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Stable pharmaceutical formulation comprising a hmg-coa reductase inhibitor

a technology of coa reductase inhibitor and stable pharmaceutical formulation, which is applied in the direction of drug composition, cardiovascular disorder, metabolic disorder, etc., can solve the problems of unstable active substance stability in acidic environment, negative impact on gastric mucosa with normal acidic environment, and variety of side effects

Inactive Publication Date: 2009-10-22
LEK PHARMA D D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012]According to the present invention, there is further provided a method for the stabilization of a HMG-CoA reductase inhibitor as an active substance in a solid pharmaceutical formulation

Problems solved by technology

Accumulation of impurities from drugs of a lower level of purity may cause a variety of side effects during treatment.
Besides impurities, that cannot be completely eliminated in the process of preparation of the active substance, degradation products occurring by subjecting the final pharmaceutical formulation to various environmental factors such as temperature, moisture, low pH and light, may also impose a problem.
The stability of the active substance in an acidic environment is one of

Method used

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  • Stable pharmaceutical formulation comprising a hmg-coa reductase inhibitor
  • Stable pharmaceutical formulation comprising a hmg-coa reductase inhibitor
  • Stable pharmaceutical formulation comprising a hmg-coa reductase inhibitor

Examples

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example 1

[0037]The pharmaceutical formulation with the active ingredient pravastatin sodium in the form of tablets was prepared as follows: the hereinunder listed ingredients were homogenised and the resulting mixture was then compressed into tablets each containing 5, 10, 20 or 40 mg of pravastatin sodium.

[0038]The pH of the aqueous dispersion of this formulation is 8.3.

Ingredients% by weightPravastatin sodium (pH 8.2)5%Lactose37.5%Microcrystalline cellulose38%Sodium citrate10%Magnesium aluminium silicate2%Polyacrylin potassium3%Talc3%Silicon dioxide0.5%Magnesium stearate1%

example 2

[0039]The pharmaceutical formulation with the active ingredient pravastatin sodium in the form of tablets was prepared as follows: the hereinunder listed ingredients were homogenised and the resulting mixture was then compressed into tablets each containing 5, 10, 20, 40 or 80 mg of pravastatin sodium.

[0040]The pH of the aqueous dispersion of this formulation is 8.0.

Ingredients% by weightPravastatin sodium (pH 8.5)10%Lactose32%Microcrystalline cellulose37%Sodium citrate10%Croscarmellose sodium2%Sodium lauryl sulphate0.5%Polyacrylin potassium3%Talc3%Silicon dioxide0.5%Calcium stearate2%

example 3

[0041]The pharmaceutical formulation with the active ingredient pravastatin sodium in the form of tablets was prepared as follows: the first six hereinunder listed ingredients were homogenised, granulated with water, dried, the remainder of the below listed ingredients were added and homogenised and the resulting mixture was then compressed into tablets each containing 5, 10, 20 or 40 mg of pravastatin sodium.

[0042]The pH of the aqueous dispersion of this formulation is 8.2.

Ingredients% by weightPravastatin sodium (pH 9)5%Lactose20%Microcrystalline cellulose20%Hydroxypropyl cellulose1.5%Sodium citrate10%Magnesium aluminium silicate2%Polyacrylin potassium3%Microcrystalline cellulose35%Talc3%Magnesium stearate0.5%

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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 destabilized 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 THE INVENTION[0001]The present invention relates to a new stable solid pharmaceutical formulation which is particularly suitable for the treatment of hypercholesterolemia and hyperlipidemia. More precisely, the present invention relates to the new stable solid pharmaceutical formulation containing as an active substance a HMG-CoA reductase inhibitor, such as atorvastatin, pravastatin, fluvastatin and cerivastatin, or pharmaceutically active salts thereof.BACKGROUND OF THE INVENTION[0002]Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, fluvastatin and cerivastatin, 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...

Claims

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Application Information

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IPC IPC(8): A61K31/40A61K31/215A61K9/20A61KA61K9/22A61K9/30A61K9/48A61K31/19A61K31/22A61K31/225A61K31/4045A61K31/4418A61K45/00A61P3/06A61P43/00
CPCA61K9/2013A61K9/2009A61P3/06A61P43/00A61P9/00A61P9/12A61K31/192
Inventor KERC, JANEZ
Owner LEK PHARMA D D