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Clopidogrel sulphate double salt compound and preparation thereof

A technology of clopidogrel sulfate and clopidogrel, applied in organic chemistry, drug combinations, blood diseases, etc., can solve problems such as poor stability and increased impurities, achieve small gastrointestinal irritation, solve poor stability, and process simple effect

Active Publication Date: 2012-04-25
ZHEJIANG ADAMERCK BIOPHARMLABS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Existing products made of pharmaceutical preparations have poor stability, and if left for too long, impurities will increase. In addition, after oral administration, the incidence of adverse reactions in the gastrointestinal tract is about 27%.

Method used

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  • Clopidogrel sulphate double salt compound and preparation thereof
  • Clopidogrel sulphate double salt compound and preparation thereof
  • Clopidogrel sulphate double salt compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] In a 100ml reaction bottle, add 420mg of clopidogrel hydrogen sulfate, dissolve in 50ml of absolute ethanol, stir, and protect with argon, add 54mg of sodium methoxide to react for 1 hour, concentrate under reduced pressure below 30°C until yellow oil, add appropriate amount of diethyl ether , precipitated a solid, filtered, washed with ether, and dried to obtain 0.439 g of clopidogrel sodium hydrogensulfate as a white solid.

Embodiment 2

[0048] In a 100ml reaction bottle, add 420mg of clopidogrel hydrogen sulfate, dissolve in 50ml of anhydrous methanol, stir, and protect with argon, add 54mg of sodium methoxide to react for 1 hour, concentrate under reduced pressure below 30°C to yellow oil, add an appropriate amount of ether , precipitated solid, filtered, washed with ether, and dried to obtain 0.432 g of clopidogrel sodium bisulfate as a white solid.

Embodiment 3

[0050] In a 100ml reaction bottle, add 420mg of clopidogrel hydrogen sulfate, dissolve in 50ml of anhydrous acetone, stir, and protect with argon, add 54mg of sodium methoxide to react for 1 hour, concentrate under reduced pressure below 30°C until yellow oil, add an appropriate amount of diethyl ether , precipitated solid, filtered, washed with ether, and dried to obtain 0.440 g of clopidogrel sodium bisulfate as a white solid.

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Abstract

The invention provides clopidogrel hydrogen sulfate compound salts. The salts are prepared through the following steps that: clopidogrel sulfate and a MOR compound are mixed according to a molar ratio of 1:1 or 1:0.5 in a polar solvent (or clopidogrel and a hydrogen sulfate are mixed according to a molar ratio of 1:1); after the reaction finishes, the mixed solution is concentrated, added with polar or nonpolar solvent for crystallization and filtered; and solid obtained is dried and the clopidogrel hydrogen sulfate compound salt is obtained. The molecular structure of the clopidogrel hydrogen sulfate compound salts contains any one of sodium ions, potassium ions, ammonium ions and cesium ions. The preparation method is reasonable in design and simple in process. The clopidogrel hydrogen sulfate compound salts prepared by the method have the characteristics of good stability, small irritant to the gastrointestinal tracts and the like. The clopidogrel hydrogen sulfate compound salts have a general structural formula as follow.

Description

technical field [0001] The invention belongs to the technical field of chemical industry and pharmacy, and relates to a clopidogrel sulfate double salt compound and a preparation method thereof. technical background [0002] The chemical name of Clopidogrel Hydrogen Shlfate is S(+)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothiophene[3,2-c] Pyridine-5) methyl acetate hydrogen sulfate, structural formula: [0003] [0004] It is mainly used for the prevention and treatment of heart, brain and other arterial circulation disorders caused by high platelet aggregation. [0005] Clopidogrel bisulfate is a platelet aggregation inhibitor developed by Sanofi Sandela Fort Pharmaceutical Company of France. The product was first launched in the United States in March 1998, and then entered the markets of Europe, North America, Australia, and Singapore. In my country, in 2001, France Sanofi Santa Dela Fort obtained the import approval document for clopidogrel bisulfate tablets in Chin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61P7/02A61P9/00
Inventor 漆又毛揭清张冯敏张君顾颖叶磊
Owner ZHEJIANG ADAMERCK BIOPHARMLABS