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Positively charged water-soluble prodrugs of acetaminophen and related compounds with very fast skin permeability

机译：对乙酰氨基酚及相关化合物的带正电荷的水溶性前药，具有极快的皮肤渗透性

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摘要

PROBLEM TO BE SOLVED: To overcome side-effects related to the use of acetaminophen and related compounds thereof.SOLUTION: The new positive charge prodrugs of acetaminophen represented by formula (1), acetaminosalol and related compounds are designed and synthesized. The amino group positively charged to the prodrugs not only remarkably increase the dissolubility of medicines but also is coupled with the negative charge on the phosphate head group of a film and puts the prodrugs into a cytoplasm sol. The prodrugs diffuse through the skin of men faster by 150 times than the acetaminophen, acetaminosalol and related compounds. The prodrugs are used for treatment in an NSAIA treatable state in the men or animals, are pharmaceutically used not only in oral administration but also in transdermal administration for every kinds of medicine treatments, and can evade most side-effects of NSAIA.

机译：解决的问题：为了克服与对乙酰氨基酚及其相关化合物的使用有关的副作用。解决方案：设计并合成由式（1）表示的对乙酰氨基酚的新正电荷前药，对乙酰氨基酚和相关化合物。带正电荷带入前药的氨基不仅显着提高了药物的溶解性，而且还与薄膜的磷酸根基上的负电荷结合，使前药进入了细胞质溶胶。前药在人体皮肤中的扩散速度比对乙酰氨基酚，对乙酰氨基酚和相关化合物快150倍。该前药用于在人或动物中以NSAIA可治疗的状态进行治疗，不仅在口服给药中还用于各种药物治疗的药物经皮给药，并且可以规避NSAIA的大多数副作用。

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公开/公告号JP6165816B2

专利类型
公开/公告日2017-07-19

原文格式PDF
申请/专利权人テックフィールズバイオケムカンパニーリミテッド;ユーチョンシー;
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申请/专利号JP20150196022
发明设计人ユーチョンシー;シューリナ;
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申请日2015-10-01
分类号C07C233/25;C07C231/12;A61K31/235;A61P1/02;A61P25/04;A61P29/00;A61P35/00;A61P15/00;A61P1/08;A61P25/00;A61P25/06;A61P19/02;A61P19/08;A61P17/00;A61P21/00;A61P17/06;A61P17/10;A61P27/06;A61P27/02;A61P27/16;A61P1/18;A61P1/04;
国家 JP
入库时间 2022-08-21 13:56:40

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