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

Method for preparing rocuronium crystalline hydrate

A technology of crystalline hydrate and rocuronium bromide, which is applied in the fields of steroids and organic chemistry, and can solve problems such as unfavorable storage, instability, and easy moisture absorption of rocuronium bromide

Inactive Publication Date: 2009-04-01
重庆人本药物研发有限责任公司
View PDF4 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Because rocuronium bromide is very easy to absorb moisture and is very unstable, the Pharmacopoeia requires storage under low temperature and sealed conditions, which makes the existing rocuronium bromide products unfavorable for preservation, which will undoubtedly increase the storage of drugs for manufacturers and users cost, and the storage of drugs also brings great troubles to manufacturers and users

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
  • Method for preparing rocuronium crystalline hydrate
  • Method for preparing rocuronium crystalline hydrate
  • Method for preparing rocuronium crystalline hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0019] Weigh 3.0g of rocuronium bromide into a 50mL single-necked bottle, add 40mL of distilled water, shake to dissolve, pour it into a petri dish, then put the petri dish into the lyophilizer, and lower the temperature in the lyophilizer to— At 40°C, the solution in the culture dish was frozen into ice, vacuumized, and when the pressure was reduced and the temperature was raised to 40°C within 15 hours, it was vacuum-dried for 20 hours to obtain rocuronium bromide crystalline hydrate (containing 1.5 crystal water) 2.8 g.

[0020] Elemental analysis: C32H53BrN2O4.1.5 H2O theoretical value C 60.28%, H 8.79%, Br 12.72%, N 4.40%, O 13.81%; measured value C 60.14%, H 8.89%, Br 12.64%, N 4.37%, O 13.96% . The organic solvent residue of rocuronium bromide was 10.36% before freeze-drying, and the organic solvent residue in rocuronium bromide crystalline hydrate was 0.05% after freeze-drying.

Embodiment approach 2

[0022] Weigh 1.5g of rocuronium bromide into a 50mL single-necked bottle, add 45mL of distilled water, shake to dissolve, pour it into a petri dish, then put the petri dish into the freeze dryer, and lower the temperature inside the freeze dryer to— 50°C, freeze the solution in the petri dish into ice, vacuumize, heat up to 50°C under reduced pressure within 20 hours, heat and vacuum dry for 30 hours, and get rocuronium bromide crystalline hydrate (containing 1.5 crystal water) 1.4 g.

[0023] Elemental analysis: C32H53BrN2O4.1.5H2O theoretical value C 60.28%, H 8.79%, Br 12.72%, N 4.40%, O 13.81%; measured value C 60.23%, H 8.81%, Br 12.69%, N 4.39%, O 13.88% . The organic solvent residue of rocuronium bromide before freeze-drying was 10.36%, and the organic solvent residue in rocuronium bromide crystalline hydrate after freeze-drying was 0.07%.

Embodiment approach 3

[0025] Weigh 1.5g of rocuronium bromide into a 50mL single-necked bottle, add 10mL of distilled water, shake to dissolve, pour it into a petri dish, then put the petri dish into the freeze dryer, and lower the temperature inside the freeze dryer to— 30°C, freeze the solution in the petri dish into ice, vacuumize it, and heat it up to 30°C under reduced pressure within 10 hours, keep it warm and vacuum dry for 10 hours, and get rocuronium bromide crystalline hydrate (containing 1.5 crystal water) 1.3 g.

[0026] Elemental analysis: C32H53BrN2O4.1.5 H2O theoretical value C 60.28%, H 8.79%, Br 12.72%, N 4.40%, O 13.81%; measured value C 60.25%, H 8.80%, Br 12.68%, N 4.37%, O 13.90% . The organic solvent residue of rocuronium bromide before freeze-drying was 10.36%, and the organic solvent residue in rocuronium bromide crystal hydrate after freeze-drying was 0.04%.

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 relates to a preparation method of bulk drugs, in particular to a preparation method of rocuronium bromide crystalline hydrate, which comprises the following steps of: preparing the rocuronium bromide aqueous solution with 2-15 percent of weight volume percent concentration, freezing the aqueous solution to ice under -50-30 DEG C, decompressing and heating up to 30-50 DEG C under vacuum state, keeping 10-20 hours of temperature-rise period and preserving heat for 10-30 hours in vacuum at the temperature. The rocuronium bromide crystalline hydrate prepared by the method enhances the stability of the rocuronium bromide bulk drugs, improves the particle exterior of the rocuronium bromide and effectively reduces the excessive organic residue of the rocuronium bromide bulk drugs.

Description

technical field [0001] The present invention relates to the preparation method of crude drug, especially the preparation method of rocuronium bromide crystalline hydrate. Background technique [0002] Rocuronium Bromide (Rocuronium Bromide) is a new type of non-depolarizing sterol muscle relaxant that was researched and developed by Organon Company and first listed in the United States and the United Kingdom in June and July 1994. It has a rapid onset of action and can Provides similar intubation conditions to succinylcholine, its effectiveness is highly evaluated, and it makes a significant clinical contribution. The chemical structural formula of rocuronium bromide is: [0003] [0004] European patent EP0287150 discloses the synthetic method and application of rocuronium bromide; WO0044334 discloses a compound injection composed of rocuronium bromide and other traditional muscle relaxants; US2006058275 and US2006058276 patents relate to preparing a pure solid powder o...

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): C07J43/00
Inventor 于国锋陈小勇王晓琳
Owner 重庆人本药物研发有限责任公司
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