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Preparation method of amorphous sugammadex sodium

A sugammadex sodium and amorphous technology, which is applied in the field of preparation of amorphous sugammadex sodium, can solve problems such as insoluble matter, unqualified product clarity, difficulty in meeting the quality requirements of raw materials, etc., and achieve stable product quality , improve quality and safety, and reduce production equipment requirements

Active Publication Date: 2018-12-21
郭辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, crystallization with alcohol as a solvent will lead to a small amount of insoluble matter in the aqueous solution of the final sugammadex sodium product, and the product clarity is unqualified, which brings potential quality control risks to the production of injections, and it is difficult to meet the quality requirements of the production of raw materials

Method used

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  • Preparation method of amorphous sugammadex sodium
  • Preparation method of amorphous sugammadex sodium
  • Preparation method of amorphous sugammadex sodium

Examples

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Effect test

Embodiment 1

[0041] Take 10 g of sugammadex sodium, add it to a three-necked flask, add 50 mL of water into the flask, and stir to dissolve. The temperature was raised to 75°C under stirring, the stirring speed was 200r / min, 300mL of 1,4-dioxane was added dropwise to the solution, and the stirring was cooled down to room temperature, a large amount of white solids were precipitated. After suction filtration, the filter cake was vacuum-dried to dryness to obtain 9.2 g of sugammadex sodium. See XRD diagram Figure 6 .

Embodiment 2

[0043] Take 10 g of sugammadex sodium, add it to a three-necked flask, add 200 mL of water into the flask, and stir to dissolve. Under nitrogen protection, the stirring speed was 100 r / min, and 1 L of tetrahydrofuran was added to the solution at room temperature. After the addition, a large amount of white solid precipitated out. Suction filtration, air-dried filter cake to dryness, 9.5g of pure Desugammadex Sodium, XRD figure see Figure 7 .

Embodiment 3

[0045] Take 10 g of sugammadex sodium crude product, add it into a three-necked flask, add 30 mL of water into the flask, and stir to dissolve. The solution is concentrated to dryness, and the pure product of Desugammadex Sodium is 10g, and the XRD pattern is shown in Figure 8 .

[0046]Different from Comparative Examples 1 to 5, the above-mentioned Examples 1 and 2 respectively select 1,4-dioxane and tetrahydrofuran as the crystallization solvent, and the sugammadex sodium prepared by direct drying in Example 3, the XRD pattern shows No obvious diffraction peaks were seen, indicating that the above products are all amorphous products.

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Abstract

The invention discloses a preparation method of amorphous sugammadex sodium. The preparation method comprises the following step of selecting a special solvent, or directly concentrating an aqueous solution of sugammadex sodium to the dry state, so as to obtain the amorphous sugammadex sodium product. Compared with the existing preparation method of the special-crystal form type sugammadex sodium,the preparation method has the advantages that the problem of clarification degree due to crystallizing of alcohol solvents is solved, and the quality safety of the finished product of the sugammadexsodium is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a preparation method of amorphous sugammadex sodium. Background technique [0002] Sugammadex sodium is a derivative of γ-cyclodextrin, its molecule is composed of a lipophilic core and a hydrophilic outer end, it is a selective muscle relaxant antagonist, and its molecular formula is C 72 h 104 Na 8 o 48 S 8 , the structure of the compound is as follows: [0003] [0004] Sugammadex sodium is a modified γ-cyclodextrin oligosaccharide, which is based on synthetic cyclodextrin and is water-soluble. With a lipophilic core, Sugammadex can wrap steroidal non-depolarizing muscle relaxants (such as: vecuronium and rocuronium bromide), forming an inactive tight complex in a 1:1 ratio, thereby hindering the muscle relaxants The redistribution of steroidal muscle relaxants accelerates the decomposition of nicotinic acetylcholine receptors, so it can antagonize neurom...

Claims

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Application Information

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IPC IPC(8): C08B37/16
CPCC08B37/0003C08B37/0012
Inventor 郭辉
Owner 郭辉
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