Amorphous hydrates of esomeprazole magnesium and process for the preparation thereof
AssigneeDr. Reddy's Laboratories, Inc.
InventorsManne Satyanarayana Reddy, Muppa Kishore Kumar, Koilkonda Purandhar, Keshaboina Sreenath
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Abstract
A hydrate of esomeprazole magnesium in the form of an amorphous solid is provided. Methods of preparation and use of, as well as formulation containing the hydrate of esomeprazole magnesium in the form of an amorphous solid are also provided.
Claims46
A compound of the formula
- 3
- wherein one of R1 and R2 is hydrogen and the other is methoxy;
- A is an alkaline earth or alkali metal;
- and m and n are 1 or 2;
- said compound being a hydrate and being in the form of an amorphous solid.
A compound which is a hydrate of esomeprazole magnesium, said compound being in the form of an amorphous solid.
The compound of claim 5, having substantially the same x-ray powder diffraction pattern shown in FIG. 1.
A composition which comprises esomeprazole magnesium as a solid, wherein at least 80% by weight of the solid esomeprazole magnesium is a hydrate of esomeprazole magnesium in the form of an amorphous solid.
A process for making a hydrate of esomeprazole magnesium in the form of an amorphous solid, said process comprising:
- a) providing esomeprazole magnesium in an alcohol-containing solvent;
- b) contacting said esomeprazole magnesium and said alcohol-containing solvent with water so that a solid mass separates;
- and
- c) isolating said separated solid mass, which is the hydrate of esomeprazole magnesium in the form of an amorphous solid.
A process for making a hydrate of esomeprazole magnesium in the form of an amorphous solid, said process comprising:
- a) providing esomeprazole magnesium in methanol;
- b) contacting said esomeprazole magnesium in methanol with water so that a solid mass separates;
- c) isolating said solid mass by filtration;
- d) washing said solid mass;
- e) dissolving said solid mass in methanol and filtering the solution so formed to separate excess magnesium solids;
- f) removing solvent from the solution to obtain isolated residual mass;
- g) re-precipitating said isolated residual mass from ethyl acetate, and
- h) drying said isolated residual mass, which is the hydrate of esomeprazole magnesium in the form of an amorphous solid.
A pharmaceutical composition comprising the compound of Formula 1 in the form of an amorphous solid and a pharmaceutically acceptable carrier.
A pharmaceutical composition comprising a hydrate of esomeprazole magnesium in the form of an amorphous solid, and a pharmaceutically acceptable carrier.
A method for reducing gastric acid secretion in a subject which comprises administering to the subject an amount of the compound of Formula 1 in the form of an amorphous solid effective to reduce gastric acid secretion by said subject.
A method for reducing gastric acid secretion in a subject which comprises administering to the subject an amount of a hydrate of esomeprazole magnesium in the form of an amorphous solid effective to reduce gastric acid secretion by said subject.
Dependencies are inferred from the claim text.