NOVEL RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF, IMPROVED METHOD FOR PURIFICATION OF SAID RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THESE

Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The...

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Hauptverfasser: KARUP, GUNNAR LEO, PEDERSEN, SOREN BOLS
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PEDERSEN, SOREN BOLS
description Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed . The raloxifene acid addition salts and/or solvates thereof are useful for th e preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation. A new method for preparation of raloxifene lactate is also disclosed.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title NOVEL RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF, IMPROVED METHOD FOR PURIFICATION OF SAID RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THESE
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