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Berberine organic acid salt, berberine organic acid salt inclusion compound and preparation methods thereof

A technology of organic acid salt and berberine, applied in the field of medicine, can solve the problems of low biological activity, low solubility, large dosage, etc.

Inactive Publication Date: 2011-01-05
SHAANXI UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its main disadvantages are two: one is low biological activity and large dosage, the actual clinical dose is as high as 1.2-1.5g / d; the other is low solubility, poor absorption in vivo and low bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Add berberine and purified water 10 to 30 times the weight of berberine into the reaction kettle, heat while stirring, and when the temperature rises to 60°C, add salicylic acid solution with a mass concentration of 1 to 5% into it , the addition amount of salicylic acid solution is 1 to 1.15 times that of berberine according to the molar ratio, then adjust the pH value of the solution to 2.4 to 3.4; Salt precipitation; then, suction filtration to separate the solid from the liquid, and finally rinse the crystals with cold purified water six times the weight of berberine, and dry the filter cake at 60°C to obtain berberine salicylate, with a melting point of 205.7 to 206.5 ℃.

Embodiment 2

[0019] Add berberine and purified water 10 to 30 times heavier than berberine into the reaction kettle, heat while stirring, and when the temperature rises to 50°C, add a succinic acid solution with a mass concentration of 5%, and the addition of the succinic acid solution The molar ratio is 1 to 1.25 times that of berberine, and then the pH value of the solution is adjusted to 2.0 to 5.3; then it is kept at 80°C for 30 minutes; then, the temperature is lowered to 10°C, and berberine succinate is precipitated; then , suction filtration to separate the solid from the liquid, and finally wash the crystals with cold purified water 3 times the weight of berberine, and dry the filter cake at 70°C to obtain berberine succinate with a melting point of 204.5-206.5°C.

Embodiment 3

[0021] Add berberine and purified water 10 to 30 times the weight of berberine into the reaction kettle, heat while stirring, when the temperature rises to 40°C, add a 0.5% cinnamic acid solution, the addition of the cinnamic acid solution The molar ratio is 1 to 1.25 times that of berberine, and then the pH value of the solution is adjusted to 2.3 to 4.9; then it is kept at 70°C for 40 minutes; then, the temperature is lowered to 30°C, and berberine cinnamate is precipitated; then , suction filtration to separate the solid from the liquid, and finally wash the crystals with cold purified water 8 times the weight of berberine, and dry the filter cake at 60°C to obtain berberine cinnamate, with a melting point of 130.7-132.3°C.

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Abstract

The invention provides a berberine organic acid salt, a berberine organic acid salt inclusion compound and preparations method thereof. The berberine organic acid salt consists of an alkali base and a salt ligand, wherein the alkali base is a jamaicin alkali base; the salt ligand is an acid radical of organic acid; the mole ratio of the alkali base to the acid radical of organic acid is 1:1; and the berberine organic acid salt inclusion compound consists of an inclusion base material and the berberine organic acid salt. The method for preparing the berberine organic acid salt comprises the following steps of: neutralizing solution of jamaicin and solution of organic acid into salt; crystallizing the salt; and filtering, leaching and drying the crystallized salt so as to obtain the berberine organic acid salt. The method for preparing the berberine organic acid salt inclusion compound comprises the following steps of: dissolving the inclusion base material; adding the berberine organic acid salt into the dissolved inclusion base material for dissolving and inclusion; cooling and standing reaction liquid to separate coprecipitate out; leaching the coprecipitate with acetone; and drying a filter cake so as to obtain the berberine organic acid salt inclusion compound. The berberine organic acid salt and the berberine organic acid salt inclusion compound provided by the invention have the advantages of high bioactivity, small dosage and high dissolubility. The preparation methods have the advantages of simple process, high product purity, easy operation control, simple equipment and easy realization of industrialized production.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a berberine organic acid salt, an inclusion compound of the berberine organic acid salt and a preparation method thereof. Background technique [0002] Berberine can be divided into berberine base and berberine salt. The so-called berberine is the hydrochloride of berberine. It is a reliable antibacterial and anti-inflammatory drug. The antibacterial ability of Staphylococcus aureus is stronger than that of penicillin, and it is clinically used for enteritis, dysentery and other diseases; in recent years, studies have found that it has pharmacological effects such as lowering blood sugar, lowering blood fat, and antiarrhythmia, making this drug more and more important in the field of medicine , the application prospect is broad. [0003] At present, the raw materials of the berberine preparations used clinically are the hydrochloride or sulfate of berberine, both of which are inorganic s...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C57/44C07C65/10C07C55/10C07C59/265C07C59/245C07C229/24C07C51/41C07C227/18A61K31/4375A61P31/04
Inventor 陈易彬刘艺陈佳希高建邦曹倩陈雯
Owner SHAANXI UNIV OF SCI & TECH
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