Ticagrelor preparation composition and preparation method thereof

A technology of ticagrelor and a composition, applied in the field of pharmaceutical preparations, can solve the problems of poor fluidity, difficult to solve the problem of rapid disintegration, difficult to realize rapid disintegration of drugs, etc. Effect

Active Publication Date: 2019-05-03
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
View PDF7 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since ticagrelor itself is a poorly soluble drug and has poor fluidity, it is difficult to achieve rapid disintegration of the drug by the above common wet granulation method. The inventor practiced the technical solution of the patent application and found that most of the obtained samples disintegrated in more than 1 minute
This technology is actually difficult to solve the rapid collapse problem

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
  • Ticagrelor preparation composition and preparation method thereof
  • Ticagrelor preparation composition and preparation method thereof
  • Ticagrelor preparation composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0046] Embodiment 1~3 preparation of ticagrelor preparation composition

[0047] The first step is the crushing of raw materials.

[0048] The raw material of ticagrelor used in the preparation of the preparation composition of the present invention is the same batch, but it needs to be pulverized before the preparation of the preparation composition of the present invention. The inventor made the batch of raw materials into two kinds of raw materials with different particle sizes by airflow pulverization method , to be distinguished by different sub-batch numbers, wherein, embodiment 1 and 2 adopt the raw material of the 1st sub-batch, and embodiment 3 adopts the raw material of the 2nd sub-batch, and the particle size distribution of the raw material after pulverization is shown in the following table:

[0049] Particle size distribution of ticagrelor raw material after crushing in table 1

[0050] Raw material (crushing) batch

Sub-batch 1

Sub-batch 2

...

Embodiment 4

[0063] Example 4 Investigation of the powder properties of ticagrelor granules

[0064] In order to investigate the fluidity improvement effect of ticagrelor granules on ticagrelor raw materials, to ensure that the direct compression method successfully prepares a qualified preparation composition suitable for disintegration, the ticagrelor prepared in Examples 1-3 The particles were tested for intermediate control as follows, and the results are shown in the table below.

[0065] Table 4 Powder Science Investigation of Ticagrelor Granules

[0066]

[0067] From the above investigation, it can be seen that after ticagrelor is prepared into ticagrelor granules by spray drying method, its fluidity is obviously improved.

Embodiment 5

[0068] Example 5 Investigation of the powder properties of ticagrelor blended granules

[0069] Table 5 Powder study of ticagrelor blended granules

[0070] Example

Example 1

Example 2

Example 3

Bulk density

0.43

0.41

0.40

Carr Coefficient

12.2％

13.6％

13.4％

angle of repose

33°

33°

33°

[0071] Note:

[0072] Carr index = (tapped density - bulk density) / tapped density * 100%, the range of Carr index: 5-15%, excellent; 12-16%, good; 18-21%, general, can be pressed into tablets; 23-35%, poor; >40%, very poor.

[0073] Particle angle of repose: 25-30° is excellent; 31-35 is good; 36-40° is fair; 41-45° can be compressed; 46-90° is poor.

[0074] From the investigation results of the physical properties of the blended granules in Examples 1 to 3, the blended powder has good fluidity and can meet the requirements of the subsequent tableting process.

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 provides a ticagrelor preparation composition. The composition is prepared from the following components in percentage by weight: 25-35 percent of ticagrelor granules, 60-70 percent of filler, 3 percent of a disintegrating agent and 2 percent of a lubricating agent. The ticagrelor granules are prepared by a spray-drying method, the content of main drugs in the granules can be increased, and the tablet weight can be reduced to improve the compliance of patients on the one hand; and on the other hand, the ticagrelor granules are prepared by the spray-drying method, the process is smooth, and the material mobility is good, and the process feasibility during high-dose drug loading is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a ticagrelor preparation composition and a preparation method thereof. Background technique [0002] Ticagrelor is a platelet aggregation inhibitor with the chemical name: (1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-difluorophenyl) Cyclopropylamino]-5-(propylthio)-3H-[1,2,3]triazol[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopenta Alkane-1,2-diol. The structural formula is as follows: [0003] [0004] Ticagrelor was developed by AstraZeneca for use in patients with acute coronary syndrome (unstable angina, non-ST-segment elevation myocardial infarction, or ST-segment elevation myocardial infarction), including drug therapy and percutaneous coronary Patients undergoing interventional (PCI) therapy to reduce the incidence of thrombotic cardiovascular events. [0005] In 2010, its tablets were first approved for marketing in the UK. Since the daily d...

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): A61K9/20A61K47/38A61K47/36A61K47/26A61K31/519A61P9/10
Inventor 唐琳李少茹生丽丹赫玉霞蔡兴诗
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap