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

Crystalline forms of azilsartan medoxomil potassium and preparation and uses thereof

A technology for azilsartan medoxomil and crystal form, which is applied in the field of medicinal chemistry, can solve the problem of inability to know the crystal form state of azilsartan medoxomil potassium salt, and achieves good bioavailability and dissolution curve, good solubility and thermal stability. Stability and excellent performance

Active Publication Date: 2014-09-10
RUYUAN HEC PHARM
View PDF3 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, US7157584 did not fully characterize the obtained crystal form of azilsartan medoxomil potassium, therefore, we cannot know the crystal form state of the obtained azilsartan medoxomil potassium salt obtained in this patent

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
  • Crystalline forms of azilsartan medoxomil potassium and preparation and uses thereof
  • Crystalline forms of azilsartan medoxomil potassium and preparation and uses thereof
  • Crystalline forms of azilsartan medoxomil potassium and preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Example 1: Preparation of Azilsartan Medoxomil Potassium Salt Form A

[0101] Azilsartan medoxomil (1.0g) was dissolved in refluxing acetone (20mL) to form a solution, the solution was cooled to 50°C, and potassium 2-ethylhexanoate (0.35g) in acetone was slowly added dropwise to the solution (1mL) solution, slowly cool down to 0°C, add acetic acid dropwise to adjust pH 5-6, continue to heat and stir for 5h, filter, and vacuum dry at 45°C for 12h to obtain a white powder, which is azilsartan by XRPD test results Potassium ester crystal form A, as attached figure 1 shown.

Embodiment 2

[0102] Example 2: Preparation of Azilsartan Medoxomil Potassium Form B

[0103] Azilsartan medoxomil (1.0g) was dissolved in refluxing acetone (20mL) to form a solution, the solution was cooled to 50°C and slowly added to a solution of potassium 2-ethylhexanoate (0.35g) in acetone (1mL) , the solution was slowly cooled to 0°C, continued to insulate and stir for 5 hours, and filtered, and the obtained solid was detected by XRPD. The results showed that the sample was azilsartan medoxomil potassium crystal form B, as figure 2 shown.

Embodiment 3 to Embodiment 25

[0104] Embodiment 3 to Embodiment 25 are the preparation of azilsartan medoxomil potassium salt crystal form 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 present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan medoxomil potassium, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L. The substantially pure crystalline forms of azilsartan medoxomil potassium of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan medoxomil potassium generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan medoxomil potassium, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new crystal form of azilsartan medoxomil potassium salt, a pharmaceutical composition comprising the crystal form of azilsartan medoxomil potassium, and a preparation method and use thereof. Background technique [0002] Azilsartan medoxomil, also known as (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2' -(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate , the structure is shown in formula I, azilsartan medoxomil is the prodrug of angiotensin Ⅱ receptor antagonist azilsartan (TAK-536), used for the treatment of adult hypertension, oral once a day, azilsartan Tansylate can be used alone or in combination with other antihypertensive agents [0003] [0004] Its structure of the potassium salt of azilsartan medoxomil is as shown in formula II: [0005] [0006] Takeda disclosed azilsartan medoxomil potassium salt for the ...

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): C07D413/10A61K31/4245A61P9/12
CPCC07D413/14A61P9/12
Inventor 雷鑫吕志卿王天明
Owner RUYUAN HEC PHARM
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