Crystals of the sodium salt of pravastatin

C - Chemistry – Metallurgy – 07 – C

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C07C 69/33 (2006.01) A61K 31/22 (2006.01) C07C 67/52 (2006.01)

Patent

CA 2379335

Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, fluvastatin and cervastatin and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products. The present invention relates to a novel crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1- naphthaleneheptanoid acid, 1, 2, 6, 7, 8, 8a-hexahydro-.beta., .delta., 6- trihydroxy-2-methyl-8 (2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance, to the method for its production and isolation, to a pharmaceutical formulation containing the crystalline form of the sodium salt of pravastatin and a pharmaceutical method of treatment. The novel crystalline form of the sodium salt of pravastatin is useful in the treatment of hypercholesterolemia and hyperlipidemia.

Lovastatine, pravastatine, simvastatine, mévastatine, atorvastatine, fluvastatine, cervastatine et les dérivés et analogues de ceux-ci sont connus sous le nom d'HMG-CoA réductase inhibiteurs et sont utilisés comme agents antihypercholesterolémiques. La majorité d'entre eux sont produits par fermentation, à l'aide de micro-organismes de différentes espèces, identifiées comme espèces appartenant au genre Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor ou Penicillium. Certains de ces produits sont obtenus, en traitant les produits fermentation, par les procédés de synthèse chimique ou ce sont eux-mêmes les produits. La présente invention concerne une nouvelle forme cristalline de sel de sodium de pravastatine, connue sous le nom chimique : 1- acide naphthalénéhéptanoïde, 1, 2, 6, 7, 8, 8a-hexahydro-.beta., .delta., 6-trihydroxy-2-méthyl-8 (2-méthyl-1-oxobutoxy)-, mono sel de sodium, qui sert comme substance pharmaceutique, au procédé pour sa production et son isolation, à une formulation pharmaceutique contenant la forme cristalline de sel de sodium de pravastatine et à un procédé pharmaceutique de traitement. La nouvelle forme cristalline de sel de sodium de pravastatine sert à traiter l'hypercholestérolemie et l'hyperlipidémie.

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