Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Non-hygroscopicity protocatechuic acid berberine monohydrate having crystal form

A kind of technology of protocatechuic acid, monohydrate

Active Publication Date: 2017-09-22
MINJIANG UNIV
View PDF5 Cites 5 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Non-hygroscopicity protocatechuic acid berberine monohydrate having crystal form
  • Non-hygroscopicity protocatechuic acid berberine monohydrate having crystal form
  • Non-hygroscopicity protocatechuic acid berberine monohydrate having crystal form

Examples

Experimental program
Comparison scheme
Effect test

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 crystal, 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 hy...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com