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Berberine hydrochloride caffeic acid eutectic compound, preparation method thereof, composition of berberine hydrochloride caffeic acid eutectic compound, and applications

A technology of berberine hydrochloride and caffeic acid, which is applied in the directions of drug combination, separation/purification of carboxylic acid compounds, organic chemical methods, etc.

Pending Publication Date: 2019-07-26
INST OF MATERIA MEDICA AN INST OF THE 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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  • Berberine hydrochloride caffeic acid eutectic compound, preparation method thereof, composition of berberine hydrochloride caffeic acid eutectic compound, and applications
  • Berberine hydrochloride caffeic acid eutectic compound, preparation method thereof, composition of berberine hydrochloride caffeic acid eutectic compound, and applications
  • Berberine hydrochloride caffeic acid eutectic compound, preparation method thereof, composition of berberine hydrochloride caffeic acid eutectic compound, and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Preparation method 1 of berberine hydrochloride and caffeic acid cocrystal:

[0056] According to the table below, take an appropriate amount of berberine hydrochloride and caffeic acid and put them into a mortar with a 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 figure 1 Consistent, indicating that the obtained sample is a co-crystal of berberine hydrochloride and caffeic acid.

[0057]

[0058]

[0059] Preparation method 2 of berberine hydrochloride and caffeic acid cocrystal:

[0060] As shown in the table below, take appropriate amount of berberine hydrochloride and caffeic acid and put them into a ball mill tank with 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

[0066] Stability characteristics of berberine hydrochloride and caffeic acid co-crystal:

[0067] High temperature test: Put the samples of berberine hydrochloride and berberine hydrochloride and caffeic acid eutectic in an open clean watch glass, place them at 60°C for 10 days, and take samples on the 0th day, the 5th day and the 10th day . Powder X-ray diffraction analysis was performed on the samples obtained at the above sampling points, and the results showed that berberine hydrochloride and the eutectic of berberine hydrochloride and caffeic acid were stable under the high temperature influence factor test.

[0068] High-humidity test: put samples of berberine hydrochloride and berberine hydrochloride and caffeic acid eutectic in an open clean surface dish, and place them at 25°C for 10 days at a relative humidity of 90%±5%, and on the 0th day , Sampling on the 5th and 10th day. Powder X-ray diffraction analysis was performed on the samples obtained at the above sampli...

Embodiment 3

[0072] Solubility characteristics of berberine hydrochloride and caffeic acid co-crystal and berberine hydrochloride API in four solvent systems: selection of solvent system: ① refer 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; according to the above two references, four solvent systems were set up: 0.1N hydrochloric acid solution with a pH value of 1.0; acetate buffer solution with a pH value of 4.5; phosphoric acid with a pH value of 6.8 Saline buffer; aqueous solution. Refer to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" for determination, the model-independent similarity factor (f2) method is used for the comparison of dissolution curves, and the comparison of berberine hydrochloride and berberine hydrochloride and caffeic acid eutectic is carried out through the calculation of f2 value The similarity of t...

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Abstract

The invention discloses a berberine hydrochloride caffeic acid eutectic compound, a preparation method thereof, a composition of the berberine hydrochloride caffeic acid eutectic compound, and applications, and more specifically, discloses a novel berberine hydrochloride caffeic acid eutectic compound taking berberine hydrochloride as a medicinal active component and caffeic acid as an eutectic precursor, a preparation method of the berberine hydrochloride caffeic acid eutectic compound, and applications of the berberine hydrochloride caffeic acid eutectic compound as a medicinal active component in preparation of medicines used for preventing and treating cardiovascular diseases, preventing virus, treating cancers, reducing blood fat, reducing blood sugar, preventing inflammation, preventing bacteria, and preventing infection.

Description

technical field [0001] The invention discloses a co-crystal of berberine hydrochloride and caffeic acid, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a co-crystal formed by berberine hydrochloride and caffeic acid; a method for preparing the co-crystal of berberine hydrochloride and caffeic acid; The application of the components in the preparation of anti-cardiovascular disease, anti-virus, anti-cancer, hypolipidemic, hypoglycemic, anti-inflammatory, antibacterial 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-crystals can enrich their crystalline forms. For chemi...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C59/52C07C51/43A61K31/4375A61P9/00A61P3/06A61P35/00A61P29/00A61P3/10A61P31/12A61P31/04
CPCC07D455/03C07C59/52A61P9/00A61P3/06A61P35/00A61P29/00A61P3/10A61P31/12A61P31/04C07C2601/16C07B2200/13Y02A50/30
Inventor 吕扬杜冠华曹俊姿杨世颖
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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