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A kind of preparation method of lenalidomide and nicotinamide co-crystal

A technology of lenalidomide and nicotinamide is applied in the field of preparation of co-crystals of lenalidomide and nicotinamide, which can solve the problems that the lifting effect is not high enough, and the medicinal requirements of lenalidomide cannot be well satisfied, and achieves the High solubility and dissolution rate, improved bioavailability and efficacy, and good stability

Active Publication Date: 2018-10-26
SHANGHAI UNIV OF ENG SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, at present, the lenalidomide-nicotinamide co-crystal is prepared by grinding method, although the prepared lenalidomide-nicotinamide co-crystal can improve the solubility and bioavailability of lenalidomide to a certain extent, but The lifting effect is not high enough to meet the medicinal requirements of lenalidomide

Method used

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  • A kind of preparation method of lenalidomide and nicotinamide co-crystal
  • A kind of preparation method of lenalidomide and nicotinamide co-crystal
  • A kind of preparation method of lenalidomide and nicotinamide co-crystal

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh 1112.7mg (4.3mmol) of lenalidomide and 522.4mg (4.3mmol) of nicotinamide into a crystallizer, add 50mL of methanol, mix and stir to form a suspension; keep stirring at 20°C for 3h; filter, filter The obtained solid was dried at room temperature (at a temperature of 25° C.) to obtain the co-crystal of lenalidomide and nicotinamide.

[0045] The crystal structure of the obtained co-crystal was determined by using an APEX II CCD X-ray single crystal diffractometer. The test results showed that the obtained crystal was a triclinic system with a P-1 space group and unit cell parameters: unit cell volume Z=2, molecular formula: C19H19N5O4;

[0046] The crystallographic parameters are specifically shown in Table 1:

[0047] Table 1

[0048]

[0049]

[0050] According to the measured data, draw the structural diagram of the cocrystal of lenalidomide and nicotinamide, as figure 1 shown.

[0051] figure 1Schematic diagram of the structure of the obtained eu...

Embodiment 2

[0057] Weigh 2014.1mg (7.8mmol) of lenalidomide and 948.7mg (7.8mmol) of nicotinamide into a crystallizer, add 50mL of methanol, mix and stir to form a suspension; keep stirring at 30°C for 2.5h; filter, The solid obtained by filtration was dried at room temperature (temperature was 25° C.) to obtain the co-crystal of lenalidomide and nicotinamide.

[0058] After determination and analysis, the resulting solid product has figure 1 The structural schematic features shown, figure 2 The PXRD spectrum shown, image 3 The characteristics of the DSC spectrum shown and Figure 4 The characteristics of the infrared spectrum shown in this example indicate that the solid product obtained in this example is also the co-crystal of lenalidomide and nicotinamide of the present invention.

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Abstract

A preparing method of a lenalidomide-nicotinamide eutectic composition is disclosed. The lenalidomide-nicotinamide eutectic composition adopts lenalidomide as a medicine active component, adopts nicotinamide as an eutectic forming component, and is prepared by mixing the lenalidomide and the nicotinamide according to a ratio into an organic solvent, stirring and reacting through adopting a slurry crystallization process. The lenalidomide-nicotinamide eutectic composition prepared by the slurry crystallization process has better stability, higher solubility and a higher dissolution rate than lenalidomide-nicotinamide eutectic compositions prepared through conventional grinding methods, and is hoped to improve bioavailability and medicine effects of the lenalidomide and to meet medicinal requirements of the lenalidomide.

Description

technical field [0001] The invention relates to a method for preparing co-crystals of lenalidomide and nicotinamide, belonging to the technical field of co-crystals of organic medicines. Background technique [0002] The pharmaceutical industry occupies an important position in the national economy. It is reported that many drugs pass clinical trials and go on the market every year. Lenalidomide (lenalidomide) is a second-generation new immunomodulator used for the treatment of fatal blood diseases and cancer, the trade name is Revlimid, and the chemical name is 3(-4-amino-1,3-dihydro-1-oxy Substitute-2H-isoindol-2-yl)piperidine-2,6-dione, its pKa is 2.77, and its chemical structural formula is as follows: [0003] [0004] However, the solubility of the pharmaceutical crystal form of lenalidomide in water is only 0.23mg / mL (25±0.5°C), which has poor solubility and low bioavailability, which affects its efficacy and greatly limits its clinical application. Therefore, ce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04C07D213/82C07D213/803
CPCC07B2200/13C07D213/803C07D213/82C07D401/04
Inventor 翟晶焕陈真真陆杰
Owner SHANGHAI UNIV OF ENG SCI
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