Novel hydroxychloroquine eutectic crystal, and preparation method, content determination method and application thereof

A hydroxychloroquine and crystallization technology, applied in the field of hydroxychloroquine new co-crystal and preparation thereof, can solve problems such as quantitative analysis of unfavorable hydroxychloroquine salt compounds, difficulties in industrial production and storage, and achieve low hygroscopicity and tabletability, Good linear relationship and less side effects

Pending Publication Date: 2022-04-12
SOUTH CHINA UNIV OF TECH
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the hydroxychloroquine sulfate obtained by modifying the hydroxychloroquine salification method is soluble in water, has strong hygroscopicity, and is easily dissociated into hydroxychloroquine and sulfuric acid after absorbing water.

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
  • Novel hydroxychloroquine eutectic crystal, and preparation method, content determination method and application thereof
  • Novel hydroxychloroquine eutectic crystal, and preparation method, content determination method and application thereof
  • Novel hydroxychloroquine eutectic crystal, and preparation method, content determination method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0096] Example 1

[0097] In this embodiment, a hydroxychloroquine is prepared, and the specific process is:

[0098]134.1 mg of hydroxyanoquine (HCQ) and 220.8 mg of 4-dimethyl aminopyridine (DIM) were dissolved in 25.1 ° C ± 0.1 ° C. After stirring, it was allowed to stand for 12 h after stirring, and after filtration The solid room temperature was dried overnight to obtain the hydroxyanoquine new eutectic. The X-ray powder diffraction diagram of the product is indicated by a diffraction angle 2θ at 6.80 °, 11.45 °, 16.88 °, which does not have a characteristic peak of 8.12 ° hydroxyl chloroquine, nor a characteristic of 4-dimethylaminopyridine 12.09 °. Peak, with figure 1 Consistency, it is confirmed that the resulting product is a hydroxychloroquine.

Example Embodiment

[0099] Example 2

[0100] In this embodiment, a hydroxychloroquine is prepared, and the specific process is:

[0101] 149.8 mg of hydroxychloroquine and 267.8 mg of 4-dimethylamine pyridine were dissolved in 25.1 ° C ± 0.1 ° C, and after stirring, the mixing solution was allowed to be pulled at 24 h after stirring, and then the solid room temperature vacuum was dried overnight. The hydroxyanoquine is new eutectic. The X-ray powder diffraction diagram of the product is shown in the diffraction angle 2θ at 6.96 °, 11.53 °, 17.07 °, and does not have a characteristic peak of 8.12 ° hydroxyl chloroquine, nor a characteristic of 4-dimethylaminopyridine 12.09 °. Peak, with figure 1 Similarly, it was confirmed that the resulting product was a hydroxyanoquine.

Example Embodiment

[0102] Example 3

[0103] In this embodiment, a hydroxychloroquine is prepared, and the specific process is:

[0104] 180.6 mg of hydroxychloroquine and 172.5 mg of 4-dimethylaminopyridine were dissolved in 1.2 ml of acetonitrile at 34.2 ° C ± 0.1 ° C. After stirring, the mixing solution was pulp for 24 h. After filtration, the solid room temperature vacuum was dried overnight. The hydroxyanoquine is new eutectic. The X-ray powder diffraction diagram of the product is indicated by the diffraction angle 2θ at 6.80 °, 11.44 °, 17.02 °, is characterized by characteristic peaks, and attached. figure 1 Similarly, the characteristic peak of 8.12 ° hydroxychloroquine is not included, nor a characteristic peak of 4-dimethylaminopyridine 12.09 °, demonstrated that the resulting product is a hydroxychloroquine.

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 invention provides a novel hydroxychloroquine eutectic as well as a preparation method, a content determination method and application thereof. The novel hydroxychloroquine eutectic comprises a eutectic formed by hydroxychloroquine and 4-dimethylaminopyridine in a molar ratio of 2: 1. Compared with hydroxychloroquine, the novel hydroxychloroquine eutectic has higher dissolution rate and lower hygroscopicity compared with forms such as sulfate, phosphate and the like of hydroxychloroquine, the novel hydroxychloroquine eutectic can be prepared by various simple methods, and the novel hydroxychloroquine eutectic pharmaceutical composition has better dissolution rate, lower hygroscopicity and tabletting property, and can be used for preparing the pharmaceutical composition for preparing the hydroxychloroquine eutectic. And a novel hydroxychloroquine eutectic improved preparation with better curative effect and smaller side effect can be developed. The content determination method disclosed by the invention can be used for simultaneously and quantitatively determining the hydroxychloroquine and the 4-dimethylaminopyridine, and has the advantages of simplicity, rapidness, accuracy, reliability and good linear relationship in a high-concentration range.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a new co-crystal of hydroxychloroquine, a preparation method, a content determination method and an application thereof. Background technique [0002] Hydroxychloroquine (Hydroxychloroquine) (HCQ) chemical name 2-[[4-[(7-chloro-4-quinolyl)-amino]pentyl]ethylamino]-ethanol has a chiral carbon center with ( -)-(R)-Hydroxychloroquine and (+)-(S)-Hydroxychloroquine are two optical isomers, which belong to 4-aminoquinoline drugs. The isomers are mixed in equal proportions, that is, racemic compound administration, the structural formula of (+)-(S)-hydroxychloroquine is shown in formula I, and the structural formula of (-)-(R)-hydroxychloroquine is shown in formula II : [0003] [0004] Hydroxychloroquine was first used in the treatment of malaria parasites, and the phosphate and sulfate salts of hydroxychloroquine are now widely used in the clinical treatmen...

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
IPC IPC(8): C07D215/46C07D213/74A61K31/4706A61P31/12A61P29/00A61P37/00A61P33/06A61P19/02A61P17/00
Inventor 张扬白昆
Owner SOUTH CHINA UNIV OF TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap