PROBLEM TO BE SOLVED: To provide an oral pharmaceutical composition which releases an active agent in the gastrointestinal tract where the absorption or therapeutic efficacy of the active agent is maximized.SOLUTION: The invention provides a composition containing minicapsules or minispheres which contain an active agent in a liquid form, or a semi-solid form which may be encapsulated with a gelling agent, or a solid form, within a hydrophobic core; wherein the minicapsules or minispheres have a release profile to release the active agent within the colon. The minicapsule consists of one or more layers and releases the active agent by the dissolution and the like in the gastrointestinal tract. The active agent is a hydroxylase inhibitor and is released in the colon.SELECTED DRAWING: None【課題】胃腸管内で活性薬剤を放出し、活性型の薬物を胃腸管での吸収又は治療を最大にする経口医薬組成物の提供。【解決手段】ミニカプセルまたはミニスフェアが、液体、又はゲル化剤を用いてカプセル化されていてよい半固体又は固体で疎水性のコア中に、活性薬剤を含み、ミニカプセルまたはミニスフェアが、結腸内で活性薬剤を放出する放出プロフィールを有する組成物。ミニカプセルが一層以上からなり、胃腸管で溶解等により活性薬剤を放出する組成物。前記活性薬剤がヒドロキシラーゼ阻害剤であり、結腸で放出される組成物。【選択図】なし