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Crystal form B of anisodine hydromide and preparation method and application of crystal form B

A kind of technology of anisodine hydrobromide and crystal form, applied in the crystal form B of anisodine hydrobromide and the field of preparation and use, can solve the problem that no patent discloses the preparation method of anisodine hydrobromide crystal form, etc. problem, to achieve the effects of low cost, good stability, and simple operation of the preparation process

Inactive Publication Date: 2016-08-17
CHENGDU FIRST PHARMA DRUG SUBSTANCE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, preparation methods and uses or pharmaceutical compositions related to anisodine are disclosed, but no patent discloses the crystal form of anisodine hydrobromide and its preparation method

Method used

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  • Crystal form B of anisodine hydromide and preparation method and application of crystal form B
  • Crystal form B of anisodine hydromide and preparation method and application of crystal form B
  • Crystal form B of anisodine hydromide and preparation method and application of crystal form B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation method of anisodine hydrobromide crystal form B:

[0054] Weigh 21.4mg of anisodine hydrobromide solid, dissolve it in 0.3mL of methanol, add 6.0mL of anti-solvent ethyl acetate dropwise to it, a solid precipitates out, centrifuge, and dry. The solid was collected, and it was detected that the obtained solid was Form B.

[0055] Table 1 shows the X-ray powder diffraction data of the crystal forms obtained in this example. Its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in image 3 .

[0056] Table 1

[0057] 2theta

Embodiment 2

[0059] Anti-solvent addition method to prepare anisodine hydrobromide crystal form B:

[0060] Weigh 9.6 mg of anisodine hydrobromide solid, dissolve it in 0.2 mL of methanol, add 3.0 mL of anti-solvent ethyl acetate dropwise to it, a solid precipitates out, centrifuge, and dry. The solid was collected, and it was detected that the obtained solid was Form B.

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Abstract

The invention relates to a novel crystal form of anisodine hydromide and a preparation method of the novel crystal form. The provided novel crystal form of the anisodine hydromide is named as the crystal form B. The crystal form is good in stability, solubility and hygroscopicity meet medicinal requirements, a preparation process is simple in operation, the cost is low, and significant value is achieved for medicine optimization and development. The crystal form can be used for preparing preparations of medicine for treating acute paralysis, shaking palsy and depressive disorder caused by migraine, vascular headache, retinal vascular spasm, ischemic optic neuropathy, inflammation of the nervous system and blood vessels of brain.

Description

technical field [0001] The invention relates to a new crystal form of anisodine hydrobromide, a preparation method and application thereof. Background technique [0002] Anisodine is a new anticholinergic drug extracted from the plant Anisodina tangutica. It is the first isolated cholinergic receptor blocker in my country. Its hydrobromide is mainly used clinically. Anisodine hydrobromide can be used to treat migraine, vascular headache, retinal vasospasm, ischemic optic neuropathy, nervous system inflammation and acute paralysis caused by cerebrovascular, paralysis agitans, depression, etc. It can also be used for organophosphate Detoxification of ester pesticide poisoning. Clinically used anisodine preparations include tablets, injections and film preparations, etc. These preparations have certain deficiencies in terms of stability, dissolution rate, etc., while playing a positive clinical therapeutic role. The structure of anisodine is shown in formula (I). [0003] ...

Claims

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Application Information

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IPC IPC(8): C07D451/10A61K31/439A61P25/06A61P27/02A61P9/10A61P25/00A61P25/24A61P25/14A61P25/16
CPCC07D451/10C07B2200/13
Inventor 刘昭华
Owner CHENGDU FIRST PHARMA DRUG SUBSTANCE CO LTD
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