81176-41-2

Upstream product

• 81093-37-0 pravastatin 
• 81093-37-0 3β-hydroxy ML-236B 
• 81093-40-5 3β-hydroxy ML-236B methylester 
• 73573-88-3 mevastatin 

Downstream Products

• 81093-37-0 pravastatin 
• 85798-96-5 lactone form of C-6 epimer of pravastatin 
• 85956-22-5 pravastatin lactone 
• 136590-28-8 R-195 

Relevant academic research and scientific papers

CRYSTALLINE FORM OF PRAVASTATINE AND PROCESS FOR THE PREPARATION THEREOF

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.

Methods for predicting the response to statins

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.

PURIFICATION OF PRAVASTATIN

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.

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.

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.

PROCESS FOR THE PREPARATION OF PRAVASTATIN

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.

Method of purifying pravastatin

The present invention provides pure pravastatin compositions and pure compactin compositions, and methods for the preparation thereof.

Method for the isolation and purification of pravastatin sodium

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.

STABILIZED PHARMACEUTICALLY EFFECTIVE COMPOSITION AND PHARMACEUTICAL FORMULATION COMPRISING THE SAME

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.

Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same

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.

Multilayered tablet containing pravastatin and aspirin and method

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.