1-CYCLOPROPYL-6-FLUORO-7-(8-METHOXYIMINO-2,6-DIAZA-SPIRO[3,4]OCT-6-YL)-4-OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID D-ASPARTATE HYDRATES AND AN ANTIBACTERIAL COMPOSITION COMPRISING THEIR HYDRATES

• Main Authors: KIM, SEUNG HWAN, CHOI, DONG RACK, CHANG, HWAN BONG, BAEK, NAM HYUN, KIM, GUN GOOK, LIM, JAE KYUNG
• Format: Patent
• Language: English; Korean
• Published: 14.09.2015
• Subjects: 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

The present invention relates to 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3,4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid D-aspartate hydrates, and an antibacterial composition comprising the hydrates. The present invention provides stable zabofloxacin D-aspartate hydrates in which adsorption and desorption of water hardly occur, and provides specifically zabofloxacin D-aspartate sesquihydrate (1.5 H_2O). Because the zabofloxacin D-aspartate hydrates according to the present invention hardly absorb moisture, thereby having outstanding physicochemical properties. Therefore, the drugs comprising zabofloxacin D-aspartate hydrate of the present invention do not easily break, especially in its tablet form, and changes little in the content of the main ingredient, thus exhibiting an excellent pharmaceutical stability.