Roelf Willem Odendaal,Wilna Liebenberg,Marique Aucamp
申请号：
US13516942
公开号：
US20130059805A1
申请日:
2010.12.15
申请国别(地区):
US
年份:
2013
代理人:
摘要：
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)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-α-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-II) of azithromycin having relatively increased solubility without decreasing the structural stability thereof.
