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Preparation method of dihydroartemisinin liquid preparation

A technology of dihydroartemisinin and liquid preparations, which is applied in the field of medicine to achieve the effects of improving water solubility, improving anti-tumor effect, and improving dispersion

Inactive Publication Date: 2010-06-16
林杨
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide a method for effectively improving the solubility of dihydroartemisinin, to solve the problem that it is difficult to dissolve in water, and to clear the way for its clinical anti-tumor application

Method used

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  • Preparation method of dihydroartemisinin liquid preparation

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Embodiment 1

[0012] 1. Preparation of DHA solution: Accurately weigh 20 mg DHA in a glass test tube, add 1 ml DMSO, shake vigorously to make it fully dissolved; then slowly add ethanol with a concentration of 88% (V / V), shake well while adding, Make the total volume to 4ml; finally, add polyethylene glycol 400, shake well while adding, until the total volume is 10ml, at this time the concentration of DHA solution is 2mg / ml. The formulation is miscible with water in any proportion. Accurately draw 200ul of DHA solution and add it to 3.8ml of 1640 medium containing 15% fetal bovine serum and dilute it into medium A containing DHA 100ug / ml; take 2ml of medium A and add it to 2ml of 1640 medium containing 15% fetal bovine serum , mix well to obtain medium B containing DHA 50ug / ml; take 2ml medium B and add it to 2ml 1640 medium containing 15% fetal bovine serum, mix well to obtain medium C containing DHA 25ug / ml; Take 2ml of medium C and add it into 2ml of 1640 medium containing 15% fetal bov...

Embodiment 2

[0017] Accurately weigh 20mg of DHA in a glass test tube, add 1ml of DMSO, shake vigorously to make it fully dissolved; then slowly add ethanol with a concentration of 90% (V / V), shake well while adding, to bring the total volume to 3ml ;Finally, add polyethylene glycol 400, shake well while adding, until the total volume is 20ml, at this time the concentration of DHA solution is 1mg / ml. The formulation is miscible with water in any proportion.

Embodiment 3

[0019] Accurately weigh 20mg DHA in a glass test tube, add 1ml DMSO, shake vigorously to make it fully dissolved; then slowly add ethanol with a concentration of 95% (V / V), shake well while adding, to bring the total volume to 2.5 ml; finally, add polyethylene glycol 400, shake well while adding, until the total volume is 8ml, at this time the concentration of DHA solution is 2.5mg / ml. The formulation is miscible with water in any proportion.

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Abstract

The invention discloses a preparation method of a dihydroartemisinin liquid preparation, which belongs to the field of medicine. The preparation method comprises the following steps: firstly, dissolving dihydroartemisinin into dimethyl sulfoxide, then adding ethanol and polyethylene glycol 400 and further diluting the dihydroartemisinin to obtain the dihydroartemisinin liquid preparation which can be mixed and dissolved with water in any proportion. Because of enhancing the dispersion degree of the dihydroartemisinin greatly, the water solubility of the dihydroartemisinin liquid preparation is obviously enhanced. The dihydroartemisinin liquid preparation is used as an anti-tumour preparation and can obviously suppress the growth and the multiplication of the cells of a leukaemia cell strain K562 which is cultured in vitro, so that the anti-tumour effect of the dihydroartemisinin liquid preparation is obviously enhanced.

Description

technical field [0001] The invention relates to a method for preparing a dihydroartemisinin liquid preparation, which belongs to the field of medicine. Background technique [0002] Artemisinin is my country's first monomer-type new drug with independent intellectual property rights. It is a sesquiterpene lactone monomer containing peroxy groups isolated from Artemisia annua. After artemisinin, my country has successfully developed three new drugs of the first class, artesunate, artemether and dihydroartemisinin, and is in the leading position in the research and application of this field in the world. These drugs have the functions of anti-malarial, anti-schistosomiasis, anti-pregnancy, and immune regulation. The research on its mechanism of action has also made great progress. Taking the antimalarial effect as an example, after Plasmodium phagocytizes hemoglobin, under the catalysis of Plasmodium hemoglobin, mainly aspartic protease, cysteine ​​protease, etc., the hemogl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/357A61K47/34A61P33/06A61K47/10
Inventor 夏庆杰李启杰杨林徐成达
Owner 林杨
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