual Science; Department of Ophthalmology, Henan Provincial Peoples Hospital; Peoples Hospital of Zhengzhou University, Zhengzhou , Henan Province, China
Zhi-Rui Zhang Xinxiang Medical College, Xinxiang , Henan Province, China
Xin Jin Henan Eye Institute; Henan Eye Hospital; Henan Key Laboratory of Ophthalmology and Visual Science; Department of Ophthalmology, Henan Provincial Peoples Hospital; Peoples Hospital of Zhengzhou University, Zhengzhou , Henan Province, China
Hong-Min Zhang Henan Eye Institute; Henan Eye Hospital; Henan Key Laboratory of Ophthalmology and Visual Science; Department of Ophthalmology, Henan Provincial Peoples Hospital; Peoples Hospital of Zhengzhou University, Zhengzhou , Henan Province, China
摘要点击次数: 2011
Hits:
全文下载次数: 120
Download times:
摘要:
      

目的:对比2%双醋瑞因滴眼液结膜囊多次给药与单次给药在角膜中的药代动力学差异,为临床医师治疗感染性角膜病时多次给药提供实验依据。

     方法:以2%双醋瑞因为实验滴眼液,选取健康无眼疾的雄性昆明白小鼠,随机分为多次给药组和单次给药组,双眼结膜囊分别给予双醋瑞因滴眼液。多次给药组间隔2min给药一次,共给药3次; 单次给药组仅给药1次。用高效液相法测定角膜中双醋瑞因的代谢产物(大黄酸)的浓度,多次给药组和单次给药组的时间点均为5、15、30、60、120、180min。将小鼠角膜组织中的药物浓度经药物动力学程序(DAS2.1.1)进行拟合,并计算相关药动学参数。

     结果:结膜囊多次给药组和单次给药组各个时间点角膜中均可检测到其活性代谢产物大黄酸; 多次给药组5、15、30、60、120、180min的浓度分别为318.678±40.88、210.02±25.66、188.83±31.74、112.24±11.70、90.28±22.01和57.67±13.71μg/g,单次给药组各时间点浓度分别为145.17±19.29、97.95±10.49、71.18±18.70、39.11±2.44、18.10±2.34和9.08±2.04μg/g。两组小鼠角膜中大黄酸的含量均于给药后5min最高,多次给药组浓度高于单次给药组浓度,差异具有统计学意义(P<0.01)。随时间延长大黄酸的浓度逐渐下降,3h后多次给药组浓度仍高于单次给药组,差异具有统计学意义(P<0.01)。单次给药组半衰期为0.89±0.31h。

     结论:结膜囊多次给药与单次给药相比具有药物有效浓度高、维持时间长的优点,双醋瑞因作为一种新的抗菌药物,可以在感染性角膜炎的早期对病程的发展起到抑制作用。多次给药后可以对急性发展期起到较好的治疗效果,而且在夜晚也可维持较高浓度,在保证患者的睡眠休息质量同时又起到了对疾病的治疗作用。

Abstract:
      AIM: To compare the pharmacokinetic differences of the 2% diacerein eye drops between conjunctival sac multiple administration and single administration in the cornea, and to provide the experimental basis for clinicians to use the conjunctival sac multiple administration.

     METHODS: Male Kunming mice were randomly divided into the multiple administration group and the single administration group. The multiple administration group were given diacerein eye drop every 2min(3 times in total). The concentrations of the metabolites of diacerein in the cornea were measured by high performance liquid chromatography after given eye drop 5, 15, 30, 60, 120, and 180min. The pharmacokinetic parameters were calculated by pharmacokinetic software(DAS2.1.1).

     RESULTS: The metabolites of diacerein, rhein, was detected in the cornea at each time point. The concentration of the metabolite of diacerein in the cornea was 318.678±40.88, 210.02±25.66, 188.83±31.74, 112.24±11.70, 90.28±22.01 and 57.67±13.71μg/g after given eye drop 5, 15, 30, 60, 120, and 180min in the multiple administration group. The concentration in the single administration group was 145.17±19.29, 97.95±10.49, 71.18±18.70, 39.11±2.44, 18.10±2.34 and 9.08±2.04μg/g respectively. The concentration of rhein in the cornea was the highest at 5min after the administration in the two groups. The concentration of the multiple administration group was higher than that in the single administration group at 5, 15, 30, 60, 120, and 180min(P<0.01). The half-life of the drug was 0.89±0.31h in the single administration group.

     CONCLUSION: Compared with the single administration, the conjunctival sac multiple administration has the advantages of high drug concentration and long duration. Therefor the conjunctival sac multiple administration is a more effective method to treat acute infectious corneal diseases.

Citation Html:
附件
查看全文PDF FullText  查看/发表评论  下载PDF阅读器