Valeri P, Romanelli L, Martinelli B, Guglielmotti A, Catanese B
Institute of Pharmacology and Pharmacognosy, University of Rome La Sapienza, Italy.
Lens Eye Toxic Res. 1989;6(3):465-75.
The time courses of aspirin and salicylate in plasma and ocular tissues of rabbits were investigated after the i.v. administration of aspirin. Unhydrolyzed aspirin rapidly disappears from plasma and many ocular compartments but persists up to 4 hours in aqueous and vitreous humours. Salicylate decreases in plasma follow an exponential kinetics; in aqueous humour and in vascularized tissues the behaviour is similar but with a half-life longer than in plasma. In the cornea, lens and vitreous humour, the concentration of salicylate reaches a peak between 2 and 4 hours, then it decreases very slowly. Our results show that aspirin is protected from the hydrolytic action of plasmatic esterases in aqueous and vitreous humours but is rapidly hydrolyzed in the cornea and lens by local esterases present in these tissues. It is possible that both aspirin and salicylate leave the eye by means of an active transport. Our results also indicate that salicylate can accumulate in the cornea, lens and retina when aspirin is administered repeatedly.
静脉注射阿司匹林后,研究了家兔血浆和眼组织中阿司匹林和水杨酸盐的时程。未水解的阿司匹林迅速从血浆和许多眼房消失,但在房水和玻璃体液中可持续长达4小时。血浆中水杨酸盐的减少遵循指数动力学;在房水和血管化组织中,其行为相似,但半衰期比血浆中长。在角膜、晶状体和玻璃体液中,水杨酸盐浓度在2至4小时之间达到峰值,然后非常缓慢地下降。我们的结果表明,阿司匹林在房水和玻璃体液中受到血浆酯酶水解作用的保护,但在角膜和晶状体中被这些组织中存在的局部酯酶迅速水解。阿司匹林和水杨酸盐都有可能通过主动转运离开眼睛。我们的结果还表明,反复给予阿司匹林时,水杨酸盐可在角膜、晶状体和视网膜中蓄积。