Eutectic of diflunisal and pyridine formamide compounds and preparation method thereof

A technology of pyridinecarboxamide and diflunisal, which is applied in the field of chemical pharmaceuticals, can solve problems in the initial stage and achieve good solubility effects

Inactive Publication Date: 2014-06-18
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, drug crystal form research is relatively mature and valued in the European and American pharmaceutical circles, but it is still in its infancy in the domestic pharmaceutical circles

Method used

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  • Eutectic of diflunisal and pyridine formamide compounds and preparation method thereof
  • Eutectic of diflunisal and pyridine formamide compounds and preparation method thereof
  • Eutectic of diflunisal and pyridine formamide compounds and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0052] Preparation of co-crystals with diflunisal and nicotinamide: the reactant diflunisal and nicotinamide are fed according to the material ratio of 1:1. Accurately weigh 131.0 mg of diflunisal and 63.9 mg of nicotinamide and dissolve them in 2.6 ml and 1.1 ml of ethanol, respectively, and ultrasonicate for 10 min to fully dissolve the two, and then slowly add the ethanol solution of nicotinamide to the two In the ethanol solution of flunisal, mix thoroughly, let it stand for one day, filter, rinse with a small amount of ethanol, and then place the filtered product in a vacuum drying oven at 40°C for one day to dry.

[0053] Figures 1 to 5 They are respectively the X-ray diffraction spectrum and solid-state nuclear magnetic resonance CP-MAS of diflunisal / nicotinamide co-crystal and its bulk drug in Example 1. 13 C spectrum, infrared spectrum and thermogram.

[0054] Depend on Figure 1 to Figure 5 It can be seen that the melting point of diflunisal and nicotinamide co-c...

example 2

[0056] Preparation of co-crystal with diflunisal and nicotinamide: the reactant diflunisal and nicotinamide are fed according to the material ratio of 2:1. Accurately weigh 131.0 mg of diflunisal and 32 mg of nicotinamide and dissolve them in 2.6 ml and 1.1 ml of ethanol, respectively, and ultrasonicate for 10 min. In the ethanol solution of flunisal, mix thoroughly, let it stand for one day, filter, rinse with a small amount of ethanol, and then place the filtered product in a vacuum drying oven at 40°C for one day to dry.

example 3

[0058] Preparation of co-crystal with diflunisal and isonicotine: the reactant diflunisal and isonicotine are fed according to the material ratio of 1:1. Accurately weigh 196.5 mg of diflunisal and 95.8 mg of isonicotine and dissolve them in 2.6 ml and 1.1 ml of ethanol respectively, and ultrasonicate for 10 min to fully dissolve the two, then slowly add the ethanol solution of isonicotine dropwise Put it into the ethanol solution of diflunisal, mix well, let stand for one day, filter, wash with a small amount of ethanol, then place the filtered product in a vacuum drying oven at 40°C, and dry for one day.

[0059] Figures 6 to 10 They are the X-ray diffraction spectrum and the solid-state nuclear magnetic resonance CP-MAS of diflunisal / isonicotine co-crystal and its bulk drug in Example 3 respectively. 13 C spectrum, infrared spectrum, thermogram and dissolution curve in water.

[0060] Depend on Figure 6 to Figure 10 It can be seen that the melting point of diflunisal / i...

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Abstract

The invention belongs to the chemical pharmaceutical technical field and in particular relates to an eutectic medicine of 2 ',4 '- difluoro-4-hydroxyl-3-biphenyl carboxylic acid and pyridine carboxamide compounds and a preparation method thereof. The eutectic medicine prepared in the invention is obviously improved in solubility.

Description

technical field [0001] The application belongs to the technical field of chemical pharmacy, and in particular relates to a co-crystal of diflunisal (2',4'-difluoro-4-hydroxy-3-biphenylcarboxylic acid) and pyridinecarboxamide compounds and a preparation method thereof. Background technique [0002] Drug solubility is one of the important factors affecting drug absorption and bioavailability. Statistics show that in current drug development, 35% - 40% of new drugs have low solubility or poor permeability, which significantly reduces the bioavailability of drugs and seriously affects the effective absorption of active drugs in the human body. Therefore, improving the solubility and bioavailability of poorly soluble drugs is one of the important directions of pharmaceutical research. [0003] At present, there are many methods for solubilizing insoluble drugs. Solid-state dispersion technology, cyclodextrin inclusion technology, liposome technology, micronization technology, et...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C65/105C07C51/43C07D213/82C07D213/81
CPCC07D213/82C07D213/81
Inventor 张海禄汪莲艳邓宗武
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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