首页> 外国专利> A PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ARTHRITIS COMPRISING HYALURONIC ACID-METHOTREXATE CONJUGATE AND A METHOD FOR PREPARATION THEREOF

A PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ARTHRITIS COMPRISING HYALURONIC ACID-METHOTREXATE CONJUGATE AND A METHOD FOR PREPARATION THEREOF

机译:用于预防或治疗含有透明质酸-甲氨蝶呤共轭物的关节炎的药物组合物及其制备方法

摘要

A purpose of the present invention relates to a pharmaceutical composition including a compound represented by chemical formula 1 as an active ingredient for preventing or treating arthritis, a method for producing a compound of chemical formula 1 comprising a step of reacting methotrexate with hyaluronic acid under the presence of 4-dimethylaminopyridine and N,N;-dicyclohexylcarbodiimide, and a hyaluronic acid-methotrexate conjugant represented by chemical formula 1. The HA-MTX conjugant of the present invention can discharge MTX when an ester bond is hydrolyzed in an acidic condition, so that a separated enzyme is not needed. Even when the HA-MTX conjugant is systemically administered by means of an intravenous injection, a drug is selectively discharged from an arthritic region which is lower than normal tissues so that side effects are minimized and the HA-MTX conjugant can be effectively used as an arthritis treating agent.
机译:本发明的目的涉及包含化学式1表示的化合物作为预防或治疗关节炎的有效成分的药物组合物,化学式1的化合物的制备方法,该方法包括使甲氨蝶呤在透明质酸下与透明质酸反应的步骤。存在4-二甲基氨基吡啶和N,N;-二环己基碳二亚胺以及化学式1表示的透明质酸-甲氨蝶呤结合剂。当在酸性条件下水解酯键时,本发明的HA-MTX结合剂可以释放MTX。不需要分离的酶。即使通过静脉内注射全身施用HA-MTX偶联剂,也可以从低于正常组织的关节炎区域选择性地释放药物,从而最大程度地减少副作用,并且HA-MTX偶联剂可以有效地用作药物。关节炎治疗剂。

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