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

0 Cites 0 Cited by

AI-Extracted 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. ...

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

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.

Application Domain

Organic active ingredientsOrganic chemistry +8

Technology Topic

High concentrationAminopyridines +8

Image

Examples

Experimental program(9)
Comparison scheme(1)
Effect test(3)

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

Description & Claims & Application Information

We can also present the details of the Description, Claims and Application information to help users get a comprehensive understanding of the technical details of the patent, such as background art, summary of invention, brief description of drawings, description of embodiments, and other original content. On the other hand, users can also determine the specific scope of protection of the technology through the list of claims; as well as understand the changes in the life cycle of the technology with the presentation of the patent timeline. Login to view more.

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

Classification and recommendation of technical efficacy words

Good dissolution rate
Simple process

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

AI-Extracted Technical Summary

Problems solved by technology

Abstract

Image

Examples

Example Embodiment

Example Embodiment

Example Embodiment

PUM

Description & Claims & Application Information

Similar technology patents

Lithium secondary battery comprising fine fibrous porous polymer membrane and fabrication method thereof

Hot rolling process of high-plasticity and low-anisotropy magnesium alloy and sheet thereof

Alkali activated solidification and stabilization treatment method of refuse incineration fly ash

Sensing Structure

Cable retraction mechanism for trigger shifters

Classification and recommendation of technical efficacy words

Linezolid tablets in stable crystal form and preparation method thereof

Novel febuxostat crystal form A and preparation method thereof

Preparation method of traditional Chinese medicinal soft capsules for treating breast diseases and product thereof

Glycine chelated calcium tablet composition and preparation method thereof

Ambroxol hydrochloride dispersible tablet and preparation method thereof

Semiconductor device and method for manufacturing the same

Connector gateway

Multimedia data recording apparatus, monitor system, and multimedia data recording method

Simultaneously desulfurization and denitration wet ammonia flue gas cleaning technology and system thereof

Method for recycling metal oxide from waste flue gas denitration catalyst