METHOD OF PREPARING AMORPHOUS TENELIGLIPTIN 2.5 HYDROBROMIDE

To provide a method of preparing amorphous teneligliptin 2.5 hydrobromide, and a method of preparing crystal form A and crystal form C of teneligliptin 2.0 hydrobromide.SOLUTION: The amorphous teneligliptin 2.5 hydrobromide is prepared by dissolving teneligliptin 2.0 hydrobromide in a polar solvent...

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Hauptverfasser:	SURESH BABU JAYACHANDRA, RAMAKOTESWARARAO JETTI, BOMMAREDDY AGGI RAMIREDDY
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	To provide a method of preparing amorphous teneligliptin 2.5 hydrobromide, and a method of preparing crystal form A and crystal form C of teneligliptin 2.0 hydrobromide.SOLUTION: The amorphous teneligliptin 2.5 hydrobromide is prepared by dissolving teneligliptin 2.0 hydrobromide in a polar solvent such as an alcohol solvent or water, adding an aqueous hydrobromic acid solution, and filtering and then spray-drying the mixture. The crystal forms A and C are prepared by dissolving teneligliptin in a mixed solvent of alcohol and water, adding an aqueous hydrobromic acid solution, then seeding respective seed crystals, and adding a poor solvent.SELECTED DRAWING: None 【課題】テネリグリプチン２．５臭化水素酸塩のアモルファスの調製方法、並びにテネリグリプチン２．０臭化水素酸塩の結晶形Ａ及び結晶形Ｃを調製する方法を提供する。【解決手段】アモルファスは、テネリグリプチン２．０臭化水素酸塩をアルコール溶剤、水などの極性溶媒に溶解し、臭化水素酸水溶液を添加、濾過後噴霧乾燥する。結晶形Ａ、Ｃについてはアルコールと水の混合溶媒にテネグリプチンを溶解し、臭化水素酸水溶液を添加後、それぞれの種結晶を播種し、貧溶媒を添加する。【選択図】なし