青光眼药物跨角膜输运特性实验研究  

Experimental Study of Glaucoma Drug Delivery Across Cornea

作　　者：徐洪涛[1] 黄飞 雷苑 屈治国[3] 陈建[1] 崔国民[1] XU Hong-Tao;HUANG Fei;LEI Yuan;QU Zhi-Guo;CHEN Jian;Cui Guo-Min(School of Energy and Power Engineering,University of Shanghai for Science and Technology,Shanghai 200093,China;Eye&Ent Hospital of Fudan University,Shanghai 200031,China;School of Energy and Power Engineering,Xi'an Jiaotong University,Xi'an 710049,China)

机构地区：[1]上海理工大学能源与动力工程学院,上海200093 [2]复旦大学附属眼耳鼻喉科医院,上海200031 [3]西安交通大学能源与动力工程学院,西安710049

出　　处：《工程热物理学报》2021年第7期1858-1863,共6页Journal of Engineering Thermophysics

基　　金：国家自然科学基金面上项目(No.81371015);自然科学基金创新群体资助项目(No.51721004);美国BrightFocus Foundation(No.G2018112);复旦大学附属眼耳鼻喉科医院青年科学家培养计划。

摘　　要：青光眼是导致眼睛失明的疾病之一。局部用药是治疗青光眼的一种有效方法,但角膜的低渗透性限制了药物快速输运至病变组织,因此亟待研究青光眼药物跨角膜输运特性。本文选用质量分数ω=0.01与质量分数ω=0.05两种不同质量分数的毛果芸香碱水溶液作为青光眼药物制剂,对其作用在猪角膜上进行了药物渗透的离体实验。实验结果表明:质量分数ω=0.05实验组接收池内药物浓度增长速率明显高于ω=0.01实验组,药物浓度增长速率与初始给药浓度成正比例;药物累积过程主要由非稳态与伪稳态两个阶段组成,得出了伪稳态阶段药物累积量与给药浓度,时间,角膜厚度以及药物扩散系数满足的函数;毛果芸香碱水溶液跨角膜输运的扩散系数约为2.47×10^(-6)cm^(2)/s。本文的研究将有助于后续进行建立青光眼药物跨角膜输运特性数学描述方程的工作,从而优化青光眼药物的药物设计。Glaucoma is one of the diseases that cause blindness in the eye.Topical application is an effective method for the treatment of glaucoma,but the low permeability of the cornea limits the rapid transport of the drug to the recombinant tissue,so it is urgent to study the transmembrane transport properties of glaucoma drugs.ω=0.01,ω=0.05 two different mass fractions of the aqueous solution of pilocarpine as a glaucoma drug preparation,acting on the porcine cornea for drug permeability in vitro experiments.The experimental results show that:The growth rate of the drug concentration in the receiving group wasω=0.05 higher than that in the experimental group,and the growth rate of the drug concentration was proportional to the initial target concentration;The drug accumulation process is mainly composed of two stages of unsteady state and pseudo steady state.The function of drug accumulation and drug concentration,time,corneal thickness,and drug diffusion coefficient were obtained in the pseudo steady state;The diffusion coefficient of aqueous solution of pilocarpine across the cornea is about 2.47×10^(-6)cm^(2)/s.This paper is helpful to establish a mathematical description equation for transmembrane transport properties of glaucoma drugs in the future,thereby optimize the drug design of glaucoma drugs.

关 键 词：毛果芸香碱 角膜 药物累积 扩散系数 

分 类 号：R77[医药卫生—眼科]