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, prevent

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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