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Atorvastatin amino acid and preparation method thereof

A technology of atorvastatin and atorvastatin tert-butyl ester, which is applied in the field of cardiovascular medicine, can solve the problems of increasing blood high-density lipoprotein levels, lowering serum triglyceride levels, etc., to promote protein synthesis, Effects of protecting liver function and improving immune function

Active Publication Date: 2013-08-14
SHANGHAI KECHOW PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its main action site is in the liver. As a result, blood cholesterol and low-density lipoprotein cholesterol levels are lowered, serum triglyceride levels are moderately lowered, and blood high-density lipoprotein levels are increased, thereby preventing and treating atherosclerosis and coronary heart disease. It is often used to treat hypercholesterolemia and mixed hyperlipidemia, prevent and treat coronary heart disease and cerebral apoplexy, but long-term use of it can also cause liver problems

Method used

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  • Atorvastatin amino acid and preparation method thereof
  • Atorvastatin amino acid and preparation method thereof
  • Atorvastatin amino acid and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0050] A kind of atorvastatin arginine salt, the structural formula after its salification is as follows:

[0051]

[0052] A preparation method of atorvastatin arginine salt, the steps are as follows:

[0053] (1) Weigh 117mg of atorvastatin, dissolve it in 1mL of ethanol, and heat it to about 75°C. The solution is uniform and opaque, forming solution A;

[0054] (2) Weigh 36mg arginine, dissolve in 0.1mL H 2 O, and heated to about 75°C, the solution was uniform and clear, forming solution B;

[0055] (3) Add the above solution B dropwise into solution A, the mixed solution starts to become clear, heat to about 75°C and reflux, cool and precipitate crystals, separate the product, and measure it with 1H NMR, MS, etc., it is Atorval Arginine salts of statins.

[0056] The present embodiment adopts the acid of atorvastatin, which has the effect of lowering blood fat, and forms a water-soluble salt with arginine, and arginine not only has the function of generating salt wit...

Embodiment 2

[0058] A kind of atorvastatin lysine salt, the structural formula after its salification is as follows:

[0059]

[0060] A preparation method of atorvastatin lysine salt, the steps are as follows:

[0061] (1) Weigh 117mg of atorvastatin, dissolve it in 1mL of ethanol, and heat it to about 75°C. The solution is uniform and opaque, forming solution A;

[0062] (2) Weigh 30mg lysine, dissolve in 0.1mL H 2 O, and heated to about 75°C, the solution was uniform and clear, forming solution B;

[0063] (3) Add the above solution B dropwise into solution A, the mixed solution starts to become clear, heat to about 75°C, heat to about 75°C to reflux, cool to precipitate crystals, separate the product, and measure it with 1H NMR, MS, etc. , which is the lysine salt of atorvastatin.

[0064] In this embodiment, atorvastatin acid is reacted with lysine to generate its salt, which further promotes the efficacy of the original drug atorvastatin. Lysine is one of the essential amino a...

Embodiment 3

[0066] A kind of atorvastatin histidine salt, the structural formula after its salification is as follows:

[0067]

[0068] A preparation method of atorvastatin histidine salt, the steps are as follows:

[0069] (1) Weigh 117mg of atorvastatin, dissolve it in 1mL of ethanol, and heat it to about 75°C, the solution is uniform and opaque, forming solution A;

[0070] (2) Weigh 32mg histidine, dissolve in 0.1mL H 2 O, and heated to about 75°C, the solution was uniform and clear, forming solution B;

[0071] (3) Add the above-mentioned solution B into the solution A drop by drop, the mixed solution starts to become clear, and is heated to about 75° C. to reflux, and the product is separated, which is the histidine salt of atorvastatin.

[0072] In this example, atorvastatin acid is reacted with basic histidine to form a salt, which can improve the side effects of the original drug atorvastatin. Histidine (L-Histidine) can maintain our growth and digestion. Histidine plays a...

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Abstract

The invention relates to an atorvastatin amino acid and a preparation method thereof. Atorvastatin acid reacts with alkaline amino acid to obtain the compound. The preparation method comprises the following steps: (1) weighing the atorvastatin acid, and dissolving the atorvastatin acid into C1-C6 alcohol solvents, water or chlorinated hydrocarbon solvent to form a solution A; (2) weighing the alkaline amino acid, and dissolving the alkaline amino acid into C1-C6 alcohol solvents or water to form a solution B; and (3) adding the solution B into the solution A, enabling the mixed solution to beclear, separating out crystals from a mother solution, i.e., the atorvastatin amino acid. The atorvastatin amino acid prepared by the invention not only has the effect of treating hypercholesterolemia and combined hyperlipidemia, but also additionally has the functions of amino acid, for example, arginine has a protection function on liver, and therefore, the salt provided by the invention effectively makes up the defect that the known calcium salt, kali salt, sodium salt and the like have the side effect of damage to liver.

Description

technical field [0001] The invention belongs to the field of cardiovascular disease medicine, and relates to atorvastatin salt, in particular to an atorvastatin amino acid salt and a preparation method thereof. Background technique [0002] Cardiovascular disease seriously endangers human health and affects human quality of life. Lipitor, also known as Atorvastatin, is a statin blood lipid regulating drug and belongs to HMG-CoA reductase inhibitor. Atorvastatin calcium salt is mainly used at present. [0003] Atorvastatin calcium salt itself is inactive, and its main active ingredient is the hydrolyzate after oral absorption. It competitively inhibits the rate-limiting enzyme hydroxymethylglutaryl-CoA reductase in the process of cholesterol synthesis in vivo, thereby reducing the synthesis of cholesterol and increasing the synthesis of low-density lipoprotein receptors. Its main action site is in the liver. As a result, blood cholesterol and low-density lipoprotein cholest...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/34C07D233/64A61K31/40A61P3/06A61P1/16A61P37/04A61P13/12
Inventor 田红旗程瑛张瀛刘春磊赵巧凤
Owner SHANGHAI KECHOW PHARMA
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