制剂新技术在双嘧达莫新剂型中的研究进展  

Novel preparation techniques used in new dosage form of dipyridamole:research advances

作　　者：田霞 丁江生 范云周 全东琴 TIAN Xia;DING Jiang-sheng;FAN Yun-zhou;QUAN Dong-qin(Yunnan Institute ofMateria Medica,Yunnan Bai Yao Group Innovation R＆D Center,Yunnan Province Company Key Laboratory for TCM and Ethnic Drug of New Drug Creation,Kunming 650111,China;Beijing Jiashilianbo Pharmaceutial Co.Ltd.,Beijing 100071,China;Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)

机构地区：[1]云南省药物研究所,云南白药集团创新研发中心,云南省中药和民族药新药创制企业重点实验室,昆明650111 [2]北京嘉事联博医药科技有限公司,北京100071 [3]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2018年第4期253-257,共5页Journal of International Pharmaceutical Research

基　　金：云南省科技计划"青年项目"资助(2014FD087)

摘　　要：双嘧达莫是临床常用的抗血小板聚集药物,近年来在抗病毒和抗肿瘤等方面也显示出极大的潜力。但因其溶解度差且具有pH依赖性,在胃肠道吸收窗窄,普通口服制剂存在生物利用度低、个体间差异大及临床疗效不一致的问题。目前,基于固体分散体、胃内漂浮、微环境pH调控、药物-蛋白质复合物和纳米技术的新型给药系统是提高双嘧达莫口服吸收的主要研究方向。本文综述了双嘧达莫新剂型和新技术研究进展,以期为开发安全有效和依从性好的新制剂提供参考。Dipyridamole,a widely used drug in clinics that inhibits platelet agregation,also shows great potential for anti-viral and anti-tumor effect in recent years. However,with its poor and p H-dependent solubility as well as the narrow absorption window in the gastrointestinal tract,the conventional oral dosage forms have problems of low bioavailability,high inter-subject variability and insufficient drug efficacy. The novel drug delivery systems based on solid dispersion,gastro-floating,microenvironmental p H-modification,drug-protein complex and nanoparticle technologies are the effective methods to enhance oral drug absorption. In this paper we review the recent advances in novel dosage form and preparation technology of dipyridamole,to provide references for development of novel preparation with good safety,therapeutic efficacy and patient compliance.

关 键 词：双嘧达莫 剂型 固体分散体 胃内漂浮 微环境pH 

分 类 号：R94[医药卫生—药剂学]