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Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods

a technology of carvedilol and free base, which is applied in the direction of biocide, drug composition, cardiovascular disorder, etc., can solve the problems of limiting the residence time of the intestine, causing the intestine to be a considerable problem, and affecting the intestine or inability to maintain the chemical stability

Inactive Publication Date: 2005-08-11
FLAMEL TECHNOLOGIES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This often results in marginal or unacceptable chemical stability upon storage.
Consequently, the short residence time in the small intestine poses a considerable problem to those skilled in the art interested in developing sustained-absorption medicinal products intended for oral administration.
The medicinal product administered orally is, in effect, subject to the natural transit of the gastrointestinal tract, thereby limiting its residence time.

Method used

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  • Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods
  • Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods
  • Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods

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embodiments

[0436] In light of the foregoing discussion, the present invention relates to and is exemplified by, but not limited to the following embodiments present below, which include corresponding pharmaceutical compositions, different controlled release formulations, respectively comprised or formed from the following components, such as carvedilol free base, carvedilol salts, anhydrous forms or solvates thereof, and which also may include, but are not limited to the various components (i.e., such as conventionally known, adjuvants, carriers, diluents, excipients, agents, plasticizers, polymers, etc. as described herein) which may be in or formed into different dosage forms (i.e., which may include, but are not limited to, tablets, capsules and the like) as described herein.

[0437] In a general or first embodiment, the present invention relates to a controlled release formulation, which comprises: [0438] a solubility enhanced carvedilol free base or a carvedilol salt, solvate or anhydrous ...

example 1

Form I Carvedilol Dihydrogen Phosphate Hemihydrate Preparation

[0627] A suitable reactor is charged with acetone. The acetone solution is sequentially charged with carvedilol and water. Upon addition of the water, the slurry dissolves quickly. To the solution is added aqueous H3PO4. The reaction mixture is stirred at room temperature and carvedilol dihydrogen phosphate seeds are added in one portion. The solid precipitate formed is stirred, then filtered and the collected cake is washed with aqueous acetone. The cake is dried under vacuum to a constant weight. The cake is weighed and stored in a polyethylene container.

example 2

Form II Carvedilol Dihydrogen Phosphate Dihydrate Preparation

[0628] Form I is slurried in acetone / water mixture between 10 and 30° C. for several days.

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Abstract

The present invention also relates to carvedilol free base, carvedilol salts, anhydrous forms, or solvates thereof, corresponding pharmaceutical compositions or controlled release formulations, and delivery or dosing methods of carvedilol forms to the lower gastrointestingal tract or methods to treat cardiovascular diseases, which may include, but are not limited to hypertension, congestive heart failure, atherosclerosis, and angina. The present invention relates to controlled release formulations, which comprise various carvedilol forms, which may include, but are not limited to a carvedilol free base or corresponding carvedilol salts, anhydrous forms or solvates thereof.

Description

FIELD OF THE INVENTION [0001] The present invention relates to carvedilol free base, carvedilol salts, anhydrous forms, or solvates thereof, corresponding pharmaceutical compositions or controlled release formulations, delivery methods of carvedilol forms to the gastrointestingal tract or methods to treat cardiovascular diseases, which may include, but are not limited to hypertension, congestive heart failure, atherosclerosis, and angina. [0002] The present invention relates to controlled release formulations, which comprise various cavedilol forms, which may include, but are not limited to carvedilol free base and corresponding carvedilol salts, anhydrous forms or solvates thereof. BACKGROUND OF THE INVENTION Carvedilol [0003] The compound, 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]-amino]-2-propanol is known as Carvedilol. Carvedilol is depicted by the following chemical structure: [0004] Carvedilol is disclosed in U.S. Pat. No. 4,503,067 to Wiedemann et al. (i.e., assig...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61KA61K9/16A61K9/22A61K9/50A61K31/403
CPCA61K9/1635A61K9/1641A61K31/403A61K9/2077A61K9/1658A61P9/04A61P9/10A61P9/12
Inventor CASTAN, CATHERINECROWLEY, PATRICK J.GUIMBERTEAU, FLORENCEMEYRUEIX, REMIOH, CHOOH K.SOULA, GERARD
Owner FLAMEL TECHNOLOGIES
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