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US 7,078,558 B1Granted
Crystals of the sodium salt of pravastatin
AssigneeLek Pharmaceutical & Chemical Co. d.d.
InventorZlatko Pflaum
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AssigneeLek Pharmaceutical & Chemical Co. d.d.
InventorZlatko Pflaum
Estimating the term…
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 an Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor, or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis (simvastatin) or they are the products of total chemical synthesis (fluvastatin, atorvastatin and cervastatin). The present invention relates to a crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1-naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-β,δ,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance. The present invention further relates to the method for its preparation and isolation, to a pharmaceutical formulation containing the sodium salt of pravastatin in the crystalline form and a pharmaceutically acceptable carrier, and to a pharmaceutical method of treatment. The novel crystalline form of the sodium salt of pravastatin is useful in the treatment of hypercholesterolemia and hyperlipidemia.
The sodium salt of pravastatin in a crystalline form wherein the crystals in the X-ray diffraction measurement produce distinct peaks having a half-value width below 2° measured at the reflection angle 2θ using CuKα radiation.
A process for preparing pharmaceutical products for the treatment of hypercholesterolemia and hyperlipidemia comprising the step of adding the active agent pravastatin as a crystalline sodium salt together with a pharmaceutically acceptable carrier;
A process for the preparation of the sodium salt of pravastatin in crystalline form, comprising the steps of:
The sodium salt of pravastatin in crystalline form having an X-ray diffraction pattern comprising characteristic peaks at 4.0±0.2;
The sodium salt of pravastatin in a crystalline form having an X-ray diffraction pattern comprising characteristic peaks at 4.0±0.2;
The sodium salt of pravastatin in a crystalline form having an X-ray diffraction pattern comprising characteristic peaks at 4.0±0.2;
The crystalline form of the sodium salt of pravastatin having an X-ray diffraction pattern comprising characteristic peaks at 4.0±0.2;
Dependencies are inferred from the claim text.