Abstract: 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.

Abstract: 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.

Abstract: 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-methoxyethoxymethoxy-imino)-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-III) 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.

Abstract: 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)-?-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-?-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.

Abstract: The invention relates to an amorphous non-crystalline glass form (Form-ll) 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-ll) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.