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Dihydroartemisinin piperaquine tablet and preparation method thereof

A technology of dihydroartemisinin and piperaquine tablets, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients. cumbersome process and other issues, to achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2021-07-02
南京致中生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound artemisinin-like piperaquine pellets prepared by this technology have regular shape, good molding and roundness, good fluidity, unaffected dissolution rate, and mask the bitter taste. Slow, only about 40% of dihydroartemisinin and piperaquine phosphate dissolve in 15 minutes, and it is difficult to take effect quickly

Method used

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  • Dihydroartemisinin piperaquine tablet and preparation method thereof
  • Dihydroartemisinin piperaquine tablet and preparation method thereof
  • Dihydroartemisinin piperaquine tablet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0051] A kind of preparation method of dihydroartemisinin-piperaquine tablet in the present embodiment, comprises the steps:

[0052] 1) Solid dispersion

[0053] Form a solution of the solvent hydrophilic matrix, surfactant and co-solvent at 60°C, keep warm at 40°C, add the prescribed amount of hydrogen artemisinin and piperaquine phosphate in sequence, stir until dissolved, and cool the obtained hot mixture , and dried the obtained solid dispersion at a temperature of 35 to 40°C.

[0054] 2) Preparation of dihydroartemisinin-piperaquine tablets

[0055] Put the solid dispersion and colloidal silicon dioxide of the prescribed amount into a low-shear V-shaped mixer and mix for 10 minutes, then put the prescribed amount of cellulose lactose and sodium carboxymethyl starch into the low-shear V-shaped mixer for Mix, mix 30min, add the magnesium stearate of recipe quantity, then mix in the low-shear V-type mixer, mix 5min, the mixed powder obtained is poured into the mold of sha...

Embodiment 2

[0059] A kind of preparation method of dihydroartemisinin-piperaquine tablet in the present embodiment, comprises the steps:

[0060] 1) Solid dispersion

[0061] Form a solution of the solvent hydrophilic matrix, surfactant and co-solvent at 60°C, keep warm at 40°C, add the prescribed amount of hydrogen artemisinin and piperaquine phosphate in sequence, stir until dissolved, and cool the obtained hot mixture , and dried the obtained solid dispersion at a temperature of 35 to 40°C.

[0062] 2) Preparation of dihydroartemisinin-piperaquine tablets

[0063] Put the solid dispersion and colloidal silicon dioxide of the prescribed amount into a low-shear V-shaped mixer and mix for 10 minutes, then put the prescribed amount of cellulose lactose and sodium carboxymethyl starch into the low-shear V-shaped mixer for Mix, mix 30min, add the magnesium stearate of recipe quantity, then mix in the low-shear V-type mixer, mix 5min, the mixed powder obtained is poured into the mold of sha...

Embodiment 3

[0067] A kind of preparation method of dihydroartemisinin-piperaquine tablet in the present embodiment, comprises the steps:

[0068] 1) Solid dispersion

[0069] Form a solution of the solvent hydrophilic matrix, surfactant and co-solvent at 60°C, keep warm at 40°C, add the prescribed amount of hydrogen artemisinin and piperaquine phosphate in sequence, stir until dissolved, and cool the obtained hot mixture , and dried the obtained solid dispersion at a temperature of 35 to 40°C.

[0070] 2) Preparation of dihydroartemisinin-piperaquine tablets

[0071] Put the solid dispersion and colloidal silicon dioxide of the prescribed amount into a low-shear V-shaped mixer and mix for 10 minutes, then put the prescribed amount of cellulose lactose and sodium carboxymethyl starch into the low-shear V-shaped mixer for Mix, mix 30min, add the magnesium stearate of recipe quantity, then mix in the low-shear V-type mixer, mix 5min, the mixed powder obtained is poured into the mold of sha...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a method for preparing a solid dispersion by mixing dihydroartemisinin and piperaquine phosphate through combination of a solid dispersion method and a surfactant addition method and developing the solid dispersion into tablets, and the solid dispersion tablets prepared by the method disintegrate rapidly in water or gastric juice under the combined action of a disintegrating agent, the hydrophilic matrix is dissolved, the drug molecules are dissolved, the supersaturated state is formed in the aqueous medium without precipitation, and the two drugs are rapidly dissolved in the gastric emptying time so as to improve the bioavailability of the drugs.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dihydroartemisinin-piperaquine tablet and a preparation method thereof. Background technique [0002] Malaria is currently a serious worldwide epidemic disease. According to the report of the World Health Organization: there are 2 billion people living in malaria-endemic areas in 102 countries around the world, 270 million people suffer from malaria, and about one million people die of malaria every year. In particular, a severe problem currently facing is drug resistance. Plasmodium falciparum has developed resistance to all antimalarial drugs, and the resistance to antimalarial drugs has led to a sharp increase in the number of infected people and more severe and complex generations. malaria, such as cerebral malaria, which has a high mortality rate. Therefore, there is an urgent need to create new antimalarial drugs with new chemical structures. For a long time, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/34A61K47/10A61K47/44A61K31/496A61K31/357A61P33/06
CPCA61K9/2095A61K9/2031A61K9/2013A61K31/496A61K31/357A61P33/06
Inventor 胡健
Owner 南京致中生物科技有限公司
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