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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  • 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

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[0054] Example 1

[0055] Preparation method of berberine hydrochloride and caffeic acid co-crystal 1:

[0056] According to the following table, take appropriate amount of berberine hydrochloride and caffeic acid into a mortar at a molar ratio of 2:1, add an appropriate amount of organic solvent, and manually grind for an appropriate time. It was analyzed by powder X-ray diffraction, and its diffraction pattern was similar to figure 1 Consistent, indicating that the obtained sample is a co-crystal of berberine hydrochloride and caffeic acid.

[0057]

[0058]

[0059] Preparation method of co-crystal of berberine hydrochloride and caffeic acid 2:

[0060] According to the following table, take appropriate amount of berberine hydrochloride and caffeic acid into a ball milling 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. It was analyzed by powder X-...

Example Embodiment

[0065] Example 2

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

[0067] High temperature test: Put the samples of berberine hydrochloride, berberine hydrochloride and caffeic acid eutectic product in an open clean watch glass, place them at 60℃ for 10 days, and take samples on the 0th, 5th and 10th days . The powder X-ray diffraction analysis of the samples obtained from the above sampling points showed that the berberine hydrochloride and the co-crystal of berberine hydrochloride and caffeic acid were stable under the high temperature influence factor test.

[0068] High humidity test: Put the eutectic substance of berberine hydrochloride and berberine hydrochloride and caffeic acid in an open clean watch glass, and place it at 25°C under the conditions of 90%±5% relative humidity for 10 days, and on day 0 , 5th day and 10th day sampling. The powder X-ray diffraction analysis of the samples obtained from the above sampling points sh...

Example Embodiment

[0071] Example 3

[0072] The solubility characteristics of the co-crystal of berberine hydrochloride and caffeic acid and berberine hydrochloride raw materials in four solvent systems: the choice of solvent system: ①refer to the solvent system used in the dissolution test method in the appendix of the Pharmacopoeia; ②reference The pH value of the digestive juice of different organs in the organism; 4 solvent systems are set up according to the above 2 reference basis: 0.1N hydrochloric acid solution with pH 1.0; acetate buffer with pH 4.5; phosphoric acid with pH 6.8 Salt buffer; aqueous solution. Refer to the "Technical Guidelines for Dissolution Tests for Oral Solid Preparations", the dissolution curve comparison adopts the model-independent similarity factor (f2) method, and the calculation of the f2 value compares the co-crystal of berberine hydrochloride and berberine hydrochloride with caffeic acid The similarity of the dissolution curves of the sample in the four solvent...

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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
CPCC07D455/03C07C59/52A61P9/00A61P3/06A61P35/00A61P29/00A61P3/10A61P31/12A61P31/04C07C2601/16C07B2200/13
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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