Method for synthesizing high-purity polysorbate-80

Abstract

The invention relates to a method for synthesizing high-purity polysorbate-80. The polysorbate-80 (I) is a partial esterified product of a sorbitan ethyoxyl compound and oleic acid. The method comprises the following steps of: (1) partially dehydrating sorbitol as a raw material under the action of an acid catalyst in a state of vacuum to obtain sorbitan (II); (2) carrying out addition polymerization on the sorbitan (II) and oxirane under the action of a base catalyst to obtain sorbitan polyethenoxy ether (III), wherein the addition number of the oxirane is 20; (3) reacting the sorbitan polyethenoxy ether (III) with the high-purity oleic acid under the action of an esterifying catalyst and refining to obtain the high-purity polysorbate-80. The invention leads the emulsifying and solubilizing performance of products to be more perfect and the quality of the products to easily meet the requirement of an injection class and has easily controlled quality and good stability; and the high-purity polysorbate-80 has lower blood dissolving rate in same concentration, and predictable and safer clinical use by being used as an auxiliary material for injection.

Description

technical field [0001] The invention relates to a chemical synthesis method, in particular to a synthesis method of high-purity polysorbate-80 (I). Background technique [0002] Polysorbate-80 (I), also known as polyoxyethylene (20) sorbitan monooleate, it is a kind of hydrophilic nonionic surfactant, because it has better solubilizing effect, in When preparing injections of poorly soluble drugs, it is often used as a cosolvent, emulsifier and stabilizer. [0003] The synthetic method of (I) reported in the literature usually has the following two kinds: [0004] Method 1: Sorbitol and oleic acid undergo simultaneous dehydration and esterification reactions under the action of a basic catalyst to obtain sorbitan monooleate, which is then condensed with 20 mole fractions of ethylene oxide to obtain polysorbate- 80(I). [0005] Method 2: Sorbitol is first dehydrated under the action of an acidic or alkaline catalyst to obtain sorbitan, then esterified with oleic acid to obt...

AI Technical Summary

Problems solved by technology

[0011] Fourth, the ester content formed by other fatty acids in the oleic acid used and sorbitan is high, which is 20%-30%, which has limitations in pharmaceutical application;

[0012] Fifth, the obtained polysorbate-80 (I) has poor color and does not meet the requirements of pharmaceutical applications (such as being used for injections);

[0013] Sixth, the plasticity of the production operation is poor, and the product quality is not easy to control

[0014] Some different traditional Chinese medicine injections had the same serious side effects in clinical use, most of which were caused by the low purity of polysorbate-80 in the excipients

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