A production process of high safety sulfobutyl ether-β-cyclodextrin sodium salt

Abstract

The invention relates to a production process of a novel high-safety sulfobutyl ether-beta-cyclodextrin sodium salt. The process comprises the following steps that 1, tetrahydrofuran and acetyl chlorid react under the catalytic action of zinc trichloride, an intermediate product is obtained and fully reacts in aqueous sodium sulfite, a reaction product reacts with hydrochloric acid, and 4-chlorine-butanesulfonate is obtained; 2, beta-cyclodextrin reacts with 4-chlorine-butanesulfonate under the alkaline condition, and after decolourization is conducted, a coarse sulfobutyl ether-beta-cyclodextrin sodium salt is obtained, and after refining is conducted on the coarse sulfobutyl ether-beta-cyclodextrin sodium salt, a sulfobutyl ether-beta-cyclodextrin sodium salt finished product is obtained. According to the production process of the novel high-safety sulfobutyl ether-beta-cyclodextrin sodium salt, the raw material 1,4-butanesultone with genotoxicity can be avoided; meanwhile, impurities in the process are easy to remove, the purification process is easier, the yield is relatively improved, and the drug risk is greatly reduced.

Description

technical field

[0001] The invention relates to a production process of high-safety sulfobutyl ether-beta-cyclodextrin sodium salt, and belongs to the technical field of pharmaceutical auxiliary material synthesis. Background technique

[0002] SBE-β-CD, the chemical name is sulfobutyl ether-β-cyclodextrin, is a new type of pharmaceutical preparation excipient, which belongs to a sulfonic acid derivative of anionic high water-soluble cyclodextrin. It can be well included with drug molecules to form non-covalent complexes, which improves the stability, water solubility and safety of drugs and effectively improves the biological activity of drug molecules. It has low nephrotoxicity and can ease drug hemolysis. , to control the drug release rate. At present, it has been commercialized and used in injection, oral, nasal, eye, etc., and has a special affinity and inclusion for nitrogen-containing drugs.

[0003] The existing synthetic method of sulfobutyl ether-β-cyclodextrin s...

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