Stable pharmaceutical formulation comprising HMC-CoA reductase inhibitor

Abstract

Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, 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, and some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The aforementioned active substances may be destabilised by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions. The present invention relates to a stable solid pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia. More precisely, the present invention relates to the new stable solid pharmaceutical formulation containing as an active ingredient a HMG-CoA reductase inhibitor, such as atorvastatin, pravastatin, fluvastatin and cerivastatin or pharmaceutically acceptable salts thereof.

Description

field of invention [0001] The invention relates to a new stable solid medicine formula, which is especially suitable for treating hypercholesterolemia and hyperlipidemia. In particular, the present invention relates to a novel stable solid pharmaceutical formulation containing active substances HMG-CoA reductase inhibitors such as atorvastatin, pravastatin, fluvastatin and cervastatin, or pharmaceutically active salts. Background of the invention [0002] Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, fluvastatin and cervastatin and their derivatives and analogs are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. They are mainly produced by fermentation with microorganisms belonging to different species of Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium. Some are chemically synthesized by processing fermentation products, such as simvastatin, or some are entirely chemically synthesized, such as flu...

AI Technical Summary

Problems solved by technology

However, the local alkaline environment that occurs at the dissolution site of the drug formulation has certain side effects on the gastric mucosa, which should normally have an acidic environment

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