新目安眼用凝胶剂等四种眼用制剂离体角膜渗透特性比较研究  

Comparison Research on Permeability in Isolated Cornea of Four Ophthalmic Preparations Including New Mu'an Ophthalmic Gel

作　　者：张湘晖[1,2] 陈光宇 赵碧清[3] 吕毅[4] 郭畅 何群[3,5] 

机构地区：[1]湖南中医药大学第一临床医学院,长沙410007 [2]国家中医药管理局中医眼科重点学科 [3]湖南中医药大学药学院 [4]湖南省食品药品职业技术学院 [5]湖南省教育厅药学“十二五”重点学科

出　　处：《中国药师》2018年第9期1570-1574,共5页China Pharmacist

基　　金：湖南省教育厅科研基金项目(编号:12C0270、14C0740));湖南省自然科学基金项目(编号:11JJ3107);大学生研究性学习和创新性实验计划项目(编号:校行教字[2012]13号)

摘　　要：目的:探索更昔洛韦替代阿昔洛韦组成的新目安眼用凝胶剂离体角膜渗透性能是否优于原目安眼用凝胶剂及市售制剂。方法:HPLC法测定更昔洛韦及阿昔洛韦含量并以此为指标,采用Franz扩散池法,进行离体角膜渗透性实验,建立数学模型,通过数学及统计学处理提取角膜渗透特性参数,比较新目安眼用凝胶剂与目安眼用凝胶剂渗透速度及渗透总量的差异。结果:新目安眼用凝胶剂角膜渗透特性优于目安眼用凝胶剂(角膜渗透速度是后者的3.452倍,角膜渗透数量是后者的1.832倍),亦优于市售0.15%更昔洛韦眼用凝胶剂(角膜渗透速度是后者的2.029倍),市售0.15%更昔洛韦眼用凝胶剂角膜渗透特性优于市售3%阿昔洛韦眼膏(角膜渗透数量是后者的2.028倍)。结论:新目安眼用凝胶剂离体角膜渗透性能符合眼用制剂需求,更昔洛韦替代阿昔洛韦组成的新目安眼用凝胶剂离体角膜渗透性能优于目安眼用凝胶剂,给药次数及间隔时间基本科学、合理、可行,并为下一步药效、毒理、临床研究提供依据。Objective： To study the permeability superiority in isolated cornea of new Mu＇an ophthalmic gel containing ganciclovir compared with that of Mu＇an ophthalmic gel containing acyclovir and commercially available preparations. Methods： The permeability test was performed on isolated cornea in Franz diffusion cells. The penetration amounts of ganciclovir and acyclovir were determined by HPLC. A mathematical model was established to calculate the extraction penetration parameters of isolated cornea through mathematical and statistical treatment. The differences of penetration velocity and total amount were compared between new Mu＇ an ophthalmic gel and old Mu＇ an ophthahnic gel. Results： The corneal permeability of new Mu＇ an ophthalmic gel was better than that of Mu＇an ophthal- mic gel. The corneal penetration velocity of new Mu＇ an ophthalmic gel was almost 3. 452 times of that of Mu＇ an ophthalmic gel. The total corneal penetration amount of new Mu＇ an ophthalmic gel was almost 1. 832 times of that of Mu＇an ophthalmic gel. New Mu＇ an ophthalmic gel was better than commercially available 0. 15% ganciclovir ophthalmic gel and 3% acyclovir eye cream. The corneal penetration velocity of new Mu＇ an ophthalmic gel was almost 2. 029 times of that of 0.15% ganciclovir ophthalmic gel. The total corne- al penetration amount of new Muan ophthalmic gel was almost 2.028 times of that of 3% acyclovir eye cream. Conclusion： The isola- ted cornea permeability characteristics of new Mu＇an ophthalmic gel meet the demand to ophthalmic preparations, which are better than those of Mu＇an ophthalmic gel containing acyclovir. The administration time and interval time are both essentially scientific ,reasonable and feasible, which provide basis for further studies on pharmacodynamics, toxicology and clinical research.

关 键 词：新目安眼用凝胶剂 目安眼用凝胶剂 更昔洛韦 阿昔洛韦 离体角膜渗透 FRANZ扩散池 

分 类 号：R945[医药卫生—微生物与生化药学]