地塞米松温敏凝胶的制备及其特性评价  

Preparation and Evaluation of Dexamethasone Thermosensitive Gel

作　　者：陈佛华 袁燕 莫镇杰 班俊峰[1,2] CHEN Fohua;YUAN Yan;MO Zhenjie;BAN Junfeng(Guangdong Provincial Key Laboratory of New Drug Formulations,Guangdong Pharmaceutical University,Guangzhou,Guangdong 510006,China;Foshan First People’s Hospital,Foshan,Guangdong 528000,China)

机构地区：[1]广东药科大学,广东省药物新剂型重点实验室,广东广州510006 [2]佛山市第一人民医院,广东佛山528000

出　　处：《今日药学》2021年第10期761-764,768,共5页Pharmacy Today

基　　金：广东省自然科学基金项目(2019A1515011018);2019年大学生创新创业项目(201910573004);广东药科大学“专创融合”研究成果。

摘　　要：目的制备具有生物黏附作用的地塞米松温敏凝胶滴眼液,降低泪液消除,提高眼部生物利用度。方法将地塞米松制成具有温敏特型的凝胶,对其胶凝温度、胶凝前后的流变特性、凝胶的黏附性质及凝胶在兔眼的泪液消除情况进行测定。结果所制备的凝胶相转变温度为(26.9±0.2)℃,在生理和非生理条件流变特性符合滴眼液要求,表现出一定的生物黏附性,与市售制剂相比,凝胶的生物利用度提高了16.1倍,泪液消除时间更长。结论所制备的地塞米松凝胶的两相变化显著,流变特性、生物黏附性和泪液消除动力学参数符合眼内制剂要求。OBJECTIVE To prepare of bioadhesive dexamethasone thermosensitive gel eye drops,to reduce tear elimination and improve bioavailability of dexamethasone in the eyes.METHODS Dexamethasone was made into a thermosensitive gel,whose gelation temperature,rheological properties,adhesion properties before and after gelation,and tear elimination in rabbit eyes were measured.RESULTS The phase transition temperatures of the thermosensitive in situ gel was(26.9±0.2)℃.The rheological properties and bioadhesion met the requirements of thermosensitive eye drops under physiological and non-physiological conditions.Compared with the commercial preparation,the bioavailability of the gel was increased by 16.1 time and tear elimination was longer.CONCLUSION The prepared dexamethasone thermosensitive in situ gel have significant changes in two phases.The rheological properties,bioadhesion and tear elimination kinetic parameters of gel meet the requirements of intraocular preparation.

关 键 词：凝胶 流变特性 生物黏附性 泪液消除动力学 生物利用度 

分 类 号：R943[医药卫生—药剂学]