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

Single-crystal crystal forms of clopidogrel hydrochloride and preparation method and application thereof

A technology of clopidogrel hydrochloride and single crystal crystal form is applied in the application field of treatment and prevention of atherosclerotic thrombosis, and can solve problems such as the influence of platelet lifespan and the like

Active Publication Date: 2014-05-07
TIANJIN CHASE SUN PHARM CO LTD
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lifespan of platelets exposed to clopidogrel affected

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
  • Single-crystal crystal forms of clopidogrel hydrochloride and preparation method and application thereof
  • Single-crystal crystal forms of clopidogrel hydrochloride and preparation method and application thereof
  • Single-crystal crystal forms of clopidogrel hydrochloride and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the preparation method of single crystal form of clopidogrel hydrochloride

[0023] Weigh 50 mg of clopidogrel hydrochloride, add 2 ml of acetone and heat to 40°C to dissolve it completely, then cool down to room temperature, slowly add 40 ml of diethyl ether dropwise, and let it stand at room temperature for 2 days to obtain a colorless block single crystal, which is filtered by suction. Example 2: Preparation method of clopidogrel hydrochloride single crystal crystal

Embodiment 2

[0024] Weigh 50mg of clopidogrel hydrochloride, add 2ml methyl ethyl ketone and heat to 40°C to dissolve it completely, then cool down to room temperature, slowly add 40ml diethyl ether dropwise, and let it stand at room temperature for 2 days to obtain a colorless blocky single crystal, which is filtered by suction .

Embodiment 3

[0025] Embodiment 3: the pharmaceutical composition of clopidogrel hydrochloride monocrystalline form

[0026]

[0027]

[0028] Preparation:

[0029] Weigh the single crystal form of clopidogrel hydrochloride according to the prescription amount and pulverize it through a 120-mesh sieve. Polyethylene glycol 6000 and silicon dioxide are respectively passed through a 100-mesh sieve, and mannitol, microcrystalline cellulose, and hydroxypropyl cellulose are respectively passed through a 80-mesh sieve; the polyethylene glycol 6000, microcrystalline cellulose and clopidogrel hydrochloride, Mannitol and hydroxypropyl cellulose were mixed uniformly by equal amount addition method, mixed for 10 minutes, dry-rolled and granulated, and the granules between 24 and 60 mesh were selected. Calculation of granule yield, silicon dioxide, mixing for about 15 minutes; tableting, film-coating.

[0030] After testing, the average dissolution rate in 30 minutes is:

[0031] seria...

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 single-crystal crystal forms of clopidogrel hydrochloride and a preparation method and application thereof. The single-crystal crystal form is the monoclinic system, wherein the crystal axes are as follows: a= 9.2985(5) Angstrom, b= 8.8930(4) Angstrom and c= 21.2663(15) Angstrom; and the crystal plane angles are as follows: alpha= 90degree, beta= 101.575(5)degree and gamma= 90degree. In addition, the invention also relates to pharmaceutical compositions with the single-crystal crystal form, wherein the pharmaceutical compositions are used to prevent and treat atherothrombosis.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to the single crystal configuration of clopidogrel hydrochloride and the application of the pharmaceutical composition thereof in the treatment and prevention of atherosclerotic thrombosis. Background technique [0002] Clopidogrel [2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5-yl)methyl acetate bisulfate] is a platelet aggregation Inhibitors. [0003] CAPRIE: <Study showed that the hazard rate of primary ischemic events (fatal or nonfatal ischemic stroke, myocardial infarction or other vascular death) was 5.32% per year in the clopidogrel group compared with 5.83% per year in the aspirin group . According to the existing clinical treatment data, Zusman et al. recommended the application of clopidogrel in the prevention and treatment of patients with atherosclerosis to prevent the occurrence of acute ischemic events such as stroke and myocardia...

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 Patents(China)
IPC IPC(8): C07D495/04A61K31/4365A61P9/10A61P7/02
Inventor 姚小青孙长海董凯王琦韩志东何晓娟王承睿张淼
Owner TIANJIN CHASE SUN PHARM 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

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com