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1. (WO2018126522) INJECTABLE INTRAOCULAR SUSTAINED-RELEASE ANTIVIRAL DRUG AND MANUFACTURING METHOD AND APPLICATION THEREOF

Pub. No.:    WO/2018/126522    International Application No.:    PCT/CN2017/074975
Publication Date: Fri Jul 13 01:59:59 CEST 2018 International Filing Date: Tue Feb 28 00:59:59 CET 2017
IPC: C07F 9/38
A61K 31/662
A61K 9/08
A61P 31/12
A61P 27/02
Applicants: BEIJING CHAOYANG HOSPITAL, CAPITAL MEDICAL UNIVERSITY
首都医科大学附属北京朝阳医院
TSINGHUA UNIVERSITY
清华大学
Inventors: TAO, Yong
陶勇
HUANG, Yanbin
黄延宾
SUN, Yuling
孙玉玲
CAO, Qingchen
曹庆辰
Title: INJECTABLE INTRAOCULAR SUSTAINED-RELEASE ANTIVIRAL DRUG AND MANUFACTURING METHOD AND APPLICATION THEREOF
Abstract:
An injectable intraocular sustained-release antiviral drug and a manufacturing method and application thereof. The antiviral drug is an insoluble phosphonoformate salt microcrystal. The insoluble phosphonoformate salt is a multivalent metal salt of phosphonoformic acid. The manufacturing method comprises: reacting a monovalent metal salt of phosphonoformic acid with a soluble multivalent metal salt in water; and obtaining a system containing the insoluble phosphonoformate salt microcrystal. An insoluble phosphonoformate salt microcrystal sustained release system is designed and developed to meet special needs of a sustained and controlled release intraocular injection. The nominal drug loading of the system is higher than 100%. The insoluble phosphonoformate salt microcrystal sustained-release antiviral can be released sustainably and stably in a vitreous chamber of a rabbit eye. The vitreous concentration of phosphonoformate continuously remains higher than an effective therapeutic concentration of sodium phosphonoformate. The antiviral drug has a sustained release period of up to 12 weeks and does not induce significant toxic or inflammatory reactions. The insoluble phosphonoformate salt can be used as an antiviral drug suitable for sustained release intravitreal injection technology.