Fujio N, Kusumoto N, Odomi M
Drug Safety Research Center, Tokushima Research Inst., Otsuka Pharmaceutical Co. Ltd., Japan.
Acta Ophthalmol (Copenh). 1994 Dec;72(6):688-93. doi: 10.1111/j.1755-3768.1994.tb04681.x.
To investigate the distribution and elimination of carteolol in pigmented rabbits, 14C-carteolol eye drops were instilled singly and repeatedly. After single ocular instillation, the radioactivity in the iris and ciliary body reached maximum levels at 24 h. The elimination rate of pigmented tissues decreased at a half-life of approximately 15 days. The concentration of radioactivity in pigmented tissues increased markedly by repeating the ocular instillation and reached a maximum after the 80th repeated instillation. The concentration of radioactivity at 1 h after 80th instillation was 63.7 times that in the iris, 61.1 times that in the ciliary body and 17.2 times that in the retina & choroid after single instillation. No accumulation of radioactivity was found in other ocular tissues.
为研究卡替洛尔在有色兔体内的分布与消除情况，单次及多次滴注14C - 卡替洛尔滴眼液。单次眼部滴注后，虹膜和睫状体中的放射性在24小时达到最高水平。有色组织的消除率以约15天的半衰期下降。通过重复眼部滴注，有色组织中的放射性浓度显著增加，并在第80次重复滴注后达到最大值。第80次滴注后1小时的放射性浓度是单次滴注后虹膜中浓度的63.7倍、睫状体中浓度的61.1倍以及视网膜和脉络膜中浓度的17.2倍。在其他眼组织中未发现放射性蓄积。
