阿奇霉素原位凝胶滴眼液眼部滞留性和刺激性研究

Corneal Retention and Irritation Behavior of Azithromycin Ophthalmic Gel

目的考察阿奇霉素原位凝胶滴眼液在家兔眼部的滞留性和刺激性。方法采用γ-闪烁扫描示踪技术,以放射强度为指标,评价制剂在眼部的滞留时间,应用Draize评分标准法考察阿奇霉素原位凝胶滴眼液单次给药和多次给药后对家兔眼部的刺激性。结果与普通滴眼液相比,阿奇霉素原位凝胶滴眼液的眼部滞留时间延长了约2.5倍,角膜刺激性评价实验表明制剂眼部相容性良好。结论阿奇霉素原位凝胶滴眼液眼部刺激性小,滞留时间长,具有广阔的研究开发前景。

Objective To investigate corneal retention and irritation behavior of azithromycin in situ gel for ophthalmic drug delivery. Methods The r-scintigraphy was used to evaluate the residence time of the preparation in rabbit eyes, using radiant intensity as the indicator. Draize method was employed to study the irritation behavior of azithromycin in ophthalmic gel through single and multiple doses. Results The corneal retention of azithromycin ophthalmic gel was enhanced significantly and the residence time was prolonged 2.5 times compared with that of ordinary eye drops. The irritation tests showed an excellent biocompatibility of azithromycin ophthalmic gel. Conclusion The azithromycin in situ gel exhibites not only little corneal irritation but also longer residence time, which is worthy of exploitation.