Cocrystal of berberine hydrochloride and fumaric acid, preparation method, composition and use thereof

A technology of fumaric acid and berberine hydrochloride, which is applied in the directions of drug combination, separation/purification of carboxylic acid compounds, and pharmaceutical formulations, etc., to achieve the effect of good safety and the advantages of finished medicines

Active Publication Date: 2022-04-15
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no report about berberine hydrochloride co-crystal

Method used

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  • Cocrystal of berberine hydrochloride and fumaric acid, preparation method, composition and use thereof
  • Cocrystal of berberine hydrochloride and fumaric acid, preparation method, composition and use thereof
  • Cocrystal of berberine hydrochloride and fumaric acid, preparation method, composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Preparation method 1 of berberine hydrochloride and fumaric acid cocrystal:

[0061] According to the table below, take an appropriate amount of berberine hydrochloride and fumaric acid and put them into a mortar according to the molar ratio of 2:1, add an appropriate amount of organic solvent, and manually grind for an appropriate time. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and image 3 Consistent, indicating that the obtained sample is a cocrystal of berberine hydrochloride and fumaric acid.

[0062]

[0063] Preparation method 2 of berberine hydrochloride and fumaric acid cocrystal:

[0064] As shown in the table below, take an appropriate amount of berberine hydrochloride and fumaric acid and put them into a ball mill tank at a molar ratio of 2:1, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate speed, and grind for an appropriate time . Carry out powder X-ray di...

Embodiment 2

[0070] Stability characteristics of berberine hydrochloride and fumaric acid cocrystal:

[0071] High temperature test: Put the samples of berberine hydrochloride and berberine hydrochloride and fumaric acid eutectic in an open clean watch glass, place them at 60°C for 10 days, and test them on the 0th day, the 5th day and the second day 10 days for sampling. Powder X-ray diffraction analysis was carried out on the samples obtained at the above sampling points, and the results showed that berberine hydrochloride and berberine hydrochloride and fumaric acid eutectic were stable under the high temperature influence factor test.

[0072] High humidity test: Put the samples of berberine hydrochloride and berberine hydrochloride and fumaric acid eutectic in an open clean watch glass, place them at 25°C for 10 days at a relative humidity of 90%±5%, and then Samples were taken on days 0, 5 and 10. The powder X-ray diffraction analysis of the samples obtained at the above sampling p...

Embodiment 3

[0076] Solubility characteristics of berberine hydrochloride and fumaric acid co-crystal and berberine hydrochloride API in four solvent systems: selection of solvent system: ①Refer to the solvent system used in the dissolution method in the appendix of the Pharmacopoeia; ② Refer to the pH value of the digestive juice of different organs in the organism; set up 4 solvent systems according to the above two references: 0.1N hydrochloric acid solution with a pH value of 1.0; acetate buffer solution with a pH value of 4.5; pH value of 6.8 phosphate buffered saline; aqueous solution. With reference to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" for determination, the dissolution curve comparison adopts the model-independent similarity factor (f2) method, and the calculation of f2 value compares the berberine hydrochloride and its fumaric acid eutectic samples in The similarity of the dissolution curves in the four solvent systems, when the f2...

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Abstract

The invention discloses a cocrystal of berberine hydrochloride and fumaric acid, a preparation method, a composition and an application thereof. Specifically, the invention discloses a new co-crystal of berberine hydrochloride and fumaric acid, which uses berberine hydrochloride as the active ingredient and fumaric acid as the co-crystal precursor; berberine hydrochloride Preparation method of fumaric acid co-crystal; berberine hydrochloride and fumaric acid co-crystal are used as pharmaceutical active ingredients in the preparation and prevention of cardiovascular disease, anti-virus, anti-cancer, lowering blood fat, lowering blood sugar, anti-aging Inflammation, antibacterial and anti-infective drugs.

Description

technical field [0001] The invention discloses a cocrystal of berberine hydrochloride and fumaric acid, a preparation method, a composition and an application thereof. Specifically, the invention discloses a cocrystal formed by berberine hydrochloride and fumaric acid; a preparation method for the cocrystal of berberine hydrochloride and fumaric acid; The application of the olefinic acid co-crystal as an active ingredient in the preparation of cardiovascular disease prevention, anti-virus, anti-cancer, blood fat-lowering, blood-sugar-lowering, anti-inflammatory, anti-bacterial and anti-infective drugs. Background technique [0002] Drug co-crystal refers to the crystal formed by the intermolecular non-covalent interaction force between the active drug molecule and the co-crystal ligand in a certain ratio. By forming co-crystals, drugs can improve their physical and chemical properties and improve clinical therapeutic effects on the one hand, and on the other hand, co-crysta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03C07C51/43C07C57/15A61K31/4375A61P9/00A61P31/12A61P35/00A61P3/06A61P3/10A61P29/00A61P31/04
CPCC07D455/03
Inventor 吕扬杜冠华曹俊姿杨世颖
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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