Amorphous roxithromycin composition

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- dimethylo...

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Bibliographic Details
Main Authors AUCAMP MARIQUE, LIEBENBERG WILNA
Format Patent
LanguageChinese
English
Published 23.01.2013
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
SUGARS
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Summary: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 characterised by the absence of peaks in the infra-red spectrum of amorphous (Form-Ill) 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 characterised 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.
Bibliography:Application Number: CN201180024588