Maren T H, Jankowska L
Curr Eye Res. 1985 Apr;4(4):399-408. doi: 10.3109/02713688509025154.
In the past five years we have studied the penetration of locally applied sulfonamides into the eye, with a view toward developing new topical carbonic anhydrase inhibitors for the treatment of glaucoma. The drugs varied by 400 fold in their permeability to the anterior chamber and 20,000 fold in permeability to the posterior chamber. We report now on two particular findings related to drug structure: 1) Transcorneal permeability of the ionic or dissociated form of the drug is relatively high -- some 1/4 that of the undissociated form. 2) Depending on the structure, certain compounds are sequestered in the cornea (presumably the stroma) and form a release system into the anterior aqueous.
在过去五年中,我们研究了局部应用的磺胺类药物进入眼部的渗透情况,目的是开发用于治疗青光眼的新型局部碳酸酐酶抑制剂。这些药物在前房的渗透率相差400倍,在后房的渗透率相差20000倍。我们现在报告与药物结构相关的两个特别发现:1)药物离子或解离形式的透角膜渗透率相对较高,约为未解离形式的1/4。2)根据结构不同,某些化合物会被隔离在角膜(可能是基质)中,并形成一个向前房水释放的系统。