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

Tablet containing ticagrelor

A technology for ticagrelor and tablets, applied in the field of tablets containing ticagrelor and its preparation, can solve the problems of drug loss, unfavorable production operations, high production costs, etc., achieve high bioavailability and facilitate absorption Effect

Inactive Publication Date: 2016-08-10
CHENGDU GUOHONG PHARMA
View PDF12 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The problem to be solved in the present invention is that the synthetic ticagrelor crude drug cannot be directly used in the preparation of existing ticagrelor tablets, and the directly synthesized particle diameter D 90 The raw material drug of ticagrelor with a size of 50μm~70μm is micronized to D 90 Only when it is less than 30 μm can a tablet with a dissolution rate of more than 70% in 45 minutes be obtained in 900ml of 0.2% (w / v) polysorbate 80 solution, paddle method 50r / min; but the micronization process is easy to bring the drug Loss, electrostatic adsorption, dust flying and other problems are not conducive to production operations, and the production cost is extremely high

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
  • Tablet containing ticagrelor
  • Tablet containing ticagrelor
  • Tablet containing ticagrelor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107]

[0108] First mix hypromellose and low-substituted hydroxypropyl cellulose evenly, and then mix with the same amount of ticagrelor, so that the amount is increased until all the ticagrelor is mixed, and then mixed with anhydrous hydrogen phosphate Calcium is mixed evenly, and finally sorbitol is added, mixed evenly, granulated with aqueous solution through a 24-mesh sieve, dried at 60°C, granulated, added with micropowder silica gel, mixed evenly, compressed into tablets, and coated.

Embodiment 2

[0110]

[0111] First mix the hypromellose and crospovidone evenly, then mix with the same amount of ticagrelor, so that the amount is increased until all the ticagrelor is mixed, and then mixed with anhydrous calcium hydrogen phosphate Uniformly, add lactose at the end, mix evenly, sieve with 24 mesh, wet granulate with aqueous solution, dry at 70°C, granulate, add talcum powder, mix evenly, compress into tablets, and coat.

Embodiment 3

[0113]

[0114] First mix hypromellose with hydroxypropyl cellulose and croscarmellose sodium evenly, then mix with the same amount of ticagrelor, and increase the amount until all ticagrelor is mixed. , mixed evenly with sucrose, then mixed evenly with calcium orthophosphate, finally mixed evenly with mannitol, granulated with an aqueous solution through a 24-mesh sieve, dried at 70°C, granulated, added with talc powder and magnesium stearate, mixed evenly After compression, coating.

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

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to a tablet containing ticagrelor. The tablet includes, by weight, 15-40% of the ticagrelor which is not micronized, 32-50% of a water-soluble filling agent, 12-28% of a water-insoluble filling agent being lower than 150 [mu]m in D90 of particles, 2-10% of a disintegrating agent, 2-5% of an adhesive and 0.5-1.5% of a lubricant. The water-insoluble filling agent is one selected from calcium hydrogen phosphate dihydrate, anhydrous calcium hydrogen phosphate and calcium phosphate. The product has effective bioavailability to most of people and has no strict requirement on particle size of the ticagrelor. A ticagrelor raw material drug which is synthesized directly through a synthesis method can be used as a preparation raw material without superfine grinding and the like special technologies, so that the tablet is simple in preparation process and has uniform and stable quality.

Description

technical field [0001] The invention relates to a pharmaceutical composition, more specifically, to a tablet containing ticagrelor and a preparation method thereof. Background technique [0002] Ticagrelor is a new type of selective small molecule anticoagulant drug developed by AstraZeneca, which can significantly inhibit platelet aggregation induced by adenosine diphosphate (ADP). It has the advantages of rapid onset of action, direct action of non-prodrugs, and not affected by individual genetic differences, and is different from thienopyridine drugs, ticagrelor binds reversibly to platelets, and can quickly restore platelets after drug withdrawal Features. At present, ticagrelor has been listed as the first-line recommended drug by multiple guidelines at home and abroad. [0003] Ticagrelor has very poor water solubility, and its solubility in water at room temperature is reported to be only 10 mg / L (Tang Zhongming. 2011 US FDA Approved Drug Profile. International Phar...

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): A61K9/20A61K31/519A61K47/02A61K47/38A61P7/02
Inventor 张令汪飞郭礼新郭晖
Owner CHENGDU GUOHONG PHARMA
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