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Crystals of the sodium salt of pravastatin

a sodium salt and sodium salt technology, applied in the field of crystallized form of the sodium salt of pravastatin, can solve the problems of not being economical in large-scale production operations for lyophilisation, and achieve the effect of improving purity and stability

Inactive Publication Date: 2006-08-17
LEK PHARMACEUTICAL & CHEMICAL CO D D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011] It is an object of the present invention to provide the sodium salt of pravastatin which is improved in purity and stability compared to the salts described in the prior art mentioned above.

Problems solved by technology

Apart from the aforementioned, lyophilisation is not very economical in large-scale production operations.

Method used

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  • Crystals of the sodium salt of pravastatin
  • Crystals of the sodium salt of pravastatin
  • Crystals of the sodium salt of pravastatin

Examples

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example 1

[0052] The sodium salt of pravastatin (1 g) was dissolved in methanol (10 ml) and while stirring ethyl acetate was added. The resulting clear yellow solution was cooled to 8° C. and allowed to stand overnight. Formed radiating clusters of thin, long needle-like crystals were filtered, washed with ethyl acetate (20 ml) and dried. Yield: 0.87 g of pale yellow crystals, melting point 172-174° C.

example 2

[0053] The sodium salt of pravastatin (2 g) was dissolved in methanol (20 ml) and while stirring ethyl acetate (80 ml) was added. The clear, slightly yellow solution was cooled to 8° C. and allowed to stand for 4 hours. Formed radiating clusters of thin, long needle-like crystals were filtered, washed with ethyl acetate (20 ml) and dried. Yield: 1.53 g of colorless crystals, melting point 172-174° C.

example 3

[0054] 20 The sodium salt of pravastatin (2 g) was dissolved in methanol (20 ml) and while stirring ethyl acetate (150 ml) was added. The resulting clear, slightly yellow solution was cooled to 8° C. and allowed to stand for 4 hours. Formed radiating clusters of thin, long needle-like crystals were filtered, washed with ethyl acetate (20 ml) and dried. Yield: 1.66 g of colorless crystals, melting point 172-174° C.

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Abstract

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 (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.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a divisional of U.S. patent application Ser. No. 10 / 408,012 which was filed with the U.S. Patent and Trademark Office on Apr. 4, 2003 which is a National Stage Entry of PCT / IB00 / 01103 dated Aug. 4, 2000. Priority is claimed for this invention and application, corresponding applications having been filed in Slovenia on Aug. 6, 1999, No. P-9900191 and is a parent of application Ser. No. 10 / 049,093 filed Apr. 22, 2002, now U.S. Pat. No. 6,740,775.BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] 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 co...

Claims

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Application Information

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IPC IPC(8): C07C59/147A61P3/06A61K31/22A61P7/00B01D9/02C07C13/00C07C67/52C07C69/33C07C69/732
CPCC07C69/33C07C2102/28C07C2602/28A61P3/00A61P3/06A61P7/00C07C69/732
Inventor PFLAUM, ZLATKO
Owner LEK PHARMACEUTICAL & CHEMICAL CO D D
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