Method for purifying lipstatin

Abstract

The invention provides a method for purifying lipstatin. The method comprises the steps that step one, a high-polarity solvent extraction solution containing the lipstatin is obtained; step two, inorganic salt, a low-polarity solvent and tertiary amine compounds are added into the extraction solution, and stirring, standing and extraction and solution separation are conducted; step three, a high-polarity solvent is added for backflushing of a low-polarity solvent phase of the upper middle layer after the extraction and solution separation in the step two, and stirring, standing and extractionand solution separation are conducted; step four, an acid aqueous solution is added for backflushing of the low-polarity solvent phase of the upper middle layer after the extraction and solution separation in the step three, stirring, standing and extraction and solution separation are conducted, and a low-polarity solvent extraction phase of the upper layer of the lipstatin is obtained. Accordingto the method for purifying the lipstatin, impurities can be easily separated and removed through solution separation of the high-polarity solution and the low-polarity solution, the product is not easily damaged, and the yield is high; the operation is simple, the requirements for equipment are low, and the convenience is provided for industrial automatic continuous production; the production period can be greatly shortened, and the production cost is reduced.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a method for purifying lipstatin. Background technique [0002] Lipstatin is a metabolite of Streptomyces toxytricini, which can selectively inhibit the activity of pancreatic lipase in the gastrointestinal tract, reduce the decomposition and absorption of fat, and its tetrahydro derivative orlistat It has been successfully developed as a weight loss drug - Xenical, which is currently the only drug for the treatment of obesity marketed as a non-central nervous system effect. [0003] Chinese patent CN101775416A discloses a method for purifying lipstatin, wherein the lipstatin-containing fermentation liquid is extracted with 60-85% ethanol aqueous solution, then phase-inverted into n-heptane, concentrated under reduced pressure and then It was extracted with acetonitrile, deoiled, backwashed, concentrated under reduced pressure, and then subjected to silica gel column chromatog...

AI Technical Summary

Problems solved by technology

The process as a whole has a long production cycle, complex process and low efficiency

[0005] Therefore, the current purification methods of lipstatin are all purely physical methods, and the impurities are not removed according to the specific chemical characteristics of the impurities in lipstatin, resulting in low separation efficiency, which is very low in efficiency in industrial scale production, and costs stay high

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