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Carvedilol sulphate crystals, preparation method and application thereof in medicine

A technology of carvedilol and sulfuric acid, applied in the field of congestive heart failure and angina pectoris, preparation and treatment of high blood pressure, can solve problems that do not involve research on crystal forms and their preparation methods

Active Publication Date: 2012-02-01
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of carvedilol sulfate is reported in the international patent application WO2005051325, but there is no research on related drug composition, crystal form and its preparation method

Method used

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  • Carvedilol sulphate crystals, preparation method and application thereof in medicine
  • Carvedilol sulphate crystals, preparation method and application thereof in medicine
  • Carvedilol sulphate crystals, preparation method and application thereof in medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Carvedilol (synthesized according to patent US4503067 (1983)) 25g (0.062mol) is dissolved in 250ml ethanol, and heating makes it dissolve, and sulfuric acid (0.031mol, 3.04g, the concentrated sulfuric acid of 1.68ml98%) is diluted in 30ml of water. Slowly added dropwise to carvedilol ethanol solution, a white solid precipitated, and continued to stir overnight. The next day, it was filtered with suction and dried under reduced pressure at 60° C. for 3 hours to obtain 25.8 g of carvedilol sulfate as a white solid with a water content of 2.29%. The molar yield is 92.1%.

[0061] Add 2.0 g (2.2 mmol) of carvedilol sulfate prepared in the previous step into 65 ml of 95% ethanol solution, heat and reflux to clarification, keep for 30 minutes, stir and cool to room temperature for crystallization, filter, and the obtained crystals are crystallized at 60 °C for 3 hours in vacuum to obtain 1.86 g of crystals with a mass yield of 93% and a water content of 2.63%. The X-ray di...

Embodiment 2

[0063] Carvedilol sulfate 2.0g (2.2mmol) prepared in Example 1 was added to 250ml of water, heated to reflux until clarified, slowly cooled to room temperature for crystallization, filtered, and the obtained crystals were vacuum-dried at 60°C for 3 hours, 1.87 g of crystals were obtained, the water content was 2.73%, and the mass yield was 93.5%.

Embodiment 3

[0065] Add 2.0 g (2.2 mmol) of carvedilol sulfate prepared in Example 1 into 25 ml of 50% acetone aqueous solution, heat to reflux until clarification, keep for 30 minutes, slowly cool to room temperature for crystallization, filter, and the obtained crystal Vacuum dried at 60° C. to obtain 1.72 g of crystals, with a mass yield of 85.9% and a water content of 2.59%. The characteristic absorption of the X-ray diffraction spectrum of the crystalline sample is the same as that of the A-type crystal.

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Abstract

The invention relates to carvedilol sulphate crystals, a preparation method and application thereof in medicine, in particular to medicaments carvedilol sulphate type A, B, C and D crystals for treating hypertension, congestive heart failure and angina pectoris, a preparation method and application thereof. The preparation method comprises the following step: crystallizing a carvedilol sulphate solid in any crystal form or an amorphous carvedilol sulphate solid with conventional polar organic solvents and aqueous solutions thereof to obtain the type A, B, C or D crystal. The carvedilol sulphate crystals disclosed by the invention have favorable crystal form, and the used crystallizing solvents have the advantages of low toxicity and low residue. The carvedilol sulphate crystals prepared by the method can be better used for clinical treatment.

Description

technical field [0001] The present invention relates to carvedilol sulfate type A, type B, type C and type D crystals, its preparation method and its use in the preparation of medicines for treating hypertension, congestive heart failure and angina pectoris. Background technique [0002] The chemical name of Carvedilol is (±)-1-(9H-carbazolyl-4-oxyl)-3-[[2-(2-methoxyphenoxy)ethyl]amino] -2-propanol, developed by the Boehringer Mannhei company in Germany, was first approved by the FDA on September 14, 1995 for listing in the United States. The trade name is DilatrendTM (Daliquan). Carvedilol is a racemic mixture of two stereoisomers. It is a non-selective β receptor blocker, and it also has the characteristics of an α receptor blocker. The two effects can be used synergistically. Patients with heart failure benefit, for the treatment of hypertension, congestive heart failure and angina pectoris, the efficacy is better than traditional beta blockers. [0003] Carvedilol con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/88A61K31/403A61P9/12A61P9/04A61P9/10
CPCC07D209/88A61K31/403A61P9/04A61P9/10A61P9/12
Inventor 孙飘扬武乖利吴玉霞陈永江
Owner JIANGSU HENGRUI MEDICINE CO LTD
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