Artemisinin/artemisinin derivative solid dispersion as well as preparation method and application thereof

A technology of artemisinin derivatives and solid dispersion, which is applied in the field of medicine to achieve high solubility and improve solubility

Pending Publication Date: 2022-05-06
CHONGQING ACAD OF CHINESE MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on the solid dispersion of artemisinin and its derivatives

Method used

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  • Artemisinin/artemisinin derivative solid dispersion as well as preparation method and application thereof
  • Artemisinin/artemisinin derivative solid dispersion as well as preparation method and application thereof
  • Artemisinin/artemisinin derivative solid dispersion as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0033] 3, measure the preparation method of solubility need testing solution

[0034] Take the raw material drug and the solid dispersion preparation, put them in a 5mL centrifuge tube, add about 3mL of water, shake on a shaker at 37°C at 150r / min for more than 12 hours, and filter through a 0.22μm filter membrane.

[0035] 4. The stability of raw materials at different temperatures and times

[0036] The raw materials of artemisinin and dihydroartemisinin were taken respectively, and samples were taken at different temperatures and at different time points to determine the stability of artemisinin and dihydroartemisinin. Results The content of artemisinin was basically stable when heated at 80°C for 6 hours, and the content of dihydroartemisinin was unstable at 80°C. Although the content measurement results showed no obvious change, it had turned pale yellow after heating for 6 hours; 60°C and 70°C When heated at ℃ for 8 hours, artemisinin and dihydroartemisinin were relativ...

Embodiment 1

[0039] Embodiment 1: the preparation of solid dispersion preparation and the mensuration of solubility

[0040] 1. Process comparison of solid dispersion prepared by solvent method

[0041] 1.1, the choice of solvent

[0042] The carrier materials selected in this study (F68, PVP10, PEG2000, PEG4000, PEG6000, PVP K30) were all easily soluble in absolute ethanol. Based on solvent toxicity and cost considerations, absolute ethanol was selected as the solvent, and the drying method was 12 hours under reduced pressure at 60°C.

[0043] 1.2. Comparison of excipient types and excipient-drug ratio

[0044] The saturated solubility of artemisinin in water is used as the evaluation index, and the types of excipients and the ratio of excipients to drugs are compared. The results are shown in image 3 , the results of different excipients and ratios showed that the drug-adjuvant ratio was 1:1, and the solubility of the solid dispersion was the best, and the solubility of the solid dis...

Embodiment 2

[0057] Example 2: IR Characterization of Artemisinin and Dihydroartemisinin Solid Dispersions

[0058] Take artemisinin API, dihydroartemisinin API, poloxamer 188, artemisinin + poloxamer 188 physical mixture, dihydroartemisinin + poloxamer 188 physical mixture, artemisinin The solid dispersion sample and the dihydroartemisinin solid dispersion sample were subjected to IR measurement, and the results are shown in Figure 6-12 .

[0059] Depend on Figure 6-12 It can be seen that the physical mixture of artemisinin and dihydroartemisinin raw materials and excipients is a physical superposition of raw materials and excipients, and the IR spectrum of the solid dispersion preparation shows no new peaks, indicating that the raw materials and excipients have not interacted.

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Abstract

The invention relates to the technical field of medicines, and discloses an artemisinin / artemisinin derivative solid dispersion as well as a preparation method and application thereof. The solid dispersion comprises artemisinin and / or an artemisinin derivative as an active drug, and poloxamer as an auxiliary material. The solid dispersion suitable for the artemisinin / artemisinin derivative is prepared by taking poloxamer as an auxiliary material, the solid dispersion enables the artemisinin / artemisinin derivative to have high solubility, and compared with artemisinin and artemisinin derivative raw material medicines, the solubility is improved by 1.18 times and 2.17 times respectively, and the solid dispersion can be used for preparing the artemisinin / artemisinin derivative. And the IR spectrum of the solid dispersion shows that the bulk drug and the auxiliary material poloxamer do not react with each other, and the solid dispersion provided by the invention improves the solubility of the artemisinin and the derivatives thereof in water, and provides a foundation for the development of pharmaceutical preparations thereof.

Description

technical field [0001] The present application relates to the field of medical technology, in particular to a solid dispersion of artemisinin / artemisinin derivatives and its preparation method and application. Background technique [0002] Artemisinin is a compound with antimalarial activity isolated from the traditional Chinese medicine Artemisia annua. It has a unique peroxy group-containing sesquiterpene lactone structure and shows good curative effect on various types of malaria, especially resistant malaria. . Artemisinin is a colorless needle-like crystal with the molecular formula C 15 h 22 o 5 , with a molecular weight of 282.34, easily soluble in ethyl acetate, chloroform, acetone, benzene and glacial acetic acid, soluble in ether, petroleum ether, ethanol and methanol, but almost insoluble in water, with a melting point of 156-157°C. Artemisinin is the preferred high-efficiency drug for human antimalarial in the long term, but its poor water solubility limits t...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/10A61K47/32A61K31/366A61K31/357A61P33/06
CPCA61K9/146A61K31/366A61K31/357A61P33/06Y02A50/30
Inventor 王云红杨炀高思佳阳勇郭延垒张小梅花雷王计瑞魏江平秦伟瀚杨大坚陈敬财程磊
Owner CHONGQING ACAD OF CHINESE MATERIA MEDICA
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