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GALENIC COMPOSITION COMPRISING ATORVASTATIN

IP.com Disclosure Number: IPCOM000223718D
Publication Date: 2012-Nov-26
Document File: 8 page(s) / 84K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure provides a galenic composition comprising atorvastatin or pharmaceutically acceptable salts thereof, the composition exhibiting a relative bioavailability measured by an area under the curve (AUC) of more than 130%.

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GALENIC COMPOSITION COMPRISING ATORVASTATIN

Abstract

The present disclosure provides a galenic composition comprising atorvastatin or pharmaceutically acceptable salts thereof, the composition exhibiting a relative bioavailability measured by an area under the curve (AUC) of more than 130%.

Reported herein is a galenic composition comprising atorvastatin or pharmaceutically acceptable salts thereof, wherein the composition exhibits a relative bioavailability measured by an area under the curve (AUC) of more than 130%.

Also reported herein is a galenic composition comprising atorvastatin or pharmaceutically acceptable salts thereof, wherein the composition exhibits a relative bioavailability measured by an AUC of more than 130% and comprises an alkali metal salt in an amount of more than 10% by weight of the composition.

Also reported herein is a galenic composition comprising:

a)   atorvastatin or a pharmaceutically salt thereof; and

b)   an alkali metal salt in an amount 10% to 25% by weight of the composition;

wherein the composition exhibits a relative bioavailability measured by an AUC of more than 130%.

Atorvastatin may be present in the form of atorvastatin or pharmaceutically acceptable salts thereof such as calcium, magnesium, potassium, etc.  Atorvastatin may exist in any of the solid state forms available such as amorphous or any other polymorphic form.

Atorvastatin may be present alone or in combination with another active ingredient such as amlodipine, ezetimibe, niacin, ramipril, aspirin, and other cardiovascular agents.

Alkali metal salt additives include sodium carbonate, sodium bicarbonate, sodium hydroxide, sodium silicate, disodium hydrogen orthophosphate, sodium dihydrogen phosphate, disodium hydrogen phosphate, sodium phosphate, and sodium aluminate.  The amount of alkali metal salts is more than 10% based on the total weight of the composition, in particular 10% to 25% by weight of the composition.  The pharmaceutical composition may further comprise additional alkanizing agents such as meglumine, tris(hydroxymethyl)aminomethane (tris).  The composition may include a combination of two or more alkali metals salts or a combination of alkali metal salt with another alkanizing agent.

The composition may further comprise an additional stabilizer.  The additional stabilizer may include antioxidants.

Examples of antioxidants include butylated hydroxy anisole, butylated hydroxy toluene, DL-alpha-tocopherol, ascorbic acid, sodium ascorbate, fumaric acid, or mixtures thereof.

The term “galenic” composition indicates a composition which is optimized for enhanced absorption.The term “composition”, as used herein, includes solid dosage forms such as tablets, capsules, pills, granules, and pellets. Tablets may be present in the form of monolayer tablets or multilayer tablets.

The composition may further include other pharmaceutically acceptable excipients such as disintegrants, binders, diluents, and lubricants/glida...