NOVEL COCRYSTAL OF EMPAGLIFLOZIN

• Main Author: AN, Ji Hun
• Format: Patent
• Language: English; French; Korean
• Published: 08.07.2021
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

As a result of efforts to improve the problems of empagliflozin, that is, low stability and water solubility, an empagliflozin cocrystal having at least 120-fold increase in stability and water solubility was developed. The empagliflozin cocrystal according to the present invention is in a novel solid form that overcomes the stability and water solubility of known crystalline forms of empagliflozin, and is very useful as an optimal active pharmaceutical ingredient that can be maximally utilized as a drug. L'objectif de la présente invention est de résoudre des problèmes se rapportant à l'empagliflozine, notamment une faible stabilité et une faible hydrosolubilité. La présente invention porte sur le développement d'un co-cristal d'empagliflozine ayant au moins 120 fois plus de stabilité et d'hydrosolubilité. Le co-cristal d'empagliflozine selon la présente invention est sous une nouvelle forme solide qui surmonte la stabilité et l'hydrosolubilité des formes cristallines connues d'empagliflozine, et est très utile en tant qu'ingrédient pharmaceutique actif optimal qui peut être utilisé au maximum en tant que médicament. 엠파글리플로진의 문제점인 낮은 안정성 및 수용해도를 개선하기 위해 노력한 결과 안정성 및 수용해도가 120배 이상 증가 된 엠파글리플로진 공결정을 개발하였다. 본 발명에 따른 엠파글리플로진 공결정은 공지된 엠파글리플로진 결정형의 안정성 및 수용해도가 극복된 새로운 고체형태로서 약물로서의 활용을 극대화할 수 있는 최적의 원료의약물질로 매우 유용하다.