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Ticagrelor crystal form and its preparation method and use

A technology of ticagrelor and crystal, which is applied in the field of crystal form of ticagrelor and its preparation, can solve the problems of poor stability and fluidity, difficult to control, etc., and achieve the effect of good thermal stability, good particle shape and high purity

Active Publication Date: 2016-06-01
SOLIPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process of amorphous ticagrelor is usually not easy to control, and compared with the crystalline form, its stability and fluidity are poor, so it is not suitable for direct application in preparations

Method used

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  • Ticagrelor crystal form and its preparation method and use
  • Ticagrelor crystal form and its preparation method and use
  • Ticagrelor crystal form and its preparation method and use

Examples

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Effect test

preparation example 1

[0079] According to the method in WO01 / 92262A1, ticagrelor amorphous form and crystal form I were prepared, specifically as follows:

[0080] a: Take 1 g of ticagrelor, dissolve it in 10 mL of 50% aqueous ethanol by volume, filter, and lyophilize to obtain amorphous ticagrelor.

[0081] b: Take 2 mg of amorphous ticagrelor, and prepare pure crystal form I in DSC according to the following operation: 35°C to 143°C to 35°C to 148°C to 35°C to 148°C to 35°C. Form I seed crystals were obtained.

[0082] c: Take 500 mg of amorphous ticagrelor, add 2.5 mL of methanol and 3.65 mL of water, add the seed crystal obtained in b, and crystallize at 30°C to obtain 340 mg of crystal form I. For the DSC spectrum of Form I, see figure 1 , and its melting onset temperature is about 149.7 °C, which is consistent with literature reports.

Embodiment 1

[0084] Take 184mg of amorphous ticagrelor, add it to 38mL (1:1.25) methanol / water mixed solution to obtain a solid suspension, raise the temperature of the solid suspension to 50°C and stir for 0.5h to dissolve completely, keep it for 2 hours, and then add 5 Cool down to 5°C at a cooling rate of °C / min, filter the resulting magma, wash with water, and dry the filter cake in a vacuum oven at room temperature 25°C for 2 hours to obtain white anhydrous Form V (yield 85%), its XRD pattern is shown in figure 2 , see the DSC spectrum image 3 , PLM map see Figure 4 , the onset temperature of its melting is 163°C, and the peak temperature is 166°C.

Embodiment 2

[0086] Take 240 mg of amorphous ticagrelor, add 72 mL of isopropyl ether solution to obtain a solid suspension, stir the solid suspension at 25 ° C for 3 hours, filter the obtained crystal slurry, wash with isopropyl ether, and place the filter cake in Drying in a vacuum oven at 40°C for 2 hours gave white crystals (yield greater than 95%). The starting temperature of melting of this product was 154°C, and the peak value was 157°C.

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Abstract

The present application discloses a new crystal form of ticagrelor, its preparation method and its use in the preparation of a medicament for reducing arterial thrombosis in patients with acute coronary syndrome.

Description

technical field [0001] This application relates to the technical field of medicinal chemical crystallization. More specifically, the present application relates to the crystal form of ticagrelor and its preparation method and use. Background technique [0002] The chemical name of Ticagrelor is (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)cyclopentane-1,2- Diols, which have the following structural formula: [0003] [0004] Ticagrelor, developed by AstraZeneca, is a selective anticoagulant and the first reversible binding P2Y12 adenosine diphosphate receptor (ADP) antagonist. Ticagrelor can reversibly act on the purine 2 receptor subtype P2Y12 on vascular smooth muscle cells (VSMC), and has obvious inhibitory effect on ADP-induced platelet aggregation, and it takes effect quickly after oral administration, and can effectively improve acute coronary syndrome. Symptoms of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P9/10A61P7/02A61P35/00
CPCC07B2200/13C07D487/04A61P7/02A61P9/10A61P35/00
Inventor 胡晨阳盛晓霞盛晓红
Owner SOLIPHARMA
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