Method for preparing antimalarial active compound artemisinin through direct column chromatography

Abstract

The invention relates to a method for preparing an antimalarial active compound artemisinin through direct column chromatography and belongs to the field of drug preparation techniques. The method comprises the steps of: weighing 1 part (by weight) of artemisia annua leaf powder which is sieved by a sieve with the particle size of 100 meshes, weighing 0.7-1.4 parts (by weight) of silica gel or alumina which is sieved by a sieve with the particle size of 80-100 meshes, mixing the artemisia annua leaf powder and the silica gel or alumina, and grinding uniformly; coating the substance, obtained in the last step, in a glass chromatography column containing 0.8-5.0 parts (by weight) of silica gel or alumina which is sieved by the sieve with the particle size of 80-100 meshes, eluting in a manner that petroleum ether-ethyl acetate, or petroleum ether-acetone, or chloroform-acetone, or chloroform-ethyl acetate or the like, which are in the volume ratio of 85: (10-20), serve as a moving phase, and collecting fractions; and carrying out depressurized concentration on a fraction containing artemisinin, and crystallizing by using petroleum ether, thereby obtaining white needle-shaped artemisinin crystals. Compared with the prior art, the method has the advantages that the extraction and purification process for artemisinin is optimized, the solvent extraction operating steps and the types of used solvents are reduced, and the consumption of the solvents is reduced; and the obtained product has the advantages of stable quality, high yield, low cost and short consumed time.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and relates to the extraction of biologically active compounds from plants, in particular to the extraction of antimalarial active compound artemisinin from Compositae plant Artemisia annua L. Background technique [0002] Artemisinin is a sesquiterpene lactone compound containing peroxy groups isolated and identified by Chinese scientists from Artemisia annua in the 1970s. It is used to treat diseases such as falciparum malaria and chloroquine-resistant malaria. Quick-acting and low-toxic, it is the most popular antimalarial specific drug after chloroquine, pyrimethamine, primaquine and sulfa (Artemisinin Structure Research Collaborative Group, Science Bulletin, 1977, 22: 142). Especially for cerebral malaria and anti-chloroquine malaria, it has the characteristics of quick action and low toxicity, and has become the first choice drug for the prevention and treatment of malaria reco...

AI Technical Summary

Problems solved by technology

[0004] The previous extraction and separation methods of artemisinin were organic solvent extraction, supercritical CO 2 Extraction, etc., need to go through separation processes such as distribution, column chromatography, and recrystallization to obtain pure artemisinin. Sherei MM, J Nat Prod, 1990, 53(6): 1560-1564; Lapkin AA, Plucinski PK, Cutler M, J Nat Prod, 2006, 69(11): 1653-1664)

So far, there is no report of obtaining artemisinin directly from Artemisia annua without extraction process

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