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A kind of refined crystallization method of sugammadex sodium

A technology of sugammadex sodium and quality, applied in the field of medicinal chemistry, can solve problems such as difficulty in the preparation process, and achieve the effects of good fluidity, good repeatability and stability, and high product yield and purity.

Active Publication Date: 2021-06-01
RUYUAN HEC PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the method is simple to operate, the sugammadex sodium obtained has higher purity and yield than other prior art, but the sugammadex sodium prepared by this method is needle-like crystals, which float in large quantities in the dissolution process. The water surface cannot be dissolved for a long time, causing great difficulties to the preparation process

Method used

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  • A kind of refined crystallization method of sugammadex sodium
  • A kind of refined crystallization method of sugammadex sodium
  • A kind of refined crystallization method of sugammadex sodium

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Weigh 10g of sugammadex sodium, add 20g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 6.178, and the temperature to 20°C; drop methanol at 20°C in 3 times Into the solution: drop 40g methanol into the solution, the dropping time is 30min, and grow the crystal for 1h; drop 8g methanol into the solution, the dropping time is 2h; drop 80g methanol into the solution, the dropping time is 1h; drop the temperature quickly after the dropping to 10° C., filtered, and vacuum dried at 90° C. for 24 hours to obtain about 9.35 g of the product with a yield of 93.5%, a product purity of 99.05%, a spherical shape and good fluidity.

Embodiment 2

[0035] Weigh 10g of sugammadex sodium, add 40g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 9.327, and raise the temperature to 70°C; drop methanol at 70°C in 3 drops Adding to the solution: drop 120g methanol into the solution, the dropping time is 5h, and grow the crystal for 1h; 80g methanol is dropped into the solution, the dropping time is 8h; 160g methanol is dropped into the solution, the dropping time is 10h; Cool down to 30°C, filter, and vacuum-dry at 90°C for 24 hours to obtain about 9.31g of product with a yield of 93.1% and a product purity of 99.02%. The product is spherical in shape and has good fluidity.

Embodiment 3

[0037] Weigh 10g of sugammadex sodium, add 25g of water to dissolve completely at room temperature, mechanically stir at 150rpm, filter to obtain a clear solution, adjust the pH of the solution to 7.574 and raise the temperature to 50°C; drop methanol at 25°C three times Add dropwise into the solution: drop 72g methanol into the solution for 100min, and grow the crystal for 1h; drop 16g methanol into the solution, dropwise for 5h; drop 112g methanol into the solution, dropwise for 3h; Rapidly cool down to 25°C, filter, and vacuum-dry at 90°C for 24 hours to obtain about 9.33g of product with a yield of 93.3% and a product purity of 99.07%. The product is spherical in shape and has good fluidity.

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Abstract

The invention relates to a method for refining and crystallizing sugammadex sodium, in particular to a method for refining sugammadex sodium by dropping an anti-solvent step by step, and belongs to the field of medicinal chemistry. The method has the advantages of simple process, good repeatability and stability, little environmental pollution, suitability for industrial production, and high product yield and purity; in addition, the dissolution rate of sugammadex sodium prepared by this method in water has also been obtained. Greatly improved, high-quality raw materials are provided for the pharmaceutical preparation process.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a method for refining and crystallizing sugammadex sodium. Background technique [0002] Sugammadex Sodium (Sugammadex Sodium, CAS No.: 343306-79-6), chemical name is 6-full deoxy-6-full (2-carboxyethyl) thio-γ-cyclodextrin sodium salt, molecular structure As follows. Sugammadex sodium, a modified γ-cyclodextrin, is the first selective relaxation antagonist for reversal of neuromuscular blocking agents, clinically used as a neuromuscular inhibitor for reversal of rocuronide or vecuronide Muscle blocking effect, with good curative effect and safety. The drug was approved for marketing in the European Union in July 2008, and is now on the market in Japan, South Korea, the United States and other countries, and has been declared for production and marketing in my country. [0003] [0004] The dosage form of sugammadex sodium preparation is injection, and the solid raw mater...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/16
CPCC08B37/0003C08B37/0012
Inventor 王磊鑫张鹏伟张杰姚加雷正陈勇罗忠华黄芳芳
Owner RUYUAN HEC PHARM
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