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A PROCESS FOR PREPARING ESOMEPRAZOLE MAGNESIUM COMPOSITIONS

IP.com Disclosure Number: IPCOM000205310D
Publication Date: 2011-Mar-25
Document File: 7 page(s) / 88K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure relates to a process for preparing esomeprazole magnesium compositions. The compositions are useful against various gastrointestinal disorders.

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A PROCESS FOR PREPARING ESOMEPRAZOLE MAGNESIUM COMPOSITIONS

Abstract

The present disclosure relates to a process for preparing esomeprazole magnesium compositions.  The compositions are useful against various gastrointestinal disorders.

Benzimidazoles are strong inhibitors of proton pump and thus are widely used as therapeutic agents for stomach ulcer, duodenal ulcer, gastro esophageal reflux disorders by inhibiting gastric acid secretion.

We report a process for preparing esomeprazole magnesium compositions as described below and exemplified.

The process comprises the steps of: a) preparing an esomeprazole magnesium core by dispersing crystalline esomeprazole magnesium, and optionally, one or more pharmaceutically acceptable additives in a non-aqueous solvent or mixtures thereof to obtain a dispersion and spraying the dispersion on pharmaceutically acceptable inert carrier; b) coating the esomeprazole magnesium core with a separating layer; and c) coating the product of step (b) with an enteric coating.  The product of step (c) may be optionally coated with an over-coat to obtain an over-coated core.  The product of step (c) or the over-coated product may be mixed with one or more tablet excipients, and the mixture compressed into tablets.

The composition described above may be prepared using amorphous esomeprazole magnesium and does not show substantial change in XRD pattern of the esomeprazole magnesium during the shelf life of the composition.

The term “esomeprazole magnesium”, as used herein, refers to esomeprazole magnesium or salts thereof, and includes anhydrates, monohydrates, dihydrates, sesquihydrates, trihydrates, alcoholates, such as, methanolates and ethanolates, and polymorphs thereof.  Preferably, esomeprazole magnesium is in the crystalline form.  For example, esomeprazole magnesium may be in the form of crystalline esomeprazole magnesium magnesium dihydrate.

The esomeprazole magnesium core may be obtained in the form of granules, pellets, beads or minitablets, which may be further processed to obtain esomeprazole magnesium composition in suitable dosage form.  For eg., the esomeprazole magnesium core may be coated with a separating layer, an enteric coating and an over coating layer to obtain over coated core.  The over coated core may be filled into capsules or compressed into tablets.

The term “composition” refers to any oral dosage form such as tablet or capsule, comprising the esomeprazole magnesium core.  The tablet may be in the form of multiple unit tablet.

The composition obtained by the process taught in the various embodiments result in a composition that is stable in terms of the polymorphic forms during the shelf life of the composition.  The compositions do not show substantial change in XRD pattern of the esomeprazole magnesium during the shelf life of the composition.

The non-aqueous solvents may be selected from methanol, ethanol, isopropanol, acetone, dichloromethane, and mixtures thereof.

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