水蛭素滴眼液的研究

Studies on ophthalmic preparation of Hirudin

目的:制备水蛭素滴眼液,考察其稳定性及其对白内障防治作用。方法:以溶红细胞试验筛选促吸收剂,用正交试验(L9(33))确定水蛭素滴眼液的处方组成。选用硒性白内障和半乳糖性白内障大鼠动物模型考察水蛭素滴眼液对白内障的防治作用。结果:在pH7.4硼酸缓冲液中,以0.5%EDTA和0.5%壳聚糖作为该滴眼液的促吸收剂。该制剂在4℃冰箱和室温放置12个月,其抗凝活力,外观和pH值均无改变。本制剂对眼无刺激性,减轻晶状体浑浊程度,降低MDA含量,增大SOD活力,增加γ蛋白含量。结论:本制剂性质稳定,对硒性及半乳糖性大鼠白内障有显著的防治作用。

Objective：To investigate the preparation, stability and effect of Hirudin eyedrops for the treatment of cataract in rats. Methods：The absorption promoters were screened using globulolytic test; the formulation was optimized by orthogonal design L9 （3^3）;the rat cataract modules induced by selenium and galactose were used as tools to evaluate the efficacy of cataract treatment. Results： In the boric acid buffer solution （pH 7.4）, 0.5 % EDTA and 0.5 % chitosan were considered to be the optimal absorption promoters The formulation was stable at 4℃ and ambient temperature for 12 months, i.e., no changes of antithrombin actlvitv, appearance and pH value. The ophthalmic fornullatinn showed no irritation to rat＇ s eyes. The Hirndin rats experienced regression of the lens opacities, decrease of MDA concentrations and increase of SOD activity and γ protein levels. Conclusion： The stable ophthalmic preparation of Hirudin could manage the cataract induced by selenium and galactose in rats .