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Thermally-stable sweet wormwood solid dispersion composition and preparation method thereof

A technology of solid dispersion and composition, applied in the field of artemisinin solid dispersion composition and preparation, can solve problems such as poor stability of artemisinin, and achieve the effect of improving thermal stability

Inactive Publication Date: 2013-04-03
CHONGQING PHARMA RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is found that the stability of artemisinin is not very good. Therefore, there is a need for a more stable artemisinin derivative composition that is more suitable for storage in a hotter African environment.

Method used

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  • Thermally-stable sweet wormwood solid dispersion composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Dissolve 50g of artesunate, 150g of sorbitol, 2.5g of thiourea, and 0.12g of disodium ethylenediaminetetraacetic acid in a mixed solvent of 5L of acetone: water (4:1), spray dry directly, and collect the powder , Plus 100 g of microcrystalline cellulose, 6 g of sodium starch glycolate, and 2 g of magnesium stearate, and directly compress the tablets to obtain 1000 artesunate-containing tablets.

Embodiment 2

[0036] Dissolve 50g of dihydroartemisinin, 500g of xylitol, 2.5g of thiourea, and 0.1g of disodium ethylenediaminetetraacetic acid in a mixed solvent of 10L ethanol: water (9:1), spray dry directly, and collect Powder is added, 100g starch is added, and the capsule is directly filled to obtain 1,250 capsules containing dihydroartemisinin.

Embodiment 3

[0038] Dissolve artemether 50g, mannitol 500g, thiourea 0.5g, and diethylenetriaminepentaacetic acid 0.2g in a mixed solvent of 1L acetone: water (4:1), spray dry directly, collect the powder, and add sucrose 100g, mix well, add 30g of water to granulate, dry, and directly bag the collected granules to obtain 1250 bags of arteether granules.

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Abstract

The invention relates to a thermally-stable sweet wormwood solid dispersion composition and a preparation method thereof. The invention is characterized in that the composition contains at least one kind of an effective amount of the sweet wormwood anti-malaria medicaments, an anti-oxidant and a solid dispersion material, wherein a ratio of the sweet wormwood derivatives and the solid dispersion accessory is 1 : 0.5 to 1 : 10, the anti-oxidant is thiourea, and a metal chelating agent is randomly added. The solid dispersion composition is high in stability, and can be transported and stored at places with relatively high temperature.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a heat-stable Artemisia annua solid dispersion composition and a preparation method, and the solid dispersion composition contains at least one effective amount of Artemisia annua derivatives, an antioxidant, a solid Dispersion material, wherein the antioxidant is thiourea. The solid dispersion composition of the present invention has significantly improved thermal stability, and can be stored for more than 12 months under the condition of 30 degrees. 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 populatio...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/48A61K31/366A61K31/357A61K45/00A61K47/20A61K47/18A61P33/06
CPCY02A50/30
Inventor 王海屿张涛张林枝樊斌
Owner CHONGQING PHARMA RES INST
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