THE EFFECT OF CHLORHEXIDINE ACETATE ON THE CORNEAL PENETRATION OF SORBITOL FROM AN ARNOLOL FORMULATION IN THE ALBINO RABBIT

被引:12
作者
ASHTON, P [1 ]
DIEPOLD, R [1 ]
PLATZER, A [1 ]
LEE, VHL [1 ]
机构
[1] UNIV SO CALIF,SCH PHARM,1985 ZONAL AVE,LOS ANGELES,CA 90033
来源
JOURNAL OF OCULAR PHARMACOLOGY | 1990年 / 6卷 / 01期
关键词
D O I
10.1089/jop.1990.6.37
中图分类号
R77 [眼科学];
学科分类号
100212 ;
摘要
The effect of chlorhexidine acetate on the corneal penetration of sorbitol was evaluated in vitro using the enucleated pigmented rabbit cornea mounted in a modified Ussing chamber. Sorbitol penetrated the cornea poorly when compared with arnolol, a beta blocker. Sorbitol penetration was improved 85% by 0.01% chlorhexidine acetate, 2.9 times by 0.1% EDTA, and 9.6 times by stripping the corneal epithelium prior to the start of the experiment. By comparison, 0.01% chlorhexidine acetate and stripping the corneal epithelium improved the corneal penetration of arnolol only 30% and 74%, respectively, whereas stripping the corneal epithelium did not affect the corneal penetration of chlorhexidine acetate. Collectively, the above findings indicate that changes in corneal integrity may dramatically affect the corneal penetration of some inert excipients in ophthalmic formulations. Such a possibility must be considered carefully in the selection of excipients. © 1990, Mary Ann Liebert, Inc. All rights reserved.
引用
收藏
页码:37 / 42
页数:6
相关论文
共 13 条
  • [1] Gasset A.R., Ishii Y., Kaufman H.E., Miller T., Cytotoxicity of ophthalmic preservatives, Am. J. Ophthalmol, 78, pp. 98-105, (1974)
  • [2] Pfister R.R., Burstein N.L., The effects of ophthalmic drugs, vehicles, and preservatives on corneal epithelium: a scanning electron microscope study, Invest. Ophthalmol, 15, pp. 246-259, (1976)
  • [3] Burstein N.L., Preservative alteration of corneal permeability in humans and rabbits, Invest. Ophthalmol. Vis. Sci, 25, pp. 1453-1457, (1984)
  • [4] Camber O., Edman P., Influence of some preservatives on the corneal permeability of pilocarpine and dexamethasone, in vitro, Int. J. Pharm, 39, pp. 229-234, (1987)
  • [5] Cohnen E., Armah B.I., Arnolol (BDF 7584): An oculoselective β-receptor antagonist for the treatment of glaucoma, Arch. Pharmacol. (Suppl.), 338, (1988)
  • [6] Schoenwald R.D., Huang H.S., Corneal penetration behavior of β-blocking agents I: Physicochemical factors, J. Pharm. Sci, 72, pp. 1266-1272, (1983)
  • [7] O'Brien J.W., Edelhauser H.F., The corneal penetration of trifluorothymidine, adenine arabinoside, and idoxuridine: a comparative study, Invest. Ophthalmol. Vis. Sci, 16, pp. 1093-1103, (1977)
  • [8] Chang S.C., Bundgaard H., Buur A., Lee V.H.L., Improved corneal penetration of timolol by prodrugs as a means to reduce systemic drug load, Invest. Ophthalmol. Vis. Sci, 28, pp. 487-491, (1987)
  • [9] Lee V.H.L., Robinson J.R., Topical ocular drug delivery: recent developments and future challenges, J. Ocular Pharmacol, 1, pp. 67-108, (1986)
  • [10] Grass G.M., Cooper E.R., Robinson J.R., Mechanisms of corneal drug penetration III: Modeling of molecular transport, J. Pharm. Sci, 77, pp. 24-26, (1988)