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Hydrate of ticagrelor and preparation method thereof

A technology of ticagrelor and monohydrate, which is applied in the field of preparation of pharmaceutical compounds and achieves the effects of rapid dissolution, high bioavailability and high dissolution rate

Active Publication Date: 2017-02-15
FUJIAN COSUNTER PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the existing patent CN1247583 discloses the preparation method of various crystal forms of ticagrelor compound, it only illustrates the crystal form of the compound and does not involve the research on the hydrate crystal form

Method used

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  • Hydrate of ticagrelor and preparation method thereof
  • Hydrate of ticagrelor and preparation method thereof
  • Hydrate of ticagrelor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] The preparation of embodiment 1 ticagrelor monohydrate

[0065] Add 1.0g of ticagrelor to 2.0ml of acetone, then add 1.0ml of purified water, and stir the suspension for 5 minutes. Dissolve the suspension in a water bath at 30-40°C and place it under normal pressure at 15-40°C. Slowly volatilized at 20°C, crystallized for 16 hours, then separated and dried under reduced pressure to obtain about 0.95 g of white crystals. The moisture content of the obtained product is: 3.3% (the theoretical moisture content of ticagrelor monohydrate is 3.3%), and the purity is 99.7%.

Embodiment 2

[0066] Embodiment 2 Preparation of ticagrelor monohydrate

[0067] Add 1.0g of ticagrelor to 2.0ml of absolute ethanol, then add 1.0ml of purified water, and stir the suspension for 5 minutes. Dissolve the suspension in a water bath at 30-40°C and place it under reduced pressure. Slowly volatilize at 15-20°C, crystallize for 16 hours, then separate and dry under reduced pressure to obtain about 0.96 g of white crystals. The moisture content of the obtained product is: 3.4% (the theoretical moisture value of ticagrelor monohydrate is 3.3%), and the purity is 99.8%.

Embodiment 3

[0068] The preparation of embodiment 3 ticagrelor dihydrate

[0069] Add 1.0g of ticagrelor to 2.0ml of 2-butanone, then add 2.0ml of purified water, and stir the suspension for 10 minutes. Dissolve the suspension in a water bath at 30-40°C and place it under reduced pressure. Slowly volatilize at 15-20°C, crystallize for 18 hours, then separate and dry under reduced pressure to obtain about 0.92 g of white crystals. The moisture content of the obtained product is: 6.4% (the theoretical moisture content of ticagrelor dihydrate is 6.4%), and the purity is 99.6%.

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Abstract

The invention relates to ticagrelor hydrates and a preparation method thereof. The ticagrelor hydrates refer to monohydrate and dihydrate. In an X-ray powder diffraction pattern of the monohydrate, characteristic absorption peaks appear at diffraction angles (2 theta) of 6.574, 7.901, 12.188, 13.503, 18.362, 19.201, 19.868 and 25.101. In an X-ray powder diffraction pattern of the dihydrate, characteristic absorption peaks appear at diffraction angles (2 theta) of 9.796, 12.201, 17.910, 18.547, 19.210, 21.209, 23.288 and 24.065. The invention further provides a preparation method and application of the monohydrate and the dihydrate. The ticagrelor hydrates are good in crystal form stability and high in dissolution rate; the preparation process is simple and can be put into industrial production easily.

Description

technical field [0001] The invention belongs to the field of preparation of pharmaceutical compounds, and in particular relates to ticagrelor monohydrate and dihydrate and a preparation method thereof. Background technique [0002] Ticagrelor, English name: Ticagrelor, belongs to cyclopentyl triazolopyrimidine compounds, chemical name is (1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3 ,4-Dichlorophenyl)cyclopropylamino]-5-(thiopropyl)-3H-[1,2,3]triazol[4,5-d]pyrimidin-3-yl]-5-(2 -Hydroxyethoxy)cyclopentane-1,2-diol, molecular formula: C 23 h 28 f 2 N 6 o 4 S, molecular weight: 522.57, chemical structural formula is the following formula (I): [0003] [0004] Ticagrelor is a platelet inhibitor developed by AstraZeneca. It is mainly used to reduce the occurrence of thrombotic events in patients with ACS (platelet aggregation in acute coronary syndrome, acute coronary syndrome, ACS). It was released in July 2011 by Approved by the US FDA for marketing. Ticagrelor reversibly acts o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04
CPCC07B2200/13C07D487/04
Inventor 周义鑫陈仕魁林伟张东姚建堤张旭周巧云熊莉
Owner FUJIAN COSUNTER PHARMA CO LTD