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Process for isolating srtemisinin from artemisia annua

A technology of absinth and Artemisia annua, applied in the field of absinth isolation, can solve problems such as lack, increased production costs, and inconvenience

Inactive Publication Date: 2005-06-15
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Then most of the methods use chromatography to obtain absinthin, which is the main factor that leads to higher production costs
[0012] Therefore, it can be seen from the above that the above-mentioned conventional methods for obtaining absinthin obviously have inconvenience and defects in actual use, and those that can be improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Selection of Absinin Extraction Solvents

[0053] Different solvents were tested for the extraction of absincin in order to choose the most efficient one. In separate tubes, 10 g of dried powdered leaves of Artemisia annua were extracted with methanol, 20% aqueous methanol, ethanol, 20% aqueous ethanol or hexane as solvents. 10 ml of solvent was removed from the tubes at extraction times of 2, 4 and 6 hours, respectively. Fractions were evaporated to dryness on a water bath, extracts were dissolved in 2ml of solvent and stained (5[mu]l) and loaded on TLC plates and dissolved together with pure absincin in 1mg / ml of the respective solvent. Complete saturation of TLC with hexane as mobile phase In a glass TLC tank: diethyl ether (1:1), plate height 15 cm. Drying and staining of the board was then evident by immersing the board in a developer (glacial acetic acid:sulfuric acid:anisaldehyde, 50:1:0.5), followed by heating the board to 110°C for 15 minutes until the absinc...

Embodiment 2

[0056] Isolation of absincin

[0057] Pure absinthin (0.2 g) was dissolved in separate tubes containing a 1:1 (v / v) mixture of two immiscible solvents, hexane and ethanol in water, varying the concentration of ethanol from 20 to 80%. . After absinthin is completely dissolved in the mixture, use a separating funnel to separate hexane and ethanol into two layers. The percentages of absincin content in individual layers were tested from different test tubes by TLC analysis in Example 1 and the results are summarized in Table 2.

[0058] Separated solvent (1:1 v / v)

[0059] This example suggests that absinthin can be selectively switched from an ethanol extract of Artemisia annua to hexane by maintaining a high ratio. From the hexane fraction, absinthin can be directly crystallized via known evaporative crystallization methods.

Embodiment 3

[0061] Dry powder leaves of Artemisia annua (100 g) were extracted by continuous filtration using 600 ml of ethanol at a temperature of 30°C over four hours. The extraction procedure was repeated four times using the same solvent ratios. The combined extracts were concentrated under vacuum to a volume of 50 ml, then water was added to the concentrated extract to bring the volume to 250 ml. It was then separated four times with 250 ml of hexane. The combined hexane layers were reduced to 5% of their original volume under vacuum and a dark green oily liquid formed. 20% v / v ethyl acetate was mixed into the liquor followed by treatment with 1% w / v activated charcoal. The liquor was filtered through a piece of 3 mm Waterman filter paper to remove activated charcoal. The dark yellow liquid was crystallized by evaporation after filtration. After evaporation and crystallization, the liquid is white, and the needle crystals are separated by a vacuum filter and weighed. The final y...

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Abstract

The present invention relates to a process for the isolation of artemisinin, an antimalarial agent from the herb of the Artemisia annuaplant, comprising of extracting the herb with ethanol, partitioning of thextract between water and hexane, followed by evaporative crystallization of artemisinin from hexane phase to produce substantially pure artemisinin.

Description

technical field [0001] The present invention relates to a method for isolating absinthin, especially an antimalarial drug isolated from Artemisia annua herb, which comprises extracting the herb with ethanol, separating the extract between water and hexane, followed by Evaporative crystallization of absincin from the hexane phase yields substantially pure absinin. Background technique [0002] Absincin is a peroxide of sesquitenolactone, which has antimalarial activity (KlaymanDL, 1985, Science 228, 1049). According to clinical studies, absinthin and its semi-synthetic derivatives such as artemether, artesunate, and arteether have been used in the treatment of malaria, which includes severe complex, drug-resistant, and brain-invasive diseases. malaria. Absincin and its derivatives are structurally different from general antimalarial agents, so there is no problem of drug resistance and transfer of drug resistance. Recently, it has been reported that absincin can be produce...

Claims

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Application Information

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IPC IPC(8): C07D493/22A61K31/357A61K31/365A61K36/00A61K36/28A61K36/282A61P33/06G11C16/04G11C16/34
CPCA61K31/365A61K36/282A61P33/06
Inventor 撒戌耳·库马夕夫·库马·格柏塔迪格维札·辛玛诞·莫旱·格柏塔哈兰·常得·展阿度·巴拉喀戌·喀侯苏曼·皮特·辛·旱奴贾枸文德·朗
Owner COUNCIL OF SCI & IND RES
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