Carvedilol dihydrogen phosphate monohydrate
AssigneeWanbury Limited
InventorsShankar Sanganabhatla, Sunanda Manoj, Ramanarasimha Moorthy Koduru
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Abstract
Disclosed herein is crystalline carvedilol dihydrogen phosphate monohydrate having high aqueous solubility and the process for preparation thereof. The invention further discloses methods for treating hypertension, congestive heart failure and angina in a mammal, using pharmaceutical compositions comprising the compound of invention.
Claims23
Crystalline carvedilol dihydrogen phosphate monohydrate.
A process for preparation of carvedilol dihydrogen phosphate monohydrate in high yield comprising the steps of:
- e. preparing a slurry of carvedilol in water;
- f. contacting the slurried carvedilol with a composition comprising a source of phosphate at a temperature from about 25 to about 55° C., thereby generating a phosphate salt of carvedilol in water;
- g. adding a water-miscible organic solvent to the aqueous carvedilol phosphate salt at a temperature from about 25 to about 55° C.;
- and
- h. cooling the aqueous-organic mixture and isolating solid carvedilol dihydrogen phosphate monohydrate salt from the mixture.
A pharmaceutical composition comprising carvedilol dihydrogen phosphate monohydrate and a pharmaceutical carrier.
Use of crystalline carvedilol dihydrogen phosphate monohydrate for the preparation of a medicament useful for treating a subject suffering from, or at risk of developing, hypertension, congestive heart failure or angina.
A method for treating a cardiovascular disease in a mammal, wherein the method comprises administering to the mammal a therapeutically effective amount of a pharmaceutical composition comprising carvedilol dihydrogen phosphate monohydrate.
Dependencies are inferred from the claim text.