Composition comprising an amorphous non-crystalline glass form of azithromycin

The invention relates to an amorphous non-crystalline glass form (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-11-{[3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl2,6-dideoxy-3-C-methyl-3-O-methyl-alp...

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Bibliographic Details
Main Authors AUCAMP MARIQUE, LIEBENBERG WILNA, ODENDAAL ROELF WILLEM
Format Patent
LanguageChinese
English
Published 03.10.2012
Subjects
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Summary:The invention relates to an amorphous non-crystalline glass form (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-11-{[3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranoside or azithromycin having an infra-red pattern displaying characteristic relatively broad peaks at approximately 3500 and 1727 cm-1 and characteristic peaks at approximately 2970 and 2938 cm-1. The invention further relates to a preparation method of increasing the solubility of azithromycin including the steps of selecting anhydrous, monohydrated or dihydrated azithromycin; elevating the temperature of the azithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-ll) of azithromycin having relatively increased solubility without decreasing the structural stability thereof.
Bibliography:Application Number: CN201080061715