Conroy C W, Buck R H
Department of Pharmacology and Therapeutics, University of Florida Health Science Center, College of Medicine, Gainesville.
J Ocul Pharmacol. 1992 Fall;8(3):233-40. doi: 10.1089/jop.1992.8.233.
The effects of cationic ammonium, phosphonium, and arsonium ion pairing salts as well as anionic organic and inorganic salts on the transcorneal permeability of ionized sulfonamide carbonic anhydrase inhibitors have been studied in the excised rabbit cornea. Benzolamide, trichloromethazolamide (TCM), MK-927, and quaternary ammonium sulfonamide (QAS) were examined. The enhancement in the first-order rate constants (k(in)) for the first compound in the presence of pairing salts was as much as 15 times the basal rate, with smaller increases seen with the remaining three drugs. Ion pairing salts may represent a means for enhancing the transcorneal permeability of highly ionized drugs.
在离体兔角膜中研究了阳离子铵盐、鏻盐和胂盐离子对盐以及阴离子有机和无机盐对离子化磺酰胺碳酸酐酶抑制剂经角膜渗透性的影响。研究了苯佐酰胺、三氯甲唑酰胺(TCM)、MK-927和季铵磺酰胺(QAS)。在存在离子对盐的情况下,第一种化合物的一级速率常数(k(in))的增强高达基础速率的15倍,其余三种药物的增加幅度较小。离子对盐可能是提高高度离子化药物经角膜渗透性的一种手段。