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Preparation of amorphous atorvastatin calcium

An atorvastatin calcium and amorphous technology, which is applied in the new preparation field of amorphous atorvastatin calcium, can solve the problems of flammability and explosion, and achieves the advantages of less time-consuming filtration, reduced hidden dangers in safety production, and easy large-scale operation. Effect

Active Publication Date: 2009-07-01
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of atorvastatin calcium in alcohol solution, especially methanol, is the best. This patent limits the dissolution solvent to non-hydroxyl solvents, especially tetrahydrofuran, and a defect of tetrahydrofuran is that it is more flammable and explosive than lower alcohols. In industry, the use of

Method used

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  • Preparation of amorphous atorvastatin calcium
  • Preparation of amorphous atorvastatin calcium
  • Preparation of amorphous atorvastatin calcium

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Take 1 kg of crystalline atorvastatin calcium, add 5 L of methanol, stir to dissolve, slowly add it into 40 L of isopropyl ether at room temperature, precipitate a solid, continue stirring for 2 hours, filter, drain, and vacuum dry at 50 ° C for 12 hours to obtain 850 g Amorphous atorvastatin calcium, X-ray powder diffraction pattern confirms the amorphous nature of the product.

Embodiment 2

[0034] Take 1kg of crystalline atorvastatin calcium, add 15L of ethanol, stir to dissolve, slowly add to 160L of isopropyl ether at room temperature, precipitate solid, continue to stir for 2 hours, vacuum filter, drain, and vacuum dry at 50°C for 12 hours to obtain 830 g of amorphous atorvastatin calcium, the X-ray powder diffraction pattern confirms the amorphous nature of the product.

Embodiment 3

[0036] Take 1kg of crystalline atorvastatin calcium, add 20L of ethanol, stir to dissolve, slowly add to 240L of isopropyl ether at room temperature, precipitate solid, continue to stir for 2 hours, vacuum filter, drain, and vacuum dry at 50°C for 12 hours to obtain 825 g of amorphous atorvastatin calcium, the X-ray powder diffraction pattern confirms the amorphous nature of the product.

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Abstract

The invention relates to a novel method for preparing amorphous atorvastatin calcium. The method comprises: dissolving crystallized atorvastatin calcium or a mixture of the crystallized atorvastatin calcium and the amorphous atorvastatin calcium in a lower alcohol and lower ketone solvent; adding an atorvastatin calcium solution into a proper nonpolar anti-solvent, and separating out solid; and removing the solvent through filtration, and obtaining the amorphous atorvastatin calcium. The novel method has the advantages of high boiling point of the solvent used, reduction of the potential safe production hazard, less filtration time, low energy consumption, and easy mass operation.

Description

technical field [0001] The invention relates to a new preparation method of amorphous atorvastatin calcium. Background technique [0002] Atorvastatin is [R-(R,R)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[ (Phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid, listed product is its hemicalcium salt trihydrate, is listed and sold by U.S. Warner Company (Warner-Lambert), trade name is LIPITOR, can be represented by formula I: [0003] [0004] Atorvastatin is a member of a class of drugs known as statins, which are currently the most effective drugs available to reduce the concentration of low-density lipoprotein (LDL) particles in the bloodstream of patients at risk of cardiovascular disease. High levels of LDL in the bloodstream are associated with coronary injury, they impede blood flow, may rupture and promote thrombus formation; Goodman Gilman, The Pharmacological Basis of Therapeutics 879 (9th ed. 1996). Lowering plasma LDL levels has been shown ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/34
Inventor 郑利刚杨汉煜马玉秀张明陈玉洁
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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