一种阿奇霉素超细粉体原位凝胶滴眼液及其制备方法技术

本发明专利技术提供一种阿奇霉素超细粉体原位凝胶滴眼液及其制备方法，首先利用适当的方法将药物进行微粉化，显著提高药物的溶出速率和溶解度。然后采用海藻酸钠为离子敏感凝胶基质，或是采用泊洛沙姆407和泊洛沙姆188为温敏凝胶基质制备成一种在体外呈现液体状态，滴入眼内后成凝胶状态的眼用制剂。本滴眼液在4℃条件下贮藏稳定，含量均一，不必二次配制，从而减少污染机会。本发明专利技术将阿奇霉素超细粉体与原位凝胶结合应用于细菌性角膜炎及沙眼的治疗，通过超细粉体和凝胶的双重作用，在延长制剂在眼部滞留时间的同时起到缓释作用，提高药物局部生物利用度及患者的顺应性，增加药物的角膜吸收以减少眼部用药的全身吸收而引起的毒副作用。

Azithromycin superfine powder in-situ gelling eye drops and preparation method thereof

The present invention provides a azithromycin superfine powder in-situ gelling eye drops and a preparation method thereof. Firstly, the medicine is micronized by an appropriate method, and the dissolution rate and solubility of the medicine are remarkably improved. Then by using sodium alginate as ion sensitive gel matrix, or by using poloxamer 407 and poloxamer 188 as gel matrix to prepare Wen Min into a state of liquid in vitro, drops into eyes into gel state ophthalmic preparations. The eye drops are stored stably at 4 DEG C and have uniform content and need not be prepared two times so as to reduce the chance of pollution. The treatment of azithromycin superfine powder and in situ gel applied to bacterial keratitis and trachoma, through the dual role of superfine powder and gel, to prolong the residence time in the preparation of sustained-release effect in the eye at the same time, improve the local drug bioavailability and patient compliance, increase the drug absorption in the cornea to reduce the ocular drug systemic absorption caused by the side effects.

【技术实现步骤摘要】

【技术保护点】
１．一种阿奇霉素超细粉体原位凝胶滴眼液，其特征在于：其处方重量百分组成为：阿奇霉素０．５％－２％，凝胶基质原料０．１％－２８％，ＨＰＭＣ　０．１％－５％，渗透压调节剂０．１％－５％，防腐剂０．０１％－５％，抗氧剂０．０１％－５％，稳定剂０．０１－５％，注射用水余量。

【技术特征摘要】

【专利技术属性】
技术研发人员：王东凯，
申请(专利权)人：沈阳药科大学，
类型：发明
国别省市：89