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A kind of 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 difficulty in solving the problem of rapid disintegration, poor fluidity, and difficulty in realizing rapid disintegration of the drug, and achieves the improvement of drug dissolution rate, good fluidity and easy dissolving. Effect

Active Publication Date: 2021-03-16
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • 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

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  • A kind of ticagrelor preparation composition and preparation method thereof
  • A kind of ticagrelor preparation composition and preparation method thereof
  • A kind of 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 Bulk...

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.

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Abstract

A ticagrelor preparation composition, which comprises ticagrelor granules, fillers, disintegrants and lubricants, wherein the ticagrelor granules account for 25 to 35% by weight of the ticagrelor preparation composition %, the filler accounts for 60 to 70% by weight of the ticagrelor preparation composition, the disintegrant accounts for 3% by weight of the ticagrelor preparation composition, and the lubricant accounts for 60% by weight of the ticagrelor preparation composition. The percentage by weight of the composition of the rello preparation is 2%. The present invention prepares ticagrelor granules by spray drying, on the one hand, it can increase the main drug content in the granules, reduce the tablet weight to increase patient compliance; on the other hand, prepare ticagrelor granules by spray drying, The process is smoother and the fluidity of the material is better, which improves the feasibility of the process when the drug is loaded at a high dose.

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

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Application Information

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Patent Type & Authority Patents(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
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