Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Refining and crystallization method of sugammadex sodium

A technology of sugammadex sodium and quality, applied in the field of medicinal chemistry, can solve problems such as difficulty in the preparation process, and achieve the effects of good fluidity, high product yield and purity, and improved dissolution rate

Active Publication Date: 2020-02-21
RUYUAN HEC PHARM
View PDF4 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the method is simple to operate, the sugammadex sodium obtained has higher purity and yield than other prior art, but the sugammadex sodium prepared by this method is needle-like crystals, which float in large quantities in the dissolution process. The water surface cannot be dissolved for a long time, causing great difficulties to the preparation process

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
  • Refining and crystallization method of sugammadex sodium
  • Refining and crystallization method of sugammadex sodium
  • Refining and crystallization method of sugammadex sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 10g of sugammadex sodium, add 20g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 6.178, and the temperature to 20°C; drop methanol at 20°C in 3 times Into the solution: drop 40g methanol into the solution, the dropping time is 30min, and grow the crystal for 1h; drop 8g methanol into the solution, the dropping time is 2h; drop 80g methanol into the solution, the dropping time is 1h; drop the temperature quickly after the dropping to 10° C., filtered, and vacuum dried at 90° C. for 24 hours to obtain about 9.35 g of the product with a yield of 93.5%, a product purity of 99.05%, a spherical shape and good fluidity.

Embodiment 2

[0035] Weigh 10g of sugammadex sodium, add 40g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 9.327, and raise the temperature to 70°C; drop methanol at 70°C in 3 drops Adding to the solution: drop 120g methanol into the solution, the dropping time is 5h, and grow the crystal for 1h; 80g methanol is dropped into the solution, the dropping time is 8h; 160g methanol is dropped into the solution, the dropping time is 10h; Cool down to 30°C, filter, and vacuum-dry at 90°C for 24 hours to obtain about 9.31g of product with a yield of 93.1% and a product purity of 99.02%. The product is spherical in shape and has good fluidity.

Embodiment 3

[0037] Weigh 10g of sugammadex sodium, add 25g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 7.574 and raise the temperature to 50°C; drop methanol at 25°C three times Add dropwise into the solution: drop 72g methanol into the solution for 100min, and grow the crystal for 1h; drop 16g methanol into the solution, dropwise for 5h; drop 112g methanol into the solution, dropwise for 3h; Rapidly cool down to 25°C, filter, and vacuum-dry at 90°C for 24 hours to obtain about 9.33g of product with a yield of 93.3% and a product purity of 99.07%. The product is spherical in shape and has good fluidity.

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 refining and crystallization method of sugammadex sodium, in particular to a method for refining sugammadex sodium by dropwise adding an anti-solvent in portions, and belongs to the field of medicinal chemistry. The method has the advantages of simple process, good repeatability and stability, low environmental pollution, being suitable for industrial production, and relatively high product yield and purity. In addition, the dissolution rate of sugammadex sodium obtained by the method is also greatly improved, and thereby the high-quality bulk drug for the pharmaceutical preparation process is provided.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a method for refining and crystallizing sugammadex sodium. Background technique [0002] Sugammadex Sodium (Sugammadex Sodium, CAS No.: 343306-79-6), chemical name is 6-full deoxy-6-full (2-carboxyethyl) thio-γ-cyclodextrin sodium salt, molecular structure As follows. Sugammadex sodium, a modified γ-cyclodextrin, is the first selective relaxation antagonist for reversal of neuromuscular blocking agents, clinically used as a neuromuscular inhibitor for reversal of rocuronide or vecuronide Muscle blocking effect, with good curative effect and safety. The drug was approved for marketing in the European Union in July 2008, and is now on the market in Japan, South Korea, the United States and other countries, and has been declared for production and marketing in my country. [0003] [0004] The dosage form of sugammadex sodium preparation is injection, and the solid raw mater...

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): C08B37/16
CPCC08B37/0003C08B37/0012
Inventor 王磊鑫张鹏伟张杰姚加雷正陈勇罗忠华黄芳芳
Owner RUYUAN HEC PHARM
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
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