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

Epinastine hydrochloride crystal form, and preparation method and application thereof

A kind of epilastine hydrochloride crystal and epilastine hydrochloride technology, which are applied in the field of epilastine hydrochloride crystal form and its preparation and use, and can solve the problems of decreased drug stability, decreased drug effect, precipitation of liquid preparations and the like , to achieve the effect of improving stability and solubility, facilitating large-scale production and simple preparation process

Active Publication Date: 2014-10-15
凯默斯医药科技上海有限公司
View PDF8 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of drug preparation, transportation and storage, physical factors such as light, temperature, humidity, chemical factors such as decomposition and oxidation, and biological factors such as bacteria and microorganisms will reduce the stability of the drug, and solid preparations will be weathered and decomposed. , liquid preparations produce precipitation, mildew and other phenomena, which will lead to the degradation of its active ingredients, the reduction of drug efficacy, and even adverse reactions

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
  • Epinastine hydrochloride crystal form, and preparation method and application thereof
  • Epinastine hydrochloride crystal form, and preparation method and application thereof
  • Epinastine hydrochloride crystal form, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Embodiment 1 The preparation method of epinastine hydrochloride crystal form IX of the present invention

[0078] Weigh 2.0g of epinastine hydrochloride, dissolve it with 3mL of water / acetone mixed solution (water:acetone=2:1) ​​at an internal temperature of 60±5°C, add 0.1g of activated carbon, stir for decolorization, and then seal it and transfer it to a clean area , filtered while hot, cooled and crystallized, when a large amount of crystals precipitated, stood at -5~0°C for 8±1h, collected the crystals, and dried under reduced pressure to obtain 1.990g of epinastine hydrochloride crystal form IX, with a yield of 99.5%, melting point 275.6°C-275.9°C.

Embodiment 2

[0079] Example 2 The preparation method of epinastine hydrochloride crystal form IX of the present invention

[0080] Weigh 2.0g of epinastine hydrochloride, dissolve it with 2mL of water / acetone mixed solution (water:acetone=1:1) at an internal temperature of 60±5°C, add 0.1g of activated carbon, stir to decolorize, and then seal it and transfer it to a clean area , filtered while hot, cooled and crystallized, and when a large amount of crystals precipitated, they were left standing at -5~0°C for 8±1h, the crystals were collected, and dried under reduced pressure to obtain 1.986g of epinastine hydrochloride crystal form IX, with a yield of 99.3%, melting point 275.5°C-275.9°C.

Embodiment 3

[0081] Example 3 The preparation method of epinastine hydrochloride crystal form IX of the present invention

[0082] Weigh 2.0g of epinastine hydrochloride, dissolve it with 10mL of dichloromethane / ethanol mixed solution (dichloromethane:ethanol=4:1) at an internal temperature of 60±5°C, add 0.1g of activated carbon, stir to decolorize, and then seal it tightly Transfer to a clean area, filter while it is hot, cool and crystallize, and when a large amount of crystals precipitate, stand still at -5~0°C for 8±1h, collect the crystals, and dry under reduced pressure to obtain 1.976g of epinastine hydrochloride crystal form IX , the yield is 98.8%, and the melting point is 275.6°C-275.9°C.

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 discloses an epinastine hydrochloride crystal form. The crystal form comprises the following characteristic peaks shown in an X-ray powder diffraction pattern when the reflection angle 2theta is equal to 5.2 DEG+ / -0.2 DEG, 6.6 DEG+ / -0.2 DEG, 12.0 DEG+ / -0.2 DEG, 12.8 DEG+ / -0.2 DEG, 14.0 DEG+ / -0.2 DEG, 16.6 DEG+ / -0.2 DEG, 25.3DEG+ / -0.2DEG, 35.6DEG+ / -0.2DEG. The invention also discloses a preparation method and application of the crystal form. The epinastine hydrochloride crystal form IX is substantially improved in compound stability and solubility, and is relatively beneficial for medicine storage, transportation and absorption, and clinical medicine safety is guaranteed. The preparation technology of the crystal form IX is simple, convenient to operate, high in yield and suitable for large-scale production.

Description

technical field [0001] The invention provides a new crystal form of epinastine hydrochloride, a preparation method and application thereof. Background technique [0002] Epinastine hydrochloride is a second-generation long-acting piperidine antihistamine, which can be used to treat allergic rhinitis, urticaria, eczema, dermatitis, allergic bronchial asthma and other diseases. Chemical name: 3-amino-9,13b-dihydro-1H-diphenyl[c,f]imidazo[1,5-a]azepine hydrochloride, the structural formula is shown in formula 1: [0003] [0004] From the analysis of chemical structure, epinastine hydrochloride is highly hydrophilic, so it is difficult to penetrate the blood-brain barrier after entering the body, and the antagonism effect on the central nervous system is weak. Slight; in terms of mechanism of action, epinastine hydrochloride acts as histamine H 1 Receptor antagonist, highly selective, it only has a strong inhibitory effect on bronchoconstriction caused by histamine and bra...

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): C07D487/04A61K31/55A61P37/08A61P11/02A61P17/00A61P17/04A61P17/06A61P11/06A61P25/06A61P29/00A61P25/00A61P27/14
CPCC07D487/04
Inventor 傅霖李文婕陈刚
Owner 凯默斯医药科技上海有限公司
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