Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Crystal form D of anisodine hydrobromide as well as preparation method and use of crystal form D

A kind of technology of anisodine hydrobromide and crystal form, applied in the crystal form D of anisodine hydrobromide and the field of preparation and use thereof, 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: 2016-08-03
CHENGDU FIRST PHARMA DRUG SUBSTANCE CO LTD
View PDF4 Cites 1 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Crystal form D of anisodine hydrobromide as well as preparation method and use of crystal form D
  • Crystal form D of anisodine hydrobromide as well as preparation method and use of crystal form D
  • Crystal form D of anisodine hydrobromide as well as preparation method and use of crystal form D

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1~2

[0055] Anti-solvent addition method to prepare anisodine hydrobromide crystal form D:

[0056] Weigh a certain mass of anisodine hydrobromide solid, dissolve it in a certain volume of positive solvent in Table 1, and add anti-solvent dropwise. After adding the anti-solvent, solids were precipitated, and the stirring was continued until a large amount of solids were precipitated, and the solids were collected by centrifugation and dried. The solids obtained in the examples in Table 1 are respectively marked as samples 1~2, and after testing, samples 1~2 are all crystal form D of anisodine hydrobromide.

[0057] Table 1

[0058] serial number

Embodiment 3~6

[0060] Preparation of anisodine hydrobromide crystal form D by gas-liquid infiltration method:

[0061] Weigh a certain mass of anisodine hydrobromide solid, dissolve it in a certain volume of positive solvent in Table 2, and place it in a 3mL vial, add 3mL of anti-solvent to the 20mL vial, place the above-mentioned 3mL vial In the above 20 mL vial, the 20 mL vial was sealed and allowed to stand at room temperature for 4 days. If a solid precipitated, centrifuge and dry; if no solid precipitated, the solution was evaporated at room temperature. The solids were collected, and the solids obtained in the examples in Table 2 were marked as samples 3-6 respectively. After testing, samples 3-6 were all crystal form D of anisodine hydrobromide.

[0062] Table 2

[0063] serial number

Embodiment 7

[0065] The preparation method of anisodine hydrobromide crystal form D:

[0066] Weigh 14.7mg of anisodine hydrobromide, heat to 165°C and cool to room temperature. The solid was collected, and it was detected that the obtained solid was Form D.

[0067] The X-ray powder diffraction data of the crystal forms obtained in this example are shown in Table 3. 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 .

[0068] table 3

[0069] 2theta

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a novel crystal form of anisodine hydrobromide and a preparation method of the novel crystal form. The novel crystal form of anisodine hydrobromide is named as a crystal form D. The crystal form has the beneficial effects that the stability is good, the solubility and the hygroscopicity meet pharmaceutical requirements, a preparation process is simple in operation and low in cost, and the crystal form has important value to the optimization and development of drugs in future. The crystal form can be used for preparing preparations of drugs for treating hemicranias, vascular headache, retinal vascular spasm, ischemic optic neuropathy, nervous system inflammation and acute paralysis, paralysis agitans, depression and the like caused by 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/10A61K31/439A61P25/06A61P25/00A61P29/00A61P25/24A61P25/02A61P9/10A61P27/02
CPCC07D451/10C07B2200/13
Inventor 刘昭华
Owner CHENGDU FIRST PHARMA DRUG SUBSTANCE CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products