Supercharge Your Innovation With Domain-Expert AI Agents!

Sugammadex sodium crystal form

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. Application, qualified solution clarity, beneficial effect on drug storage

Active Publication Date: 2021-03-30
LUNAN PHARMA GROUP CORPORATION
View PDF10 Cites 0 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
  • Sugammadex sodium crystal form
  • Sugammadex sodium crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Add sugammadex sodium (20.05g) into purified water (100ml) and stir to dissolve; slowly add ethanol (20ml) dropwise to the sugammadex sodium aqueous solution, put it into a lyophilizer, and maintain it at -40°C for 12 hours ; After it is completely solidified, open the cold trap and vacuumize. When the vacuum reaches 150mT, raise the temperature to -20°C at 1°C / 4min, and maintain at -20°C for 15 hours for sublimation drying. ℃ / 2min to raise the temperature to 5°C, and maintain at 5°C for 15 hours for analysis and drying. After drying, close the cold trap to obtain white crystals of sugammadex sodium with a purity of 99.85%.

Embodiment 2

[0054] Add sugammadex sodium (20.03g) into purified water (90ml) and stir to dissolve; slowly add acetone (10ml) dropwise to sugammadex sodium aqueous solution, put it into a lyophilizer, and maintain it at -30°C for 15 hours ; After it is completely solidified, open the cold trap and vacuumize. When the vacuum reaches 150mT, raise the temperature to -15°C at 1°C / 3min, and maintain at -15°C for 20 hours for sublimation drying. ℃ / 3min to raise the temperature to 0°C, and maintain at 0°C for 20 hours for analysis and drying. After drying, close the cold trap to obtain white crystalline sugammadex sodium with a purity of 99.81%.

Embodiment 3

[0056] Add sugammadex sodium (20.06g) into purified water (100ml) and stir to dissolve; slowly add methanol (30ml) dropwise to sugammadex sodium aqueous solution, put it into a lyophilizer, and maintain it at -45°C for 14 hours ; After it is completely solidified, open the cold trap and vacuumize. When the vacuum reaches 150mT, raise the temperature to -25°C at 1°C / 4min, and maintain at -25°C for 20 hours for sublimation drying. ℃ / 2min to raise the temperature to 10°C, and maintain at 10°C for 15 hours for analysis and drying. After drying, close the cold trap to obtain white crystalline sugammadex sodium with a purity of 99.80%.

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, and relates to the technical field of crystal form drug molecules. The sugammadex sodium crystal form uses Cu-K[alpha] radiation, and X-ray diffraction patterns represented by 2[theta] have 4.49 + / -0.2 degrees, 5.47+ / -0.2 degrees, 7.20+ / -0.2 degrees, 7.77+ / -0.2 degrees, 8.80+ / -0.2 degrees, 9.96+ / -0.2 degrees, 10.24+ / -0.2 degrees, 12.54+ / -0.2degrees, 15.75+ / -0.2 degrees, 16.28+ / -0.2 degrees, 16.85+ / -0.2 degrees, 17.59+ / -0.2 degrees, 18.06+ / -0.2 degrees and 19.16+ / -0.2 degrees. The invention further provides a related preparation method and application. The sugammadex sodium crystal form is good in stability, the clarity and the color of a solution of the sugammadex sodium crystal form 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
CPCC08B37/0012A61K31/724A61P21/00A61K9/0019Y02A50/30
Inventor 张贵民鲍广龙肖建东刘云娜
Owner LUNAN PHARMA GROUP CORPORATION
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com