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Ticagrelor pharmaceutical cocrystals and preparation methods thereof

A technology of ticagrelor and drugs, applied in the field of preparation of new ticagrelor organic drug co-crystals and drug co-crystals

Active Publication Date: 2014-02-26
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this stage, foreign research on drug co-crystals has gradually increased and deepened; while domestic research on it is still relatively small

Method used

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  • Ticagrelor pharmaceutical cocrystals and preparation methods thereof
  • Ticagrelor pharmaceutical cocrystals and preparation methods thereof
  • Ticagrelor pharmaceutical cocrystals and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1: Add 0.3g of ticagrelor and 0.07g of nicotinamide into a solution of 5ml of ethyl acetate, heat to reflux at 75°C, stir to dissolve, then cool down naturally, and slowly precipitate white crystals after reaching room temperature, 48 After 1 hour, it was filtered to obtain the white organic drug cocrystal 1 of ticagrelor.

Embodiment 2

[0070] Example 2: Add 0.6g and 0.14g of ticagrelor and nicotinamide to 15ml of ethyl acetate solution, heat to 40°C, stir and dissolve, then place at room temperature, slowly crystallize, and obtain white Organic pharmaceutical cocrystal of ticagrelor 1.

Embodiment 3

[0071] Example 3: Dissolve 1.5g of ticagrelor and 0.21g of nicotinamide in a mixed solvent of 10ml of acetone and ethyl acetate (volume ratio of acetone and ethyl acetate (mL / mL=1:4)), and heat to Reflux at 50°C, stir to dissolve, and when the solution is clear, stop heating, cool down naturally, and slowly crystallize to obtain ticagrelor organic drug co-crystal 1.

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical cocrystals, specifically to two ticagrelor pharmaceutical cocrystals and preparation methods thereof. The pharmaceutical cocrystals use ticagrelor as an active pharmaceutical ingredient (API) and nicotinamide as a precursor, ticagrelor is connected with nicotinamide through a hydrogen bond and is in a ratio (mol ratio) of 1 1. In preparation of the pharmaceutical cocrystals, ester and ketone are preferred solvents, and an adopted crystallization method is a cooling crystallization method or solvent evaporation method. The cocrystals prepared in the invention inherit pharmacological activity of ticagrelor and have substantial improved dissolvability, stability and the like compared with ticagrelor.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to two novel organic drug co-crystals of ticagrelor and a preparation method of the drug co-crystals. Background technique [0002] Drug co-crystals are based on the principle of supramolecular chemistry, that is, molecular recognition and supramolecular self-assembly through intermolecular synergy. The active pharmaceutical ingredient (API) self-assembles with a suitable cocrystal former (CCF) through hydrogen bonds, or non-covalent bonds with saturation and directionality (such as van der Waals forces of aromatic hydrocarbons or benzene rings, π- π conjugation and halogen bonds) to form a new structure, namely drug co-crystal. It is based on hydrogen bonds, and neither needs to form new covalent bonds nor destroy existing covalent bonds. While retaining the pharmacological effects of the drug itself, it can also modify the physical and chemical proper...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D213/82A61K31/519A61P7/02
CPCC07D213/82C07D487/04
Inventor 胡秀荣吴佳佳吴素香汤谷平
Owner ZHEJIANG UNIV
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