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Naringenin isonicotinamide co-crystal

A technology of isonicotinamide and naringenin, applied in the field of medicine, can solve the problems of limited clinical application, poor solubility, low oral absorption bioavailability, etc.

Inactive Publication Date: 2015-08-05
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Naringenin is the aglycone of naringin, which belongs to dihydroflavonoids. It has antibacterial, anti-inflammatory, free radical scavenging, anti-oxidation, cough and expectorant, blood lipid lowering, anti-cancer and anti-tumor, antispasmodic and choleretic, preventive It can be widely used in medicine, food and other fields, and has great development value, but because naringenin is almost insoluble in water, its solubility is poor Lead to extremely low oral absorption bioavailability, which greatly limits clinical application

Method used

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  • Naringenin isonicotinamide co-crystal
  • Naringenin isonicotinamide co-crystal
  • Naringenin isonicotinamide co-crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Take 250.5 mg of naringenin and 224.6 mg of isonicotinamide into a beaker, add 5ml of ethanol, stir at room temperature for 12 hours, filter the resulting suspension, and dry the product in a vacuum oven to obtain the co-product of naringenin and isonicotinamide 427.2mg.

Embodiment 2

[0060] Take 500.2 mg of naringenin and 450.6 mg of isonicotinamide into a beaker, add 10 ml of methanol, stir at room temperature for 12 hours, filter the resulting suspension, and dry the product in a vacuum oven to obtain naringenin and isonicotinamide eutectic 846.2mg.

Embodiment 3

[0062]Take 252.2mg of naringenin and 226.2mg of isonicotinamide into a beaker, add 50ml of ethyl acetate, stir and dissolve at room temperature, evaporate at room temperature, and dry the product in a vacuum oven to obtain 455.7mg of naringenin-isonicotinamide co-crystal.

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Abstract

The invention belongs to the field of a medical technology and specifically relates to a co-crystal formed by naringenin and isonicotinamide, wherein stoichiometric ratio of naringenin to isonicotinamide in the co-crystal is 1:2. The co-crystal has an X-ray powder diffraction pattern, a differential scanning calorimetry pattern and an infrared spectrogram which are different from those of naringenin crystals and a physical mixture of naringenin and isonicotinamide, is a novel crystalline form completely different from naringenin, and has remarkably-enhanced solubility.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-crystal of naringenin-isonicotinamide and a preparation method thereof. Background technique [0002] For pharmaceutical active ingredients, different crystalline forms have different physical and chemical properties, such as melting point, solubility, dissolution rate, stability, etc. Studies have shown that drug co-crystals can use the functional groups contained in drug molecules that can form intermolecular forces to combine active pharmaceutical ingredients and suitable co-crystal formers through hydrogen bonds or other non-covalent bond forces to form API-CCF super Molecular complexes, which can effectively improve the physical and chemical properties and efficacy of the drug itself, are a new option for solid pharmaceutical preparations. Since the formation of pharmaceutical co-crystals does not destroy the covalent bonds of active ingredients of pharmac...

Claims

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Application Information

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IPC IPC(8): C07D311/32C07D213/81
CPCC07D311/32C07D213/81
Inventor 张建军夏典蓉许姣姣高缘
Owner CHINA PHARM UNIV
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