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A crystalline form of non-hygroscopic protocatechin berberine monohydrate

A technology of protocatechuic acid and monohydrate, which is applied in the field of non-hygroscopic protocatechuic acid berberine monohydrate, can solve the problems of strong bitterness and side effects, high berberine hydrochloride, poor bioavailability, etc. The method is simple and easy to implement, the crystal structure is clear, and the dissolution rate is fast.

Active Publication Date: 2019-03-29
MINJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Berberine hydrochloride has good water solubility, but poor bioavailability, which seriously restricts its clinical application in cardiovascular diseases and anticancer
In addition, the high water solubility of berberine hydrochloride also causes a strong bitter taste and side effects
At present, there is no public report on the crystalline form of berberine and protocatechuic acid organic salt monohydrate

Method used

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  • A crystalline form of non-hygroscopic protocatechin berberine monohydrate
  • A crystalline form of non-hygroscopic protocatechin berberine monohydrate
  • A crystalline form of non-hygroscopic protocatechin berberine monohydrate

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Embodiment

[0029] Dissolve 1.86 g of berberine hydrochloride, 0.77 g of protocatechuic acid and 0.2 g of sodium hydroxide in 50 mL of 95 vt% ethanol solution under heating conditions at 60 °C, stir for 1 hour, and cool to obtain a large amount of yellow precipitate, which is filtered by suction , the resulting precipitate was washed with 95vt% ethanol and dried in the air; the resulting powder was recrystallized in absolute ethanol to obtain berberine protocatechuate monohydrate crystals.

[0030] figure 1 It is the XRD figure of the berberine protocatechuate monohydrate crystal prepared in the present embodiment. Depend on figure 1 It can be seen that the prepared crystals, with a diffraction angle of 2 θ °±0.1 is expressed as: 6.3°, 8.6°, 9.5°, 12.5°, 16.8,° 17.2°, 17.6°,18.2°, 18.9°, 19.1°, 19.5°, 20.5°, 21.9°, 22.9°, 24.1° , 24.5°, 24.9°, 25.5°, 26.2°, 27.8°, 29.0°, 30.7°, 31.0°, 31.7°, 34.8°, 36.9°, 37.9 ° have characteristic diffraction peaks.

[0031] figure 2 It is the h...

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Abstract

The present invention discloses a non-hygroscopicity protocatechuic acid berberine monohydrate having a crystal form, and belongs to the technical field of drug crystallization. According to the present invention, berberine hydrochloride, protocatechuic acid and sodium hydroxide are dissolved in an ethanol aqueous solution according to a certain ratio to form the protocatechuic acid berberine monohydrate crystal; the preparation method has characteristics of simpleness, easy performing, low cost, and high crystal yield; and the prepared protocatechuic acid berberine monohydrate crystal does not have the hygroscopicity, has the moderate solubility in water, can be rapidly dissolved, and can be used in cardiovascular diseases and anti-cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine crystallization, and in particular relates to non-hygroscopic protocatechuic acid berberine monohydrate in crystal form. Background technique [0002] The crystalline form of drug molecules is a key constraint on the efficacy of solid dosage forms. For a specific drug, different crystalline forms such as salt, hydrate, and polymorph determine different pharmaceutical effects, and one crystalline form may be better than another. For example, crystalline salts of basic drugs generally have better solubility, crystallinity, and stability than free bases. Common acids used to form salts are hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, lactic acid, oxalic acid, tartaric acid, p-toluenesulfonic acid, methanesulfonic acid, citric acid, fumaric acid, horse To acid etc. Recently, combining two different drug molecules to form a drug-dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03C07C51/43C07C65/03
CPCC07B2200/13C07D455/03
Inventor 娄本勇张燕杰黄雅丽黄晓东郑国才林棋
Owner MINJIANG UNIV
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