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Production process of novel high-safety sulfobutyl ether-beta-cyclodextrin sodium salt

A technology of cyclodextrin sodium and sulfobutyl ether, which is applied in the field of pharmaceutical excipient synthesis to achieve the effects of reduced risk of use, high yield, and simple purification process

Active Publication Date: 2016-09-07
SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Chinese patent documents CN103694376A and CN 104892797A still use 1,4-butane sultone as the main raw material, so there is a great risk when the prepared sulfobutyl ether-β-cyclodextrin sodium salt is used as a preparation auxiliary material

Method used

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  • Production process of novel high-safety sulfobutyl ether-beta-cyclodextrin sodium salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] A novel, high-safety sulfobutyl ether-beta-cyclodextrin sodium salt production process, comprising the following steps:

[0041] (1) Preparation of 4-chloro-butanesulfonic acid

[0042] 80kg tetrahydrofuran and 77kg acetyl chloride were reacted under the catalysis of 50g zinc chloride to obtain an intermediate product, and then the intermediate product was fully reacted in 300kg 30wt% sodium sulfite aqueous solution, and then hydrochloric acid was hydrolyzed to obtain 4-chloro-butanesulfonate acid reaction solution.

[0043] (2) Preparation of sulfobutyl ether-β-cyclodextrin sodium salt

[0044] Add 96L of purified water into the K1000 reactor, and start stirring. Add 80kg of β-cyclodextrin, turn on and heat to 100-130°C, the pressure inside the kettle is 0.2-0.4MPa, add sodium hydroxide dropwise (50kg sodium hydroxide is dissolved in 75kg purified water) to adjust the pH of the solution in the kettle to ≈13, and then add dropwise The 4-chloro-butanesulfonic acid rea...

Embodiment 2

[0051] A novel, high-safety sulfobutyl ether-beta-cyclodextrin sodium salt production process, comprising the following steps:

[0052] (1) Preparation of 4-chloro-butanesulfonic acid

[0053] 80kg tetrahydrofuran and 77kg acetyl chloride were reacted under the catalysis of 50g zinc chloride to obtain an intermediate product, and then the intermediate product was fully reacted in 300kg 30wt% sodium sulfite aqueous solution, and then hydrochloric acid was hydrolyzed to obtain 4-chloro-butanesulfonate acid reaction solution.

[0054] (2) Preparation of sulfobutyl ether-β-cyclodextrin sodium salt

[0055] Add 96L of purified water into the K1000 reactor, and start stirring. Add 80kg of β-cyclodextrin, turn on and heat to 100-130°C, the pressure inside the kettle is 0.2-0.4MPa, add sodium hydroxide dropwise (50kg sodium hydroxide is dissolved in 75kg purified water) to adjust the pH of the solution in the kettle to ≈11, and then add dropwise The 4-chloro-butanesulfonic acid rea...

Embodiment 3

[0062] A novel, high-safety sulfobutyl ether-beta-cyclodextrin sodium salt production process, comprising the following steps:

[0063] (1) Preparation of 4-chloro-butanesulfonic acid

[0064] 80kg tetrahydrofuran and 77kg acetyl chloride were reacted under the catalysis of 50g zinc chloride to obtain an intermediate product, and then the intermediate product was fully reacted in 300kg 30wt% sodium sulfite aqueous solution, and then hydrochloric acid was hydrolyzed to obtain 4-chloro-butanesulfonate acid reaction solution.

[0065] (2) Preparation of sulfobutyl ether-β-cyclodextrin sodium salt

[0066] Add 96L of purified water into the K1000 reactor, and start stirring. Add 80kg of β-cyclodextrin, turn on and heat to 100-130°C, the pressure inside the kettle is 0.2-0.4MPa, add sodium hydroxide dropwise (50kg sodium hydroxide is dissolved in 75kg purified water) to adjust the pH of the solution in the kettle to ≈11, and then add dropwise The 4-chloro-butanesulfonic acid rea...

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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 novel and high-safety sulfobutyl ether-beta-cyclodextrin sodium salt production process, which belongs to the technical field of pharmaceutical auxiliary materials 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-cycl...

Claims

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Application Information

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IPC IPC(8): C08B37/16A61K47/48
CPCC08B37/0015
Inventor 李媛媛申健陈晋波王希卫
Owner SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD
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