Purification method of cetirizine hydrochloride

A technology of cetirizine hydrochloride and a purification method, applied in the field of drug preparation, can solve problems such as adverse drug reactions, and achieve the effects of low health hazard, simple operation and simple equipment

Active Publication Date: 2014-09-17
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the amount of impurities in drug raw materials is the main cause of adverse drug reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 10g cetirizine hydrochloride, 0.50g potassium iodide are dissolved in the mixed solution of 90ml water and ethanol (3: 1), stir; In mixed reaction solution, add 40% concentration potassium bicarbonate solution, until reaction solution pH is 7.5 -8.5, stand for 15min; continue to add the mixed solution of 360ml ethanol, dichloromethane (1:1) in the reaction solution, add hydrochloric acid, until the pH of the reaction solution reaches 6.0-7.0, crystallize 1.5 hours; Filter, use two The product was washed three times with methyl chloride and dried to obtain 9.4 g of the product with a yield of 94%. The purity of the product was 99.6% as detected by HLPC.

Embodiment 2

[0022] 10g cetirizine hydrochloride, 0.40g potassium iodide are dissolved in the mixed solution of 90ml water and ethanol (3: 1), stir; In mixed reaction solution, add 40% concentration potassium bicarbonate solution, until reaction solution pH is 7.5 -8.5, let stand for 15min; continue to add the mixed solution of 270ml ethanol, dichloromethane (1:1) to the reaction solution, add hydrochloric acid, until the pH of the reaction solution reaches 6.0-7.0, crystallize for 1.5 hours; filter, use two The product was washed three times with methyl chloride and dried to obtain 9.0 g of the product with a yield of 90%. The purity of the product was 99.5% as detected by HLPC.

Embodiment 3

[0024] 10g cetirizine hydrochloride, 0.56g potassium iodide are dissolved in the mixed solution of 90ml water and ethanol (3: 1), stir; In mixed reaction solution, add 40% concentration potassium bicarbonate solution, until reaction solution pH is 7.5 -8.5, let stand for 15min; continue to add the mixed solution of 450ml ethanol, dichloromethane (1:1) to the reaction solution, add hydrochloric acid, until the pH of the reaction solution reaches 6.0-7.0, crystallize for 1.5 hours; filter, use dichloromethane The product was washed three times with methyl chloride and dried to obtain 9.2 g of the product with a yield of 92%. The purity of the product was 99.2% as detected by HLPC.

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PUM

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Abstract

The invention relates to a purification method of cetirizine hydrochloride. The method comprises the following steps: (1) dissolving cetirizine hydrochloride and a small amount of potassium iodide in a mixed solution of water and ethanol, and stirring evenly; (2) adding a proper amount of potassium bicarbonate solution with concentration of 40% to the mixed reaction solution, adjusting the pH value of the reaction solution to 7.5-8.5, and standing for 15-30 min; (3) continuing adding a proper amount of a mixed solution of ethanol and dichloromethane, adding hydrochloric acid to regulate the pH value of the reaction solution to 6-7, and crystallizing for 1-1.5 h; and (4) filtering, washing the products with methylene chloride more than 2 times, and drying to obtain the products.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a method for purifying cetirizine hydrochloride. Background technique [0002] Cetirizine is an over-the-counter potent H1 receptor antagonist, mainly used for seasonal and perennial allergic rhinitis, allergic reactions caused by drugs, food and insect bites, and urticaria and skin itching caused by allergens. After oral administration into the body, it quickly binds to histamine H1 on the target cell membrane [0003] Receptor binding, blocking histamine activation of target cells. Cetirizine has no obvious anticholinergic and anti-serotonin effects. In normal doses, it is difficult to pass through the blood-brain barrier. This product can inhibit the transmission of histamine in the early stage of allergic reaction, reduce the migratory activity of inflammatory cells and the release of transmitters in the late stage of allergic reaction, so it is also effective for delay...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/088
CPCC07D295/088
Inventor 王燕清莫德欢吴起娟周禹
Owner LIVZON PHARM GRP INC
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