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A preparing method of a lenalidomide-nicotinamide eutectic composition

A technology of lenalidomide and nicotinamide, which is applied in the field of preparation of co-crystals of lenalidomide and nicotinamide, can solve problems such as insufficient enhancement effect and failure to meet the medicinal requirements of lenalidomide, and achieve Large solubility and dissolution rate, improved bioavailability and drug efficacy, and the effect of meeting pharmaceutical requirements

Active Publication Date: 2016-08-10
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 preparing method of a lenalidomide-nicotinamide eutectic composition
  • A preparing method of a lenalidomide-nicotinamide eutectic composition
  • A preparing method of a lenalidomide-nicotinamide eutectic composition

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Experimental program
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Effect test

Embodiment 1

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

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

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

[0047] Table 1

[0048]

[0049]

[0050] According to the measured data, draw the structure diagram of the co-crystal of lenalidomide and nicotinamide, such as figure 1 shown.

[0051] figure 1For the structural schematic diagram of the obtained ...

Embodiment 2

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

[0058] After analysis, the obtained solid product has figure 1 The structural schematic features shown, figure 2 The PXRD spectrum shown, image 3 The DSC spectral characteristics shown and Figure 4 The characteristics of the infrared spectrum shown 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 preparation method of a co-crystal of lenalidomide and nicotinamide, and belongs to the technical field of organic medicine co-crystal. Background technique [0002] The pharmaceutical industry occupies an important position in the national economy, and it is reported that many drugs pass clinical trials and are marketed every year. Lenalidomide is a second-generation new immunomodulatory agent for the treatment of fatal blood diseases and cancer. Its trade name is Revlimid and its chemical name is 3(-4-amino-1,3-dihydro-1-oxygen Substituted-2H-isoindol-2-yl)piperidine-2,6-dione, its pKa is 2.77, and its chemical structure is as follows: [0003] [0004] However, the solubility of the medicinal crystal form of lenalidomide in water is only 0.23 mg / mL (25±0.5°C), with poor solubility and low bioavailability, which affects its efficacy and greatly limits its clinical application. Therefore, certain measures need to be tak...

Claims

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Application Information

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Patent Type & Authority Applications(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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