Edelhauser H F, Maren T H
Department of Physiology, Medical College of Wisconsin, Milwaukee 53226.
Arch Ophthalmol. 1988 Aug;106(8):1110-5. doi: 10.1001/archopht.1988.01060140266039.
Corneal penetration of sulfonamide carbonic anhydrase inhibitors for topical treatment of glaucoma has been tested in human eye bank and rabbit tissue. Paired corneas, with the epithelia intact or removed, and excised sclera were perfused in vitro. Corneal permeability (Kp) to methazolamide and ethoxzolamide was similar in both species, but for benzolamide and bromacetazolamide the Kp was greater in humans. Human corneas without epithelium had Kp the same as scleral Kp. Topical methazolamide (6 mmol/L) was studied in vivo in rabbits and in ten humans before cataract surgery. The mean (+/- SE) concentration in the rabbit aqueous was 3.2 +/- 1.4 mumol/L at eight minutes and 1.2 +/- 0.16 mumol/L at one hour. In humans, less than 0.2 mumol/L was detected at eight minutes; at one hour none was detected in three cases, and 0.4 +/- 0.08 mumol/L was detected in four cases. Lower permeability in humans than rabbits may result from a fourfold greater blinking rate, a twofold greater tear turnover, and a twofold lower corneal/conjunctival area.
用于青光眼局部治疗的磺胺类碳酸酐酶抑制剂的角膜穿透性已在人眼库组织和兔组织中进行了测试。将上皮完整或去除的配对角膜以及切除的巩膜进行体外灌注。两种物种中，角膜对甲唑酰胺和乙氧唑酰胺的渗透率（Kp）相似，但对于苯唑酰胺和溴醋唑酰胺，人的Kp更高。无上皮的人角膜的Kp与巩膜的Kp相同。在兔和十名白内障手术前的人中对局部用甲唑酰胺（6 mmol/L）进行了体内研究。兔房水中的平均（±SE）浓度在8分钟时为3.2±1.4 μmol/L，1小时时为1.2±0.16 μmol/L。在人中，8分钟时检测到的浓度低于0.2 μmol/L；1小时时，3例未检测到，4例检测到0.4±0.08 μmol/L。人比兔的渗透率低可能是由于眨眼频率高四倍、泪液更新率高两倍以及角膜/结膜面积低两倍所致。
