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Dihydroartemisinin beta-cyclodextrin inclusion compound, preparation method thereof and antimalarialdrug with same

A technology of cyclodextrin inclusion complex and dihydroartemisinin, which can be applied to medical preparations containing active ingredients, anti-infective drugs, drug combinations, etc. Problems such as public reports of dextrin inclusion, to achieve the effects of improving water-insoluble properties, improving storage conditions, and extending storage validity

Active Publication Date: 2011-01-26
GUILIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many literature reports on the inclusion technology of β-cyclodextrin at home and abroad, but there is no public report on the inclusion of dihydroartemisinin and β-cyclodextrin

Method used

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  • Dihydroartemisinin beta-cyclodextrin inclusion compound, preparation method thereof and antimalarialdrug with same
  • Dihydroartemisinin beta-cyclodextrin inclusion compound, preparation method thereof and antimalarialdrug with same
  • Dihydroartemisinin beta-cyclodextrin inclusion compound, preparation method thereof and antimalarialdrug with same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Preparation of dihydroartemisinin β-cyclodextrin inclusion compound

[0027] Dissolve 0.1g of dihydroartemisinin in 10ml of acetone to obtain a solution of dihydroartemisinin in acetone, set aside, then take 2g of β-cyclodextrin and dissolve it in 110ml of distilled water; Add dihydroartemisinin acetone solution to the aqueous solution, continue to stir for 4 hours, let it stand overnight, evaporate the acetone under reduced pressure, filter, and freeze-dry the filtrate to obtain 1.8 g of white powder, which is dihydroartemisinin β-cyclodextrin package Compound (referred to as dihydroartemisinin inclusion compound), detected by ultraviolet spectroscopy, the content of dihydroartemisinin in the obtained inclusion compound (the ratio of dihydroartemisinin in the inclusion compound) is 5.14 %. The calculated inclusion yield (actually measured content of dihydroartemisinin × yield of inclusion compound ÷ input amount of dihydroartemisinin) is: 92.52%.

[0028] ...

Embodiment 2

[0042] Example 2: Preparation of dihydroartemisinin β-cyclodextrin inclusion compound

[0043] Dissolve 1g of dihydroartemisinin in 120ml of acetone to obtain a solution of dihydroartemisinin in acetone, and then take 60g of β-cyclodextrin and dissolve it in 3333ml of distilled water; Add dihydroartemisinin acetone solution to the saturated aqueous solution of β-cyclodextrin, continue ultrasonication for 1 hour, let it stand overnight, evaporate the acetone under reduced pressure, filter, and freeze-dry the filtrate to obtain a white powder, which is confirmed by thin-layer chromatography to be dihydroartemisinin The hydrogen artemisinin β-cyclodextrin inclusion compound is detected by the ultraviolet spectrum detection method, and the content of dihydroartemisinin in the obtained inclusion compound is 2.01%, and the inclusion rate is 98.89%.

Embodiment 3

[0044] Example 3: Preparation of dihydroartemisinin β-cyclodextrin inclusion compound

[0045] Take 1g of dihydroartemisinin and dissolve it in 150ml of ethanol to obtain dihydroartemisinin ethanol solution, set aside, then take 10g of β-cyclodextrin and dissolve it in 833ml of distilled water; Add dihydroartemisinin in acetone solution, continue to stir for 2h, let it stand overnight, evaporate ethanol under reduced pressure, filter, and dry the filtrate under reduced pressure and low temperature to obtain 9.1g of white powder, which is dihydroartemisinin β-cyclodextrin The clathrate is detected by the ultraviolet spectroscopic detection method, and the content of dihydroartemisinin in the clathrate obtained is 7.53%, and the clathrate yield is 68.52%.

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Abstract

The invention discloses a dihydroartemisinin beta-cyclodextrin inclusion compound, a preparation method thereof and an antimalarialdrug with the inclusion compound. The inclusion compound is composed of dihydroartemisinin and beta-cyclodextrin based on the weight ratio of 1:5-80. The preparation method comprises the following the steps: dissolving the dihydroartemisinin in ethanol or acetone, obtaining a solution for later use, and preparing a beta-cyclodextrin saturated aqueous solution; and adding the dihydroartemisinin ethanol or acetone solution under the stirring condition, then continuously stirring or performing ultrasound for 1 to 4 hours, standing the mixture and passing the night, volatilizing the ethanol or acetone, filtering and drying the filtrate in a freezing mode or a decompression and low temperature mode to obtain the dihydroartemisinin beta-cyclodextrin inclusion compound. Compared with the prior art, in the invention, the inclusion compound is prepared from the dihydroartemisinin and the beta-cyclodextrin, thereby increasing the solubility of the dihydroartemisinin in water greatly, improving the stability of the dihydroartemisinin, and being beneficial for the follow-up operation of the dihydroartemisinin in pharmacy.

Description

technical field [0001] The invention relates to a dihydroartemisinin beta-cyclodextrin inclusion compound, and also relates to a preparation method of the inclusion compound and an antimalarial drug containing the inclusion compound. Background technique [0002] As one of the most dangerous diseases, malaria is still widely prevalent in the world (especially in tropical areas), threatening human health, and the situation is grim. With the intensification of drug resistance and changes in the human living environment, the current malaria epidemic situation is more serious than 30 years ago, involving more than 100 countries, with a population of 3 billion, and 500 million clinically diagnosed cases each year; 90% of them Occurs in Africa, about 7% occurs in India, Brazil, Sri Lanka, Southeast Asia, Colombia and Solomon Islands, the death toll exceeds 1 million, most of them are children under 5 years old in Africa; malaria seriously threatens the economic development of deve...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/357A61K31/675A61P33/06A61K47/61
CPCY02A50/30
Inventor 黄姝华郑清四潘梅
Owner GUILIN PHARMA
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