PHARMACEUTICAL COMPOSITION AND METHOD FOR PRODUCING THE SAME

• Main Authors: ZHANG XIAO, WANG ZE REN, SUN MEI LI, JO TAKASHI, JIANG GUI SHENG, WANG LI JIANG, ZHAO YU LAN, CHEN SHUNGIN
• Format: Patent
• Language: English; Japanese
• Published: 26.12.2019
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide pharmaceutical compositions for oral administration comprising a pharmaceutically acceptable surface-modified acidic pharmaceutical adjuvant, and dabigatran etexilate or a pharmaceutically acceptable salt or hydrate thereof, to provide use thereof, and furthermore to provide methods for modifying the surface of a medicinal adjuvant.SOLUTION: Provided is a pharmaceutical composition for oral administration containing an acidic medicinal adjuvant and a surface-modified acidic medicinal adjuvant having a neutral salt layer on the surface of the acidic medicinal adjuvant, and dabigatran etexilate, the acidic medicinal adjuvant being tartaric acid, fumaric acid, succinic acid, citric acid, lactic acid or malic acid powder particles, the neutral salt layer containing an anion of the acidic medicinal adjuvant and a cation of a modifying alkaline substance, and the modifying alkaline substance being a hydrogen oxide salt, a water-soluble alkaline carbonate salt, or a water-soluble phosphoric acid alkaline salt.SELECTED DRAWING: Figure 1 【課題】本発明は、薬学的に許容される表面改質された酸性薬用補助剤と、ダビガトランエテキシラート又はその薬学的に許容される塩又は水和物とを含有する、経口投与用の医薬組成物及びその用途を提供する。更に、本発明は薬用補助剤表面改質方法を提供する。【解決手段】酸性薬用補助剤及び該酸性薬用補助剤の表面に中性塩層を有し表面改質された酸性薬用補助剤と、ダビガトランエテキシラートとを含有し、酸性薬用補助剤は、酒石酸、フマル酸、コハク酸、クエン酸、乳酸又はリンゴ酸の粉末粒子であり、中性塩層は、前記酸性薬用補助剤のアニオン及び改質用アルカリ性物質のカチオンを含み、前記改質用アルカリ性物質は、水素酸化物の塩、水溶性の炭酸のアルカリ性塩、又は水溶性のリン酸のアルカリ性塩である、経口投与用の医薬組成物。【選択図】図１