提高乙酰唑胺滴眼液眼内通透性的实验研究  

Experimental study on improving ocular penetrability of acetazolamide ophthalmic solution

作　　者：陈瑛[1] 杨国华[1] 陈祖基[1] 徐岩[1] 张俊杰[1] 

机构地区：[1]河南省眼科研究所

出　　处：《眼科研究》2004年第6期614-616,共3页Chinese Ophthalmic Research

摘　　要：目的观察不同种类的穿透促进剂对乙酰唑胺滴眼液的眼内通透性作用.方法每次给兔滴药50 μL,30 min后抽取房水并进行反相高效液相色谱分析,计算房水中乙酰唑胺的质量浓度.结果1%、3.3%、10%乙酰唑胺滴眼液滴眼后30 min,前房药物质量浓度分别为( 0.073±0.013) μg/mL、(0.250±0.075) μg/mL、(0.032±0.074) μg/mL.与对照组相比,0.01%苯扎溴铵,1%甲基纤维素,1%、5%正丁醇以及5%、10%、20%二甲基亚砜均不能提高房水中乙酰唑胺的质量浓度(P＞0.05).0.012 5%～0.4%氮酮均可促进乙酰唑胺的眼内吸收,分别可提高前房药物质量浓度5.8～38.7倍(P＜0.01).此外,氮酮质量浓度和其对应的房水乙酰唑胺质量浓度的关系呈正相关(r= 0.92,P＜0.05).结论选择性地应用穿透促进剂可提高乙酰唑胺的眼内通透性.Objective To investigate the promoting effect of penetration enhancers on acetazolamide eye drop in rabbit. Methods Thirty minutes after instillation of 50 μL of acetazolamide ophthalmic solution, the aqueous humor samples were withdrawn and quantified by RP-HPLC, and the drug concentration in aqueous humor was measured. Results The acetazolamide concentration in aqueous humor was (0. 073±0. 013) , (0. 250±0. 075) and (0. 232±0. 074) μg/mL respectively at 30 minutes after the instillation of 1% , 3. 3% and 10% acetazolamide solution. Compared with the control group, 0.01% benzalkonium bromide, 1% methylcellulose, 1% and5% n-butyl alcohol as well as 5%, 10%,20% dimethyl sulfoxide could not increase the concentration of acetazolamide in aqueous humor(P>0.05). 0. 0125%-0. 4% of azone significantly enhanced the concentration of acetazolamide in aqueous humor by 5. 8 - 38. 7 times (P < 0. 01) , respectively. On the other hand, the concentrations of azone in ophthalmic solutions had a positive correlation with the concentration of acetazolamide in aqueous humor(r = 0.92, P < 0. 01). Conclusion A selective use of penetration enhancers can improve intraocular penetrability of acetazolamide eye drops.

关 键 词：乙酰唑胺滴眼液 穿透促进剂 眼内通透性 兔 

分 类 号：R775[医药卫生—眼科] R988.1[医药卫生—临床医学]