Berberine hydrochloride eutectic crystal and preparation method thereof

A technology of berberine hydrochloride and diacid, applied in the field of four berberine hydrochloride co-crystals and their preparation, berberine hydrochloride co-crystals and their preparation, can solve problems such as poor therapeutic effect

Active Publication Date: 2021-03-19
SHANGHAI UNIV OF ENG SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug needs to be disintegrated and dissolved before it can be absorbed by the human body. If the drug concentration is lower than its effective concentration, it will lead to poor therapeutic effect
In the market, more than 80% of drugs are sold in the form of tablets, and water-soluble drugs account for about 40%. Due to this shortcoming, the candidate drugs that were eliminated during the drug development stage reached 90%

Method used

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  • Berberine hydrochloride eutectic crystal and preparation method thereof
  • Berberine hydrochloride eutectic crystal and preparation method thereof
  • Berberine hydrochloride eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Add berberine hydrochloride and succinic acid with a molar ratio of 2:1 to methanol, ultrasonically heat to 40°C, the solution is clear, continue ultrasonication for 10min, take it out and let it stand at room temperature, wait for 48h for complete precipitation, filter and dry Dry to obtain light yellow solid powder, which is berberine hydrochloride-succinic acid eutectic; wherein, the mass volume ratio of the total mass of berberine hydrochloride and succinic acid to methanol is 1:30g / ml.

Embodiment 2

[0092] Add berberine hydrochloride and succinic acid at a molar ratio of 2:1 to 10 mL of ethanol, ultrasonicate, heat to 50°C, the solution is clear, continue ultrasonication for 10 min, take it out and let it stand at room temperature, wait for 48 hours for complete precipitation, filter, After drying, a pale yellow solid powder is obtained, which is a berberine hydrochloride-succinic acid cocrystal; wherein, the mass volume ratio of the total mass of berberine hydrochloride and succinic acid to ethanol is 1:40g / ml.

Embodiment 3

[0094] Add berberine hydrochloride and succinic acid with a molar ratio of 2:1 to isopropanol, ultrasonically heat to 60°C, the solution is clear, continue ultrasonication for 10 minutes, take it out and let it stand at room temperature, wait for 72 hours for complete precipitation and then filter , drying, to obtain light yellow solid powder, berberine hydrochloride-succinic acid eutectic; Wherein, the mass volume ratio of the total mass of berberine hydrochloride and succinic acid and isopropanol is 1:10g / ml.

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Abstract

The invention relates to a berberine hydrochloride eutectic crystal and a preparation method thereof. The method comprises the steps that: berberine hydrochloride and diacid are dissolved in a solvent, then cooling crystallization or standing crystallization is adopted, and a separated crystal is the berberine hydrochloride eutectic crystal; the berberine hydrochloride eutectic crystal is a berberine hydrochloride-diacid eutectic crystal of a basic structural unit formed by taking the berberine hydrochloride as an API and the diacid as a CCF; and the berberine hydrochloride-diacid eutectic crystal is a triclinic system and a P1 space group. According to the berberine hydrochloride eutectic crystal and the preparation method thereof of the invention, by means of the eutectic crystal mode, the powder dissolution rate and the inherent dissolution rate of the berberine hydrochloride are improved, and the hygroscopicity of the berberine hydrochloride is reduced, the berberine hydrochloridehas better stability, the bioavailability of the berberine hydrochloride can be greatly improved, and the curative effect of the berberine hydrochloride can be better exerted. In addition, the preparation method of the eutectic crystal is simple and easy to implement, mild in condition, easy to control, good in reproducibility and low in production cost, and has a great commercial application value; and the large-scale industrial production of the eutectic crystal is easy to achieve.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and relates to a berberine hydrochloride co-crystal and a preparation method thereof, in particular to four berberine hydrochloride co-crystals and a preparation method thereof. Background technique [0002] According to statistics, 90% of pharmaceutical active ingredients (API) belong to BCS II drugs (high permeability, low solubility), which is a great challenge in the pharmaceutical industry, which is limited due to their unsatisfactory solubility and dissolution rate. In order to change the physical and chemical properties of API, many preparation methods are applied, such as polymorphism, salt, solvate and amorphous, etc., which can well adjust the performance of API and play a certain role in improving oral bioavailability . Among them, drug co-crystallization is a potential method to change the physicochemical properties (such as solubility, dissolution rate, bioavailabil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07C55/10C07C55/12C07C55/14C07C55/16C07C51/43
CPCC07D455/03C07C55/10C07C55/12C07C55/14C07C55/16C07C51/43C07B2200/13
Inventor 刘书妤王礼丽
Owner SHANGHAI UNIV OF ENG SCI
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