Igarashi H, Katsuta Y, Sawa K, Nakazato Y, Kawasaki T
Department of Dental Pharmacology, Ohu University School of Dentistry, Fukushima, Japan.
Fundam Appl Toxicol. 1990 Apr;14(3):554-9.
Using an in vitro method the authors have investigated whether 8-hydroxycarteolol.HCl(8-OH carteolol) and 8-OH carteolol with benzalkonium chloride affected intact isolated porcine corneas to the same or to a different degree as carteolol.HCl (carteolol) or carteolol with benzalkonium chloride. These ophthalmically used drugs were applied as solutions of varying concentrations to the epithelial surface only, to the endothelial surface only, or to both surfaces of porcine corneas. The resultant opacities were determined using an opacitometer. In general, 8-OH carteolol and 8-OH carteolol with benzalkonium chloride caused less opacity to develop than carteolol and carteolol with benzalkonium chloride. This suggests that 8-OH carteolol may be a safer drug than carteolol for ophthalmic use. It is very interesting to note that compounds with two nitrogens, e.g., 8-OH carteolol, caused greater opacity in the intact cornea when applied to the endothelial surface than when applied to both the epithelial and endothelial surfaces; however, compounds with none or one nitrogen caused greater opacity in the intact cornea when applied to both surfaces than when applied to the endothelial surface.
作者采用体外方法研究了盐酸8 - 羟基卡替洛尔（8 - OH卡替洛尔）以及8 - OH卡替洛尔与苯扎氯铵的组合对完整离体猪角膜的影响，其程度与盐酸卡替洛尔（卡替洛尔）或卡替洛尔与苯扎氯铵的组合相同或不同。这些眼科用药以不同浓度的溶液形式仅应用于猪角膜的上皮表面、仅应用于内皮表面或应用于猪角膜的两个表面。使用不透光度计测定由此产生的混浊度。一般来说，8 - OH卡替洛尔以及8 - OH卡替洛尔与苯扎氯铵的组合所导致的混浊度比卡替洛尔以及卡替洛尔与苯扎氯铵的组合要低。这表明8 - OH卡替洛尔作为眼科用药可能比卡替洛尔更安全。非常有趣的是，含有两个氮原子的化合物，例如8 - OH卡替洛尔，当应用于内皮表面时，在完整角膜中产生的混浊度比同时应用于上皮和内皮表面时更大；然而，不含氮原子或含有一个氮原子的化合物，当应用于两个表面时，在完整角膜中产生的混浊度比应用于内皮表面时更大。
