自微乳给药系统的促吸机制、固化及评价方法-药学论文-基础医学论文-医学论文.docxVIP

自微乳给药系统的促吸机制、固化及评价方法-药学论文-基础医学论文-医学论文 ——文章均为WORD文档，下载后可直接编辑使用亦可打印—— 　　摘 要：　自微乳给药系统能够显着提高水难溶性药物的口服生物利用度,且最终的给药形式多样,在推进高生物利用度口服递药系统的发展中,表现出良好的应用前景。但自微乳给药系统也存在诸如存储运输不便、稳定性不佳、体外释药评价局限等问题。随着近年来新型载体材料和制剂技术的发展,对固体自微乳给药系统、过饱和自微乳给药系统等新型制剂的研究日益增多,在弥补传统自微乳给药系统不足的同时,可发挥自微乳给药系统的优势。综述自微乳给药系统的辅料组成、促进药物口服吸收的机制、固化方法及体外释药评价方法的研究进展。 　　关键词：　自微乳给药系统; 淋巴摄取; 药物沉淀; 自微乳固化; 体外释药评价; 　　Abstract：　Self-microemulsifying drug delivery system (SMEDDS) can significantly improve the oral bioavailability of water-insoluble drugs with diversified forms of administration,which has shown great application prospects in promoting the development of oral drug delivery system with high bioavailability.There are still some problems in SMEDDS such as inconvenience of storage and transportation,poor stability,and limitations of drug release evaluation.Recently,with the development of new materials and new technology in drug preparation,there have been an increasing number of researches on new pharmaceutical preparations such as solid self-microemulsifying delivery system and supersaturated self-microemulsifying delivery system,which can make up the deficiency of traditional SMEDDS and make use of its advantages.This paper reviews the excipients composition,oral absorption mechanism,solidification methods and release evaluation methods of SMEDDS. 　　Keyword：　self-microemulsifying drug delivery system; lymphatic uptake; drug precipitation; solidification; evaluation of drug release; 　　自微乳给药系统(self-microemulsifying drug delivery system,SMEDDS)是由药物、油相、乳化剂和助乳化剂形成的均一澄清液体,在室温下遇水可自发乳化形成水包油型(O/W)微乳[1]。SMEDDS口服后在胃肠道作用下,先经胃液分散稀释形成微乳,再于小肠中经各种消化酶和胆盐等作用被消化。SMEDDS能够通过提高药物溶解度、增加细胞通透性、触发淋巴转运等机制显着提高水难溶性药物的口服生物利用度[2,3]。虽然SMEDDS能够显着改善难溶性药物的口服生物利用度,但传统的自微乳制剂仍存在剂型单一、稳定性不佳、存储运输不便、无法实现缓控释等问题和挑战[4],因此新型自微乳给药系统的开发也成为近几年的研究热点。 　　1 、自微乳给药系统的新型辅料 　　SMEDDS中油相可增大药物的溶解度,避免药物与外周环境直接接触,保护药物不被体内活性物质降解,增加药物稳定性的同时降低药物刺激性。乳化剂对SMEDDS的稳定性、自乳化性起重要作用,常用乳化剂有脂肪酸山梨坦、聚山梨酯及十二烷基硫酸钠等。助乳化剂可通过改变油水界面曲率、增加界面膜流动性帮助纳米乳的形成并维持其热力学稳定,常用的助乳化剂有乙醇、丁醇、丙