醋酸地塞米松脂质体滴眼液的制备

Preparation of dexamethasone acetate ophthalmic liposomal solution

目的制备醋酸地塞米松脂质体滴眼液,考察包封率及粒径的影响因素并进行质量评价。方法以葡聚糖凝胶分离脂质体和游离醋酸地塞米松;采用紫外分光光度法测定醋酸地塞米松脂质体滴眼液的包封率。考察制备工艺和处方因素对醋酸地塞米松脂质体滴眼液的包封率及粒径的影响。评价醋酸地塞米松脂质体滴眼液的质量。与醋酸地塞米松滴眼液相比,考察醋酸地塞米松脂质体滴眼液的眼部滞留时间。结果通过优化制备工艺和处方,醋酸地塞米松脂质体滴眼液的包封率达88.70%,粒径为133.8nm,醋酸地塞米松脂质体滴眼液的眼部滞留时间是普通滴眼液的4倍。结论制备的醋酸地塞米松脂质体滴眼液包封率较高,粒径小,显著延长了药物的滞留时间,方法可行。

Objective To prepare dexamethasone acetate （DA） ophthalmic liposomal solution, to determine the in- fluence factors for entrapment efficiency and size, and to evalue its quality. Methods Free DA and liposomes were separated by Sephadex G-50. Ultraviolet spectrophotometry was used to determine the entrapment efficiency of DA ophthalmic liposomal solution. Various influence factors for the entrapment efficiency and size of DA ophthalmic liposomal solution were investigated. The quality of DA ophthalmic liposomal solution was evaluated. Compared with DA eye drops, the tention time of DA ophthalmic liposomal solution was tested. Results Through optimizing the formulations and preparation conditions, DA ophthalmic liposomal solution was obtained with high entrapment efficiency at 88.70% and the mean diameter at 133.8 nm. The retention time of DA ophthalmic liposomal solution was 4 times that of DA eye drops. Conclusion DA ophthalmic liposomal solution with high entrapment efficiency and small size is prepared, and the method proves feasible. The retention time is extended obviously.