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6-羟基乙氧基-2-苯并噻唑磺酰胺的角膜和巩膜穿透性研究:一种局部碳酸酐酶抑制剂

Corneal and scleral penetration studies of 6-hydroxyethoxy-2-benzothiazole sulfonamide: a topical carbonic anhydrase inhibitor.

作者信息

Kao K D, Lu D W, Chiang C H, Huang H S

机构信息

Department of Ophthalmology, National Defense Medical Center, Taipei, Taiwan, Republic of China.

出版信息

J Ocul Pharmacol. 1990 Winter;6(4):313-20. doi: 10.1089/jop.1990.6.313.

Abstract

A newly synthesized topical carbonic anhydrase inhibitor, 6-hydroxyethoxy-2-benzothiazole sulfonamide (6-HS), was used as a model drug to determine its corneal and scleral permeabilities in rabbit eyes. The corneal permeability coefficient of 6-HS for short duration glaucoma and normal rabbit eye was not significantly different (its mean value was around 2.9 x 10(-6) cm/sec), while the corneal permeability coefficient for long duration glaucoma rabbit eye was 1.8 times greater than that for the normal eye. The sclera was found to have a higher permeability than the cornea in that after four hours perfusion the amount of drug which passed through the sclera was 11 times greater than that of the cornea. In addition, it was also noted that after topical instillation of 50 microL of 3% 6-HS gel the aqueous humor concentrations of 6-HS in short duration glaucoma eye and normal eye were not statistically different.

摘要

一种新合成的局部碳酸酐酶抑制剂6-羟基乙氧基-2-苯并噻唑磺酰胺(6-HS)被用作模型药物,以测定其在兔眼中的角膜和巩膜通透性。6-HS在短期青光眼兔眼和正常兔眼中的角膜通透系数无显著差异(其平均值约为2.9×10⁻⁶厘米/秒),而在长期青光眼兔眼中的角膜通透系数比正常眼大1.8倍。研究发现巩膜的通透性高于角膜,因为在灌注4小时后,通过巩膜的药物量是通过角膜的11倍。此外,还注意到在局部滴注50微升3%的6-HS凝胶后,短期青光眼眼和正常眼中6-HS的房水浓度无统计学差异。

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