PROBLEM TO BE SOLVED: To provide a prodrug of a bile acid exhibiting performances inherent in a bile acid such as ursodeoxycholic acid or the like, particularly a prodrug of a bile acid which can be converted into a prodrug in an aqueous solution form to be used as a subcutaneously or intravascularly administerable medicine by injection or drip infusion, and its production method.SOLUTION: The prodrug comprises as an effective ingredient an N-acetylcysteine-conjugated bile acid such as N-acetylcysteine-conjugated ursodeoxycholic acid and the like. The production method thereof is also provided.COPYRIGHT: (C)2009,JPO&INPIT【課題】ウルソデオキシコール酸等の胆汁酸が本来有する効能をもたらす胆汁酸のプロドラッグであって、特に水溶液状のプロドラッグとすることにより、注射や点滴による皮下及び血管内投与薬として使用可能な胆汁酸のプロドラッグ及びその製造方法を提供すること。【解決手段】N‐アセチルシステイン抱合型ウルソデオキシコール酸等のN‐アセチルシステイン抱合型胆汁酸を有効成分として含むプロドラッグ及びその製造方法とする。【選択図】図1