胰岛素经眼给药的药物代谢动力学

Pharmacokine tics of insulin via topical ocular administration

用国产胰岛素在54只新西兰大耳白家兔体内观察其经眼给药后药物代谢动力学特征。结果表明,分子量约为6000的胰岛素滴眼后能有效地进入血液循环。体内药物动力学为开放性一级动力学—房室模型。消除半衰期为40～60min,与静脉注射相比,消除半衰期明显延长。达峰时间为20～50min。金属络合剂EDTA对胰岛素的经眼吸收有促进作用。经眼给药后体内药物的浓度呈现出剂量依赖性。

54 New Zealand rabbits were used to study the pharmacokinetic parameters of insulin through ophthalmic absorption. It was shown that insulin with a moiecular weight of 6000 when instilled to the eyes could reach the blood circulation and was dose dependece. The pharmacokinetic model was of first order and the half life of insulin thus instituted was 40 ~60 minutes being much prolonged than a i.v. bolus injection. EDTA could enhance the insulin absorption through the eyes.