- CRYSTALLINE FORM OF PRAVASTATINE AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to a novel form of pravastatin, notably pravastatin sodium, and a method for the preparation of a novel form of pravastatin.
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Page/Page column 8-9
(2012/07/13)
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- Methods for predicting the response to statins
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The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
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- PURIFICATION OF PRAVASTATIN
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The present invention provides a method for the purification of pravastatin or a pharmacologically acceptable salt thereof by treating an aqueous solution comprising pravastatin with a nitrogen-containing base having a pKa value of 12 or higher. Furthermore, the present invention provides a composition comprising pravastatin sodium and 6-epi-pravastatin the quantity of which is 0.2% or less by weight of the composition and 3-α-isopravastatin the quantity of which is 0.2% or less by weight of the composition.
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Page/Page column 9
(2009/07/03)
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- Method of purifying pravastatin
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The present invention provides pure pravastatin compositions and pure compactin compositions, and methods for the preparation thereof.
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Page/Page column 6
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF 1,2,6,7,8,8A-HEXAHYDRO-BETA,DELTA,6-TRIHYDROXY-2-METHYL-8-[(2S)-2-METHYL-1-OXOBUTOXY]-, (BETA R,DELTA R,1S,2S,6S,8S,8AR)-1-NAPHTHALENEHEPTANOIC ACID, SODIUM SALT.
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A process for the preparation of substantially pure 1,2,6,7,8,8a-hexahydro-beta,delta,6-trihydroxy-2-methyl-8-[(2S)-2-methyl-1-oxobutoxy]-, (beta R,delta R,1S,2S,6S,8S,8aR)- 1-Naphthaleneheptanoic acid, sodium salt is disclosed.
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Page/Page column 8
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF PRAVASTATIN
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The invention relates to a process for the preparation of pure pravastatin or a salt thereof using an adsorption chromatography technique. The invention also relates to pharmaceutical compositions that include the pure pravastatin and to use of the compositions for treating hypercholesterolemia.
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Page/Page column 6-7
(2008/06/13)
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- STABILIZED PHARMACEUTICALLY EFFECTIVE COMPOSITION AND PHARMACEUTICAL FORMULATION COMPRISING THE SAME
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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 HMG-CoA reductase inhibitor which is stabilized by forming a homogeneous composition with a buffering substance or a basifying substance. This homogeneous composition is suitably used as the active substance in a pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia.
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- Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
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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 HMG-CoA reductase inhibitor which is stabilized by forming a homogeneous composition with a buffering substance or a basifying substance. This homogeneous composition is suitably used as the active substance in a pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia.
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- Multilayered tablet containing pravastatin and aspirin and method
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A multilayered tablet having three or more layers is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a first layer containing aspirin, another layer containing pravastatin, and a middle barrier layer, which preferably contains a buffering agent, which separates the first layer containing aspirin from the other layer containing pravastatin, and prevents or minimizes interaction of aspirin with pravastatin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.
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- Method for the isolation and purification of pravastatin sodium
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The invention relates to a method for the isolation and purification of pravastatin sodium, intended for application in the pharmaceutical industry. The application of the method results in pravastatin sodium salt of high yield and purity without recovery and additional purification of intermediate products. After the process the fermentationta broth is alkalized to pH 10.2, centrifuged, the resultant filtrate is extracted with butyl acetate and then reextracted with water. The obtained reextract is treated with sodium hydroxide to concentration of the hydroxide in the reextract of 0.5-4 %, and is again extracted with butyl acetate in the presence of sodium chloride. The precipitation of pravastatin is performed with t-octylamine. The obtained crystalline pravastatin-t-octylamine salt is converted into sodium salt, which is purified and recovered.
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- Salts of HMG-CoA reductase inhibitors
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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, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The present invention relates to the new amine salts of HMG-CoA reductase inhibitors, the preparation thereof, the preparation of pure HMG-CoA reductase inhibitors via amine salts thereof, the use of the amine salts of HMG-CoA reductase inhibitors in the process for semisynthetic preparation of HMG-CoA reductase inhibitors, the use of the amine salts of HMG-CoA reductase inhibitors in the process for biotechnological modification of HMG-CoA reductase inhibitors as well as the conversion of the amine salts of HMG-CoA reductase inhibitors into the pharmaceutically acceptable salts of the HMG-CoA reductase inhibitors and the conversion of the amine salts of HMG-CoA reductase inhibitors into the HMG-CoA reductase inhibitors in the lactone form.
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- Process for the purification of pravastatin
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A method of isolating or purifying pravastatin or its pharmaceutically acceptable salt characterized by involving, in the process of isolating or purifying pravastatin or its pharmacologically acceptable salt, the step of extracting pravastatin using an organic solvent represented by the formula CH3CO2R wherein R represents an alkyl group having 3 or more carbon atoms or the step of decomposing impurities using an inorganic acid or an inorganic base; and compositions containing pravastatin sodium thus obtained.
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- Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
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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 HMG-CoA reductase inhibitor which is stabilized by forming a homogeneous composition with a buffering substance or a basifying substance. This homogeneous composition is suitably used as the active substance in a pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia.
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- Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
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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 HMG-CoA reductase inhibitor which is stabilized by forming a homogeneous composition with a buffering substance or a basifying substance. This homogeneous composition is suitably used as the active substance in a pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia.
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- Pravastatin sodium substantially free of pravastatin lactone and epi-pravastatin, and compositions containing same
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The present invention provides pravastatin sodium substantially free of pravastatin lactone and epiprava, the C-6 epimer of pravastatin. The present invention further provides a novel process for recovering pravastatin sodium from a fermentation broth in such high purity. The process includes the stages of forming an solution of the compound by extraction, obtaining an ammonium salt of pravastatin from the solution, purifying the ammonium salt of the compound and transposing the salt of the compound to pravastatin sodium.
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- Process for recovering statin compounds from a fermentation broth
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A novel process for recovering a compound from a fermentation broth that includes the stages of forming an enriched solution of the compound by extraction, obtaining a salt of the compound from the enriched solution, purifying a salt of the compound and trans-salifying the salt of the compound to a metal salt of the compound is disclosed.
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- Novel forms of pravastatin sodium
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New polymorphic forms of pravastatin sodium are provided. Each of the new forms is selectively obtained by crystallization from different solvent systems, each solvent system having a protic component, and by controlling the rate of crystallization through temperature. The new polymorphic forms are suitable for use as active substances of pharmaceutical dosage forms for reduction of serum cholesterol levels in the bloodstream.
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