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Curcumin-2,5-dihydroxy-benzoic acid eutectic crystal and preparation method thereof

A technology of dihydroxybenzoic acid and curcumin, which is applied in the separation/purification of carboxylic acid compounds, separation/purification of carbonyl compounds, organic chemistry, etc., and can solve the problems of potential toxicity, limited drug loading, and increased volume of administration. Major problems, to achieve the effect of protecting the liver

Active Publication Date: 2018-03-23
MEDONCARE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above methods have certain improvements in dissolution or oral absorption, there are still deficiencies: (1) low drug loading, such as microspheres, nanoparticles, solid dispersions, liposomes, etc. require a large amount of carrier materials, and the volume of administration increases. (2) Potential toxicity, such as microemulsion preparations contain a large amount of surfactant; (3) The preparation process may cause curcumin degradation, such as phospholipid complexes need to be mixed with phospholipids at a certain temperature Perform complex reaction and remove solvent

Method used

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  • Curcumin-2,5-dihydroxy-benzoic acid eutectic crystal and preparation method thereof
  • Curcumin-2,5-dihydroxy-benzoic acid eutectic crystal and preparation method thereof
  • Curcumin-2,5-dihydroxy-benzoic acid eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Co-crystals were synthesized by solvent evaporation at room temperature using curcumin and 2,5-dihydroxybenzoic acid:

[0059] The reactants are fed according to the mass ratio of curcumin:2,5-dihydroxybenzoic acid=1:1. Accurately weigh 20.00 mg of curcumin and 20.00 mg of 2,5-dihydroxybenzoic acid with an electronic analytical balance, and put them into a transparent glass vial.

[0060] Dissolution of API:

[0061] Use a pipette gun to accurately pipette 1mL of dichloromethane, 2mL of ether and 1mL of acetone into a glass vial, stir on a magnetic stirrer for 4 hours at 25°C, take out the stirring bar, and add A layer of tin foil increases the airtightness and tightens.

[0062] Solvent room temperature evaporation method:

[0063] Place the glass vial at room temperature, seal it slightly with tin foil to prevent foreign matter from entering the culture solution, let it stand for 30 hours, the solution reaches saturation, and crystals begin to precipitate. With the...

Embodiment 2

[0070] Co-crystals were synthesized by solvent evaporation at room temperature using curcumin and 2,5-dihydroxybenzoic acid:

[0071] The reactants are fed in a mass ratio of curcumin: 2,5-dihydroxybenzoic acid=1:5. Accurately weigh 10.00 mg of curcumin and 50.00 mg of 2,5-dihydroxybenzoic acid with an electronic analytical balance, and put them into a transparent glass vial.

[0072] Dissolution of API:

[0073] Use a pipette gun to accurately pipette 1mL of dichloromethane, 2mL of ether and 1mL of acetone into a glass vial, stir on a magnetic stirrer for 4 hours at 25°C, take out the stirring bar, and add A layer of tin foil increases the airtightness and tightens.

[0074] Solvent room temperature evaporation method:

[0075] Place the glass vial at room temperature, seal it slightly with tin foil to prevent foreign matter from entering the culture solution, let it stand for 30 hours, the solution reaches saturation, and crystals begin to precipitate. With the continuous...

Embodiment 3

[0077] Co-crystals were synthesized by solvent evaporation at room temperature using curcumin and 2,5-dihydroxybenzoic acid:

[0078] The reactants are fed according to the mass ratio of curcumin: 2,5-dihydroxybenzoic acid=1:1. Accurately weigh 20.00 mg of curcumin and 20.00 mg of 2,5-dihydroxybenzoic acid with an electronic analytical balance, and put them into a transparent glass vial.

[0079] Dissolution of API:

[0080] Use a pipette gun to accurately pipette 2mL of dichloromethane, 1mL of ethanol and 1mL of acetone into a glass vial, stir on a magnetic stirrer for 4 hours at 25°C, take out the stirring bar, and add A layer of tin foil increases the airtightness and tightens.

[0081] Solvent room temperature evaporation method:

[0082] Place the glass vial at room temperature, seal it slightly with tin foil to prevent foreign matter from entering the culture solution, let it stand for 30 hours, the solution reaches saturation, and crystals begin to precipitate. With ...

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Abstract

The invention discloses a curcumin-2,5-dihydroxy-benzoic acid eutectic crystal. The curcumin-2,5-dihydroxy-benzoic acid eutectic crystal is an eutectic crystal formed by curcumin and 2,5-dihydroxy-benzoic acid, and is obtained by the steps of self-assembling curcumin and 2,5-dihydroxy-benzoic acid according to the mass ratio of 1:0.5 to 1:5 in a mixed solvent of dichloromethane, ethanol, ethyl ether and acetone, volatilizing and performing crystallization. The invention also provides a preparation method of the eutectic crystal. In the eutectic crystal, the pharmacological activity of the traditional raw material medicines is inherited and the dissolubility and the stability are obviously improved.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a novel curcumin drug co-crystal and a preparation method thereof. Background technique [0002] Traditional crystalline drugs exist in various solid forms, such as polymorphs, hydrates, solvates, amorphous forms, and salts. The curative effect of a drug largely depends on the physical and chemical properties of the drug itself and the selected dosage form, and the different solid forms of the drug have an impact on the solubility, stability, dissolution rate and bioavailability of the drug. [0003] Crystal engineering provides a wider space for the crystal form design of drugs. For example, the concept of supramolecular chemistry is introduced into the crystal design of drug molecules, and new crystal forms with specific physical and chemical properties can be obtained through weak intermolecular forces. crystal. [0004] Drug co-crystals are essentially ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/255C07C65/05C07C45/81C07C51/43
CPCC07C45/81C07C49/255C07C51/43C07C65/05
Inventor 刘晓忠靳奇峰潘蕊郑和校李郡
Owner MEDONCARE PHARMA CO LTD
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