Berberine hydrochloride pharmaceutical co-crystal as well as preparation method and application thereof

A technology of berberine hydrochloride and medicine, which is applied in the field of berberine hydrochloride drug co-crystal and its preparation, can solve problems such as poor treatment effect, achieve large commercial application value, realize large-scale industrial production, and have low production cost Effect

Pending Publication Date: 2022-01-21
SHANGHAI UNIV OF ENG SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, the dissolution rate and dissolution rate are important indicators of the performance of the raw material drug in the body. The drug must be disintegrated and dissolved before it can be absorbed by the human body. If the drug concentration is lower than its effective concentration, the therapeutic effect will be poor.

Method used

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  • Berberine hydrochloride pharmaceutical co-crystal as well as preparation method and application thereof
  • Berberine hydrochloride pharmaceutical co-crystal as well as preparation method and application thereof
  • Berberine hydrochloride pharmaceutical co-crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Add berberine hydrochloride (100mg) and 4-aminobenzoic acid with a molar ratio of 1:1 into methanol, ultrasonicate, heat to 40°C, the solution is clear, continue ultrasonication for a period of time, take it out and let it stand at room temperature for 48 hours After the precipitation is complete, filter and dry to obtain light yellow solid powder, which is berberine hydrochloride-4-aminobenzoic acid eutectic; wherein, the total mass g of berberine hydrochloride and 4-aminobenzoic acid and the volume of methanol The ml ratio is 1:50–100.

Embodiment 2

[0059] Add berberine hydrochloride (100mg) and 4-aminobenzoic acid with a molar ratio of 1:1 into ethanol, ultrasonicate, heat to 50°C, the solution is clear, continue ultrasonication for 10min, take it out and let it stand at room temperature for 48h to precipitate After complete filtration and drying, a light yellow solid powder is obtained, which is the co-crystal of berberine hydrochloride-4-aminobenzidine; wherein, the total mass g of berberine hydrochloride and 4-aminobenzidine and the volume ml of ethanol The ratio is 1:100–150.

Embodiment 3

[0061] Add berberine hydrochloride (100mg) and 4-aminobenzoic acid with a molar ratio of 1:1 into isopropanol, ultrasonicate, heat to 60°C, the solution is clear, continue ultrasonication for 10min, take it out and let it stand at room temperature, After 72 hours of complete precipitation, filter and dry to obtain light yellow solid powder, which is berberine hydrochloride-4-aminobenzoic acid eutectic; wherein, the total mass g of berberine hydrochloride and 4-aminobenzoic acid and isopropyl The volume ml ratio of alcohol is 1:150–200.

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Abstract

The invention discloses a berberine hydrochloride pharmaceutical co-crystal as well as a preparation method and application thereof, which belongs to the technical field of organic pharmaceutical co-crystals. The berberine hydrochloride pharmaceutical co-crystal is a berberine hydrochloride-aromatic acid co-crystal which takes berberine hydrochloride as an active pharmaceutical molecule and takes aromatic acid as a co-crystal former to form a basic structural unit, and the berberine hydrochloride-aromatic acid co-crystal is obtained by dissolving berberine hydrochloride and aromatic acid in a solvent, cooling, standing and crystallizing. The aromatic acid is 4-aminobenzoic acid or 4-hydroxybenzoic acid, and the formed berberine hydrochloride-4-aminobenzoic acid co-crystal is a monoclinic system and has a P-21 / C space group; the berberine hydrochloride-4-hydroxybenzoic acid co-crystal is a triclinic crystal system and has a P-1 space group. The powder dissolution rate and the inherent dissolution rate of berberine hydrochloride are improved by forming the pharmaceutical co-crystal, the stability is improved while the hygroscopicity is reduced, the bioavailability of berberine hydrochloride is improved, the curative effect is fully exerted, the preparation condition is mild, the reproducibility is good, and large-scale production is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and relates to a berberine hydrochloride drug co-crystal and a preparation method and application thereof. Background technique [0002] Drug co-crystal refers to the co-crystal formed by the interaction of active drug molecules (API) and co-crystal formers (CCF) according to a fixed stoichiometric ratio through the interaction of non-covalent bonds and non-ionic bonds. The physical and chemical properties of insoluble drugs will not change the structure of the active drug molecules, and the methods for preparing drug co-crystals in the prior art, such as solvent evaporation, grinding, supercritical fluid technology, etc., are formed due to different preparation techniques. The product form is also different. The formation of drug co-crystals can effectively improve the physicochemical properties of drugs, and the development cycle will be greatly shortened compared with new che...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C51/43C07C65/03C07C227/42C07C229/60A61K31/4375A61P31/04A61K47/12A61K47/18
CPCC07D455/03C07C51/43C07C65/03C07C227/42C07C229/60A61K31/4375A61P31/04A61K47/12A61K47/183C07B2200/13Y02A50/30
Inventor 刘书妤高紫尧
Owner SHANGHAI UNIV OF ENG SCI
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