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New crystal form B of Betahistine mesilate and preparation method therefor

A technology of methanesulfonic acid and stin crystal, applied in the field of medicine, can solve the problems of strong hygroscopicity and difficult preparation, and achieve the effects of good stability, good reproducibility and mild reaction conditions

Inactive Publication Date: 2015-08-26
BEIJING ENCHENG KANGTAI BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Betahistine mesylate crystal form A has strong hygroscopicity and is difficult to prepare

Method used

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  • New crystal form B of Betahistine mesilate and preparation method therefor
  • New crystal form B of Betahistine mesilate and preparation method therefor
  • New crystal form B of Betahistine mesilate and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Put 10g of betahistine mesylate into 100mL of isopropanol, add 2mL of water, heat up to 50°C under stirring, dissolve all the solids, keep stirring for 30min, cool down to 30°C and stir for 3h to slowly crystallize, filter, The filter cake was air-dried at 45±5°C to obtain 6.6 g of white crystals of betahistine mesylate, whose melting point was 136-138°C according to differential scanning calorimetry (DSC). figure 2 The main test data of its X-ray diffraction is shown in the table below (listing the test data with relative intensity greater than 2%), and the accompanying drawings are shown in the attached description. Figure 4 .

[0038]

Embodiment 2

[0040] Put 10g of betahistine mesylate into 75mL of ethanol, add 1mL of water, heat up to 50°C under stirring, dissolve all the solids, keep stirring for 30min, cool down to 0°C and stir for 3h to crystallize, filter, and filter cake in Blow drying at 45±5°C to obtain 4.2 g of white crystals of betahistine mesylate. The differential scanning thermogram (DSC chart) and X-ray diffraction chart are respectively attached to the instructions figure 2 , Figure 4 Consistent within the margin of error.

[0041] implementation

[0042] Put 10g of betahistine mesylate into 150mL of tetrahydrofuran, add 3mL of water, heat up to 50°C under stirring to dissolve all the solids, keep stirring for 30min, cool down to 0°C and stir for 3h to slowly crystallize, filter, and the filter cake is Blow drying at 45±5°C to obtain 3.7 g of white crystals of betahistine mesylate B. The differential scanning thermogram (DSC chart) and X-ray diffraction chart are respectively attached to the instruc...

Embodiment 4

[0044]Put 10g of betahistine mesylate into 100mL of a mixed solution of ethylene glycol and acetonitrile (50:50), add 1mL of water, heat up to 55°C with stirring to dissolve all the solids, keep stirring for 30min, and cool down to 30°C Slowly crystallized, filtered, and the filter cake was air-dried at 45±5°C to obtain 3.3 g of white crystals of betahistine mesylate B. The differential scanning thermogram (DSC chart) and X-ray diffraction chart are respectively attached to the instructions figure 2 , Figure 4 Consistent within the margin of error.

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Abstract

The invention provides a new crystal form B of Betahistine mesilate treating hemangiectasis and a preparation method therefor. The new crystal form B of Betahistine mesilate is characterized in that the melting point is 136-138 DEG C; the X-ray powder diffraction spectrum has corresponding characteristic diffraction peaks at positions of the 2theta value being 17.250, 19.690, 21.141, 21.400, 21.649, 22.570, 25.518, 32.389 and 35.760+ / -0.2 degrees. The new crystal form has advantages of high purity, high stability, convenient for industrial production and the like.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new crystal form B of betahistine mesylate and a preparation method thereof. Background technique [0002] Betahistine mesilate (Betahistine mesilate, CAS: 54856-23-4), its chemical structure is shown in the figure below: [0003] [0004] Betahistine mesylate has a similar chemical structure to histamine and is a histamine drug. It is a vasodilator developed by Eisai Co., Ltd. of Japan, which is used for the treatment of vertigo, vomiting and tinnitus caused by inner ear vertigo (ie Meniere's syndrome), cerebral arteriosclerosis, insufficient cerebral blood supply and high blood pressure. Betahistine mesylate as a strong H 3 Receptor antagonists can increase inner ear microcirculation, reduce vestibular afferent nerve discharge rate, enhance central vestibular compensation, and improve blood supply of vertebral and low base arteries, thereby effectively improving vertigo caused by v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/38C07C309/04C07C303/44A61K31/4458A61P27/16A61P9/10A61P9/12
CPCC07D213/38A61K9/0053A61K9/2054C07B2200/13
Inventor 卢建勋张锦聪孙占国龚万渠张海滨王斌
Owner BEIJING ENCHENG KANGTAI BIOLOGICAL TECH
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