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AMORPHOUS ROXITHROMYCIN COMPOSITION
专利权人:
发明人:
申请号:
EP11722543.3
公开号:
EP2563373A1
申请日:
2011.04.14
申请国别(地区):
EP
年份:
2013
代理人:
摘要:
This invention relates to a macrolide composition, more particularly an amorphous form (Form-III) of 3R, 4S, 5S, 6R, 7R, 9R, 11S, 12R, 13S, 14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one or roxithromycin characterized by the absence of peaks in the infra-red spectrum of amorphous (Form-I11) of roxithromycin at 3577.15 3526.03 3465.27 and 3276.24 cm-1 relative to the infra-red spectrum of the prior art roxithromycin raw material displaying peaks at 3577.15 3526.03 3465.27 and 3276.24 cm-1 and further characterized by an increased solubility of at least 50% over prior art anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5), phosphate buffer (pH 6.8) and water.
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