INFLUENCE OF ION-PAIRING SALTS ON THE TRANSCORNEAL PERMEABILITY OF IONIZED SULFONAMIDES

被引:3
作者
CONROY, CW
BUCK, RH
机构
[1] Department of Pharmacology and Therapeutics, University of Florida Health Science Center, College of Medicine, Gainesville, Florida
来源
JOURNAL OF OCULAR PHARMACOLOGY | 1992年 / 8卷 / 03期
关键词
D O I
10.1089/jop.1992.8.233
中图分类号
R77 [眼科学];
学科分类号
100212 ;
摘要
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.
引用
收藏
页码:233 / 240
页数:8
相关论文
共 11 条
[1]  
Monoi H., Possible existence of ion pairs at the mouths of ion channels, Biochim. Biophys. Acta, 693, pp. 159-164, (1982)
[2]  
Neubert R., Ion pair across membranes, Pharmaceutical Res, 6, pp. 743-747, (1989)
[3]  
Hadgraft J., Walters K.A., Wotton P.K., Facilitated transport of sodium salicylate across an artificial lipid membrane by azone, J. Pharm. Pharmacol, 37, pp. 725-727, (1985)
[4]  
Langguth P., Mutchler E., Lipophilisation of hydrophilic compounds: Consequences on transepidermal and intestinal transport of trospium chloride, Arzneim.-Frosch./Druq Res, 37, 11, pp. 1362-1366, (1987)
[5]  
Davis S.S., Tomlinson E., Wilson C.G., The effect of ion-association on the transcorneal transport of drugs, Br. J. Pharmacol, 64, pp. 444-445, (1989)
[6]  
Maren T.H., Ash V.I., Bailey E.M., A method for determination of carbonic anhydrase inhibitors, particularly of Diamox, Bull. Johns Hopk. Hosp, 95, pp. 244-255, (1954)
[7]  
O'Brien W.J., Edelhauser H.F., The corneal penetration of trifluorthymidine, adenine arabinoside, and idoxuridine: A comparative study, Invest. Ophthalmol, 16, pp. 1093-1103, (1977)
[8]  
Grant W.M., A study of the actions of quaternary ammonium compounds on the eye, Trans. Am. Ophthalmol. Soc, 54, pp. 417-451, (1956)
[9]  
Maren T.H., Jankowska L., Sanyal G., Edelhauser H.E., The transcorneal permeability of sulfonamide carbonic anhydrase inhibitors and their effect on aqueous humor secretion, Exp. Eye Res, 36, pp. 457-480, (1983)
[10]  
Plakogiannis F.M., Lien E.J., Harris O., Biles J.A., Partition of alkylsulfates of quaternary ammonium compounds: Structure dependence and transport study, J. Pharm. Sci, 59, pp. 197-200, (1970)