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

Sugammadex sodium crystal form M

A technology of sugammadex sodium and crystal form, applied in the field of crystal form drug molecules, can solve the problems of thermal stability, photostability, dissolution, and bioavailability that cannot be well satisfied, and is suitable for large-scale promotion. Simple application, preparation method, and color-qualified effect

Active Publication Date: 2021-03-23
LUNAN PHARMA GROUP CORPORATION
View PDF10 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] As we all know, sugammadex sodium, which is an effective muscle relaxant antagonist, is an injection raw material drug, and injection preparations have strict requirements on various aspects of the raw material drug. , thermal stability, light stability, dissolution rate, bioavailability and other aspects can not meet the requirements of pharmaceutical preparations, so it is necessary to develop more crystal forms, on the one hand to provide more sugammadex sodium crystals for pharmaceutical applications Type, improve drug performance in terms of chemical purity, fluidity, solubility, stability (such as storage stability, dehydration stability, polymorph transformation stability, low hygroscopicity, low residual solvent content), clarity, etc., developed It has more efficient drugs; on the other hand, it is also necessary to develop sugammadex sodium crystals that are more suitable for industrial production and have high economic benefits

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
  • Sugammadex sodium crystal form M
  • Sugammadex sodium crystal form M
  • Sugammadex sodium crystal form M

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Under the protection of argon, add sugammadex sodium (10.03g) into purified water (15ml), put it into an ultrasonic instrument (45KHz) and stir to dissolve; add methanol (20ml) to the sugammadex sodium aqueous solution, and control the temperature Ultrasonic reaction at 35°C for 2 hours; when the reaction is complete, the temperature of the reaction liquid is controlled by ultrasonic (45KHz) at 25°C, and acetone (150ml) is added dropwise while stirring. , and the filter cake was dried under reduced pressure at 40°C to constant weight to obtain white crystalline sugammadex sodium with a yield of 98.8% and a purity of 99.91%.

Embodiment 2

[0054] Under the protection of argon, add sugammadex sodium (10.06g) into purified water (10ml), put it into an ultrasonic instrument (50KHz) and stir to dissolve; add ethanol (10ml) to the sugammadex sodium aqueous solution, and control the temperature Ultrasonic reaction at 30°C for 3 hours; after the reaction, the temperature of the reaction solution was controlled by ultrasonic (50KHz) at 25°C, and methanol (100ml) was added dropwise while stirring. , and the filter cake was dried under reduced pressure at 40°C to constant weight to obtain white crystalline sugammadex sodium with a yield of 97.4% and a purity of 99.85%.

Embodiment 3

[0056] Under the protection of argon, add sugammadex sodium (10.04g) into purified water (20ml), put it into an ultrasonic instrument (45KHz) and stir to dissolve; add methanol (25ml) to the sugammadex sodium aqueous solution, and control the temperature Ultrasonic reaction at 40°C for 2 hours; after the reaction, the temperature of the reaction solution was controlled at 20°C under ultrasonic (45KHz), and acetonitrile (200ml) was added dropwise while stirring. , and the filter cake was dried under reduced pressure at 40°C to constant weight to obtain white crystalline sugammadex sodium with a yield of 97.6% and a purity of 99.82%.

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 provides a sugammadex sodium crystal form M, and relates to the technical field of crystal form drug molecules. The sugammadex sodium crystal form M uses Cu-K alpha radiation, and an X-ray diffraction pattern represented by 2 theta has characteristic peaks at 5.93 + / -0.2 degrees, 7.47 + / -0.2 degrees, 8.38 + / -0.2 degrees, 17.80 + / -0.2 degrees, 18.83 + / -0.2 degrees, 20.05 + / -0.2 degrees, 21.55 + / -0.2 degrees, 22.39 + / -0.2 degrees and 24.03 + / -0.2 degrees. The invention further provides a related preparation method and application. The sugammadex sodium crystal form M is good in stability, the clarity and the color of a solution of the sugammadex sodium crystal form M meet injection crude drug standards, and the safety and the stability of a sugammadex sodium injection preparation are improved.

Description

technical field [0001] The invention relates to the technical field of crystal drug molecules, in particular to a crystal form of sugammadex sodium. Background technique [0002] Sugammadex Sodium, the chemical name is octa-6-perdeoxy-6-full(2-carboxyethyl)thio-γ-cyclodextrin sodium salt, CAS number: 343306-79-6, The specific structural formula is as follows: [0003] [0004] Sugammadex sodium is a new type of muscle relaxant reversal agent, which was first developed by Organon in the Netherlands. It is used to reverse the blocking effect of the routinely used neuromuscular blocking drugs rocuronium or vecuronium. Reverse the effect of rocuronium bromide used by adults, routinely reverse the effect of rocuronium bromide used by children and adolescents (2-17 years old). Sugammadex sodium is the first and only selective relaxant binding agent (selective relaxant binding agent, SRBA), which is the first major drug development in the field of anesthetics in the past 20 ye...

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): C08B37/16A61K31/724A61P21/00
CPCC08B37/0012A61P21/00A61K9/0019Y02A50/30
Inventor 鲍广龙张乃华
Owner LUNAN PHARMA GROUP CORPORATION
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