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New compound for muscle relaxation antagonism

A compound and antagonistic technology, applied in the field of medicine, can solve the problems of difficult synthesis and uncertainty, and achieve the effects of easy preparation, convenient storage and transportation, and convenient storage

Pending Publication Date: 2021-01-29
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although medicinal chemistry and pharmacy are practical sciences that continue to develop, they constantly guide pharmaceutical progress through innovation, continuously improve drug safety to guide the development of drugs and preparations and guide clinical medication, and even though pharmaceuticals have reached the point of changing the physical state of raw materials However, due to the difficulty and uncertainty of synthesis, so far, there are no published literature reports on the in-depth innovation of the new stable chemical state of sugammadex sodium at home and abroad. Research and precise synthesis, new compounds with chemical molecular formula and molecular weight or structural formula that are easier to prepare or have better stability, such as ω-type crystal compounds and ν-type compounds, etc., that is, new compounds with different molecular formulas or structural forms, their preparation methods and uses

Method used

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  • New compound for muscle relaxation antagonism
  • New compound for muscle relaxation antagonism
  • New compound for muscle relaxation antagonism

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Example 1 Preparation of sugammadex sodium 7.5 hydrate (ω-type compound)

[0106] In a 250ml three-necked flask, add 5g of sugammadex, add 1ml of methanol, and 8ml of water, stir, protect with nitrogen, heat up to 30-40°C, stir, add 6M sodium hydroxide solution to adjust the pH of the solution to about 9.5, After stirring and dissolving, continue to stir for about 20 minutes, evaporate part of the solvent under reduced pressure, then add 20ml of acetonitrile and 80ml of absolute ethanol, place at 0°C, wait for the precipitate to be fully separated, filter with suction, wash with a small amount of ethanol for 3 times, and filter with suction to dilute the obtained solid Air-dried in an oven at about 35°C for about 2 hours, then at about 58°C for about 3 hours to obtain about 4.2 g of off-white solid; identification: ①HPLC: the retention time of the main peak of HPLC in the content determination is compared with that of sugammadex sodium The main peak retention time of th...

Embodiment 2

[0107] Embodiment 2 Preparation of sugammadex sodium 7 hydrate (v type compound)

[0108]In a 250ml three-necked flask, add 8g of sugammadex, add an appropriate amount of water, stir, protect with nitrogen, heat up to 30-40°C, stir, add 4M sodium hydroxide solution to adjust the pH of the solution to about 9.8, stir to dissolve, Then add 50ml of methanol and 100ml of ethanol, place it at about 0°C, wait for the precipitate to be fully separated, filter with suction, wash with a small amount of ethanol, and filter with suction, the obtained solid is diluted and dried in an oven at about 61°C for about 2 hours to obtain an off-white solid of about 7.3 g; Identification: ①HPLC: The retention time of the main peak of HPLC in the determination of the content is consistent with the retention time of the main peak of the HPLC of the sugammadex sodium reference substance; the water content measured by Karl Fischer's method is 5.51%, and thermal analysis: the weight loss on the platform...

Embodiment 3

[0109] Embodiment 3 Preparation of sugammadex sodium 3.5 hydrate (theta type compound)

[0110] Add 8g of sugammadex sodium anhydrous to a 250ml three-necked flask, add appropriate amount of water, protect with nitrogen, stir, heat up to about 40°C, stir until completely dissolved, add 60ml of acetonitrile, 100ml of methanol, cool to below 5°C and place , when the precipitate was fully separated, filtered with suction, washed with a small amount of ethanol for 3 times, and filtered with suction, the obtained solid was diluted in an oven at 35°C for about 3 hours, and at about 81°C for about 3 hours, and 7.3g of off-white solid was obtained; Identification: ①HPLC: the main peak retention time of its HPLC in the content determination is consistent with the main peak retention time of the HPLC of sugammadex sodium anhydrous; Karl Fischer's method determines that the moisture content is 2.83%, and thermal analysis: the weight loss on the platform is about 2.76% (see appendix Figu...

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Abstract

The invention discloses a new compound for muscle relaxation antagonism. The new compounds of theta type, beta type, gamma type, lambda type, kappa type, nu type, tau type, omega type, upsilon type and the like of sugammadex sodium have less hygroscopicity and better storage stability, are more beneficial to quality control of medicines and preparations and the like, and are suitable for preparingspecific binding neuromuscular block antagonists. And the compound can be applied to drugs for antagonizing treatment or prevention of neuromuscular block induced by rocuronium bromide or vecuroniumbromide and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, and in particular provides a new compound with a new molecular formula of sugammadex sodium, a muscle relaxant antagonist, with better stability. Background technique [0002] Sugammadex Sodium (Sugammadex Sodium, CAS: 343306-79-6, molecular formula C 72 h 104 Na 8 o 48 S 8 , M=2178.01) is a synthetic sodium salt of γ-cyclodextrin with a ring structure surrounded by 8 glucose molecules, and it is also the first selective muscle relaxation antagonist (SRBA) successfully developed in the past 20 years. Sugammadex has a lipophilic inner cavity and a hydrophilic outer edge, and its inner cavity size is suitable for ROC, an aminosteroid muscle relaxant. It uses 8 negatively charged side chain carboxyl groups protruding from the edge to increase its inner lipophilicity and outer edge hydrophilicity, and closely binds positively charged quaternary ammonium ions of ROC molecules in a ratio of 1:1 t...

Claims

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Application Information

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IPC IPC(8): C08B37/16A61K31/724A61P21/00A61P25/00
CPCC08B37/0012C08B37/0003A61K31/724A61P25/00A61P21/00
Inventor 刘力
Owner 刘力
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