COMPOSITION COMPRISING AN AMORPHOUS NON-CRYSTALLINE GLASS FORM OF AZITHROMYCIN

The invention relates to an amorphous non-crystalline glass form (Form-II) 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)...

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Bibliographic Details
Main Authors AUCAMP MARIQUE, LIEBENBERG WILNA, ODENDAAL ROELF WILLEM
Format Patent
LanguageEnglish
Korean
Published 04.10.2012
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:The invention relates to an amorphous non-crystalline glass form (Form-II) 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-oxa-cyclotetradecan-2-one or roxithromycin having at least one characteristic infra-red spectrum peak at approximately 3580 to 3464 cm−1. The invention further relates to a preparation method of increasing the solubility of roxithromycin including the steps of selecting anhydrous roxithromycin or monohydrated roxithromycin; elevating the temperature of the roxithromycin 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-II) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.
Bibliography:Application Number: KR20127018143