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Preparation method of rosuvastatin

A technology of rosuvastatin and inhibitors, applied in the field of preparation of rosuvastatin, can solve the problems of insufficient lipid-lowering effect and slow treatment process, so as to enhance weight-loss and lipid-lowering efficacy, skin health, prevention and Migraine Relief Effects

Inactive Publication Date: 2018-11-23
ABA CHEM NANTONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides a preparation method of rosuvastatin, which has the advantages of good lipid-lowering effect, solves a method for preparing amorphous rosuvastatin calcium without impurities and can be used for the treatment of Symptoms such as hyperlipidemia, hypercholesterolemia and atherosclerosis, but the lipid-lowering effect of the method for preparing amorphous rosuvastatin calcium without impurities is not good enough, and the treatment process is slow

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A preparation method of rosuvastatin, comprising the following steps:

[0021] 1) Tris(4-fluorophenyl)phosphine 0.2mg, tert-butyl group 0.2mg, carboxyl protecting group 0.2mg, sec-butylamine 0.5mg, nicotinic acid 0.2mg, fibrates 0.3mg, sulfonyl Urea 0.2mg, peripheral calcium channel blocker 0.5mg, angiotensin-converting enzyme inhibitor 0.9mg, anti-obesity drug 0.2mg, vitamin D2 (ergocalciferol) 0.2mg and heteroaryl 0.2mg are mixed by machine core, and reserve the core as a spare;

[0022] 2) Spray the medicament onto the tablet core prepared in step 1), mix rosuvastatin calcium 1mg, calcium acetate 0.2mg and film tablet coating 0.2mg via machine to prepare the first layer of coating to provide Rosuvastatin layer, then coat the tablet core prepared in step 1) with the first layer of coating to make rosuvastatin granules, and keep the rosuvastatin granules for subsequent use;

[0023] 3) Coating the rosuvastatin granules prepared in step 2) with 0.8 mg of granule coati...

Embodiment 2

[0027] A preparation method of rosuvastatin, comprising the following steps:

[0028] 1) Add 0.6mg of tris(4-fluorophenyl)phosphine, 0.6mg of tert-butyl group, 0.6mg of carboxyl protecting group, 0.75mg of sec-butylamine, 0.6mg of nicotinic acid, 0.65mg of fibrates, sulfonyl Urea 0.6 mg, peripheral calcium channel blocker 0.75 mg, angiotensin converting enzyme inhibitor 1.15 mg, anti-obesity drug 0.6 mg, vitamin D2 (ergocalciferol) 0.6 mg and heteroaryl 0.6 mg are mixed by machine core, and reserve the core as a spare;

[0029] 2) Spray the medicament onto the tablet core prepared in step 1), mix 1.3 mg of rosuvastatin calcium, 0.6 mg of calcium acetate and 0.6 mg of film tablet coating via machine to obtain the first layer of coating to provide Containing the rosuvastatin layer, then coating the tablet core prepared in step 1) with the first layer of coating to obtain rosuvastatin granules, and keeping the rosuvastatin granules for subsequent use;

[0030] 3) Coat the rosuv...

Embodiment 3

[0034] A preparation method of rosuvastatin, comprising the following steps:

[0035] 1) Tris(4-fluorophenyl)phosphine 1mg, tert-butyl group 1mg, carboxyl protecting group 1mg, sec-butylamine 1mg, nicotinic acid 1mg, fibrates 1mg, sulfonylureas 1mg, peripheral calcium Channel blocker 1mg, angiotensin-converting enzyme inhibitor 1.4mg, anti-obesity drug 1mg, vitamin D2 (ergocalciferol) 1mg and heteroaryl 1mg were mixed by machine to make a tablet core, and the tablet core was reserved for use;

[0036]2) Spray the medicament onto the tablet core prepared in step 1), mix rosuvastatin calcium 1.5mg, calcium acetate 1mg and film tablet coating 1mg via machine to prepare the first layer of coating to provide Suvastatin layer, then coat the tablet core prepared in step 1) with the first layer of coating to make rosuvastatin granules, and keep the rosuvastatin granules for subsequent use;

[0037] 3) Coating the rosuvastatin granules prepared in step 2) with 1.5 mg of granule coatin...

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Abstract

The invention relates to the technical field of medicines and discloses a preparation method of rosuvastatin. The preparation method comprises the following steps: 1) mixing 0.2 to 1mg of tri(4-fluorophenyl)hydrogen phosphide, 0.2 to 1mg of a tert-butyl group, 0.2 to 1mg of a carboxyl protection group, 0.5 to 1mg of sec-butylamine, 0.2 to 1mg of nicotinic acid, 0.3 to 1mg of fibrates, 0.2 to 1mg of sulfonylurea, 0.5 to 1mg of a peripheral calcium channel blocker, 0.9 to 1.4mg of an angiotensin converting enzyme inhibitor, 0.2 to 1mg of an anti-obesity drug, 0.2 to 1mg of vitamin D2 (ergocalciferol) and 0.2 to 1mg of heteroaryl through a machine to prepare a chip and taking the chip for later use. According to the preparation method of the rosuvastatin, the rosuvastatin has the effects of alleviating gastrointestinal disorders, enabling skin to be more healthy, preventing and alleviating serious cephalagra, promoting blood circulation, lowering blood pressure and alleviating a diarrheaphenomenon; the weight-losing and lipid-lowering effects of the rosuvastatin are totally enhanced; the rosuvastatin is applicable to various diseases and daily weight loss and the aim of good lipid lowering effect is realized.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of rosuvastatin. Background technique [0002] Rosuvastatin is an HMG coenzyme A reductase inhibitor. Rosuvastatin has a high affinity for hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, and reduces cholesterol by competing with HMG-CoA reductase Biosynthesis, causing increased clearance of cholesterol from the blood. [0003] For example, the Chinese invention CN 101208307 B discloses a method for preparing impurity-free amorphous rosuvastatin calcium, which can be used to treat hyperlipidemia and hypercholesterolemia symptoms such as hyperemia and atherosclerosis, but the lipid-lowering effect of the method for preparing amorphous rosuvastatin calcium without impurities is not good enough, and the treatment process is slow, so a preparation method of rosuvastatin is proposed to solve the problems raised above. Contents of the invention [0004] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/12A61K31/505A61K31/455A61K45/06A61P3/06A61P9/10
CPCA61K9/1617A61K9/167A61K9/1682A61K31/455A61K31/505A61K31/592A61K45/06A61P3/06A61P9/10A61K2300/00
Inventor 蒋信义徐军刘汝章
Owner ABA CHEM NANTONG
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