Preparation method of high-purity sugammadex sodium

A technology of high-purity sugammadex sodium, applied in the field of preparation of high-purity sugammadex sodium, to achieve the effects of no genotoxicity, wide sources and reduction of metal ions

Active Publication Date: 2020-11-24
HEFEI BOSIKC PHARMTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] There are many disadvantages in the purification method in the prior art, therefore, be badly in need of a kind of preparation method of new high-purity sugammadex sodium, realize effective purification and obtain sugammadex sodium pure product

Method used

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  • Preparation method of high-purity sugammadex sodium

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preparation example Construction

[0047] Preparation of Crude Sugammadex Sodium

[0048] Put 3-mercaptopropionic acid (12.2mL, 140mol) into the reaction flask, add 450mL of N,N-dimethylformamide, add sodium hydride (12.3g, 308mol, 60% ), stirred at room temperature for 30 minutes after the addition, added dropwise γ-iodocyclodextrin (31.2g, 14mmol, dissolved in 450mL of N,N-dimethylformamide), after the dropwise addition was completed, the temperature was raised to 70 Degree, reaction 12h. After completion of the reaction, cool to room temperature, add 100mL of water, stir, distill under reduced pressure until the solvent remains 400mL, add 2L of ethanol, filter, collect the solid, and dry in vacuo to obtain 45g of off-white solid with a purity of 91.92%. See the test results figure 1 .

[0049] Sugammadex Sodium Injection Sterilization Color Inspection Experiment:

[0050] Take 1g of sugammadex sodium sample, under the protection of nitrogen filling, dissolve it in 8ml of water for injection, heat to diss...

Embodiment 1

[0054] Embodiment 1: Refining of sugammadex sodium

[0055] Take 100.0 g of sugammadex sodium crude product, dissolve it with 0.3 L of water until clear, add 2.0 g of inositol hexaphosphate (50% aqueous solution) under stirring, and raise the temperature to 80° C. under nitrogen protection, and add 0.8 L of After adding N,N-dimethylformamide, stir and cool down to room temperature, a large amount of white solid precipitates, filter with suction, and obtain 39.8g of pure sugammadex sodium with a purity of 99.8%, see figure 2 .

[0056] Of course, stirring and cooling can also be carried out to -20-30 degrees Celsius.

Embodiment 2

[0057] Embodiment 2: Refining of sugammadex sodium

[0058] Take 100 g of sugammadex sodium crude product, dissolve it with 1 L of water until clear, add 1 g of inositol diphosphate under stirring, raise the temperature to 70°C under nitrogen protection, and add 6 L of acetonitrile to the solution. After the addition was completed, the temperature was lowered to room temperature with stirring, and a large amount of white solids were precipitated. After suction filtration, 32.3 g of pure sugammadex sodium was obtained, with a purity of 99.5%.

[0059] The protective gas can also be one selected from nitrogen, argon, helium, and carbon dioxide.

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Abstract

The invention discloses a preparation method of high-purity sugammadex sodium. The high-purity sugammadex sodium is prepared from inositol phosphate and derivatives thereof. The specific process comprises the following steps of adding a specific type of protective agent into a crude sugammadex sodium product, and performing recrystallizing under the protection of inert gas to obtain a pure sugammadex sodium product, wherein the protective agent is selected from the inositol phosphate and the derivatives thereof, such as inositol hexaphosphate and salts or esters thereof, partial degradation products of the inositol hexaphosphate, such as inositol pentaphosphate, inositol tetraphosphate, inositol triphosphate, inositol diphosphate and inositol monophosphate, and one or a mixture of two or more of the above-mentioned substances and salts or esters thereof in any proportion. The method is simple and convenient to operate, high in product purity, good in safety, few in anaphylactic reaction, good in economical efficiency and more suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical production, in particular to a preparation method of high-purity sugammadex sodium. Background technique [0002] The chemical name of sugammadex sodium is 6A, 6B, 6C, 6D, 6E, 7F, 6G, 6H-octa-S-(2-carboxyethyl)-6A, 6B, 6C, 6D, 6E, 7F, 6G, 6H-octathio-γ-cyclodextrin, octasodium salt, [0003] The structural formula is: [0004] [0005] Sugammadex sodium is a new type of muscle relaxant reversal agent developed by Organon in the Netherlands. It is clinically used to reverse the neuromuscular blockade of rocuronium or vecuronium. Since the European Union approved its listing in July 2008, it has been listed in Japan, South Korea, the United States and other countries, and in April 2018 in China. [0006] Sugammadex sodium is a supramolecular cyclic compound obtained after structural modification of the 6-hydroxyl on the γ-cyclodextrin molecule, and its structure is complex. Since there...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/16A61K9/08A61K31/724A61P21/00
CPCC08B37/0012A61K9/08A61K9/0019A61K31/724A61P21/00A61K47/32
Inventor 郭辉吴友灵潘攀李明明沈剑飞
Owner HEFEI BOSIKC PHARMTECH CO LTD
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