首页> 外国专利> 1-CYCLOPROPYL-6-FLUORO-7-(8-METHOXYIMINO-2,6-DIAZA-SPIRO3,4OCT-6-YL)-4-OXO-1,4-DIHYDRO-1,8NAPHTHYRIDINE-3-CARBOXYLIC ACID D-ASPARTATE HYDRATES AND AN ANTIBACTERIAL COMPOSITION COMPRISING THEIR HYDRATES

1-CYCLOPROPYL-6-FLUORO-7-(8-METHOXYIMINO-2,6-DIAZA-SPIRO3,4OCT-6-YL)-4-OXO-1,4-DIHYDRO-1,8NAPHTHYRIDINE-3-CARBOXYLIC ACID D-ASPARTATE HYDRATES AND AN ANTIBACTERIAL COMPOSITION COMPRISING THEIR HYDRATES

机译:1-环丙基-6-氟-7-(8-甲氧亚氨基-2,6-二氮杂螺[3,4] OCT-6-YL)-4-氧-1-,4-二氢-[1,8]萘啶-3-羧酸D-天冬氨酸水合物及其构成的抗微生物组合物

摘要

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.
机译:本发明涉及1-环丙基-6-氟-7-(8-甲氧基亚氨基-2,6-二氮杂-螺[3,4]辛-6-基)-4-氧代-1,4-二氢-[ 1,8]萘啶-3-羧酸D-天冬氨酸水合物,以及包含该水合物的抗菌组合物。本发明提供了稳定的唑泊沙星D-天冬氨酸水合物,其中几乎不发生水的吸附和解吸,并且具体地提供了唑泊沙星D-天冬氨酸倍半水合物(1.5 H_2O)。因为根据本发明的唑泊沙星D-天冬氨酸水合物几乎不吸收水分,因此具有优异的理化性质。因此,包含本发明的沙伯沙星D-天冬氨酸水合物的药物不易破裂,尤其是其片剂形式,并且主要成分的含量变化很小,因此表现出优异的药物稳定性。

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