Amorphous hydrous esomeprazole magnesium
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.
Claims11
A hydrous compound of the formula
- 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 having a moisture content of 2 percent to 10 percent as measured by the Karl Fischer method and being in the form of an amorphous solid.
A compound which is a hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium, said compound being in the form of an amorphous solid, having substantially the same X-ray powder diffraction pattern as shown in FIG. 1.
A solid composition which comprises hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium as a solid, wherein at least 80% by weight of the solid (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium has a moisture content of 2 percent to 10 percent as measured by the Karl Fischer method and is in an amorphous form, wherein the (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium has substantially the same X-ray powder diffraction pattern as shown in FIG. 1.
Hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium in the form of an amorphous solid, made by a process comprising:
- a) providing (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium in an alcohol-containing solvent;
- b) contacting said (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium in an alcohol-containing solvent with water so that a solid mass separates;
- and
- c) isolating said separated solid mass, which is a hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium in the form of an amorphous solid;
- wherein the hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium has substantially the same X-ray powder diffraction pattern as shown in FIG. 1.
A solid pharmaceutical composition comprising a hydrous (S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole magnesium in the form of an amorphous solid, wherein the esomeprazole magnesium has substantially the same X-ray powder diffraction pattern as shown in FIG. 1, and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.