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Compound three-segment pin of hydrochloric acid amodiaquine and artesunate

A technology of amodiaquine hydrochloride and artesunate, which can be applied in the directions of drug combination, suppository delivery, organic active ingredients, etc., can solve the problems of increased resistance of wild artemisia annua amodiaquine hydrochloride and the like

Active Publication Date: 2008-01-23
FRONT PHARM PLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The biggest challenge that mankind will face is the shortage of wild Artemisia annua and the increase of drug resistance of amodiaquine hydrochloride in some areas

Method used

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  • Compound three-segment pin of hydrochloric acid amodiaquine and artesunate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Formula composition and the amount of ingredients:

[0039] Upper layer: Amodiaquine Hydrochloride 98g

[0040] Stearin 550g,

[0041] Middle layer: food coloring red 40 (FD&C Red40) 0.1g

[0042] Hard fat 450g,

[0043] Bottom: Artesunate 25g

[0044] Stearin 930g,

[0045] A total of 1000 capsules (2g per capsule) were made, specification: 75mg: 25mg.

[0046] The specific preparation process is as follows:

[0047] (1) Prepared with a double-layer suppository mold with a 0.5ml quantitative addition device.

[0048] (2) Amodiaquine hydrochloride and artesunate were respectively crushed through a 100-mesh sieve for later use.

[0049] (3) After melting the stearin in a water bath at 60°C, add amodiaquine hydrochloride under continuous stirring to fully suspend it, pour into the lower mold, refrigerate at about 10°C for 10 minutes, and assemble the upper mold.

[0050] (4) After melting the stearin in a water bath at 60°C, add the r...

Embodiment 2

[0054] Upper layer: Amodiaquine Hydrochloride 196g

[0055] Hard fat 500g,

[0056] Middle layer: food coloring red 40 (FD&C Red40) 0.1g

[0057] Hard fat 450g,

[0058] Lower layer: Artesunate 50g

[0059] Stearin 900g,

[0060]A total of 1000 capsules (2g per capsule) were made, specification: 150mg: 50mg.

Embodiment 3

[0062] Formula composition and the amount of ingredients:

[0063] Upper layer: Amodiaquine Hydrochloride 98g

[0064] Hard fat 350g,

[0065] PEG-4000 200g,

[0066] Middle layer: food coloring red 40 (FD&C Red40) 0.1g

[0067] Hard fat 350g,

[0068] PEG-4000 100g,

[0069] Bottom: Artesunate 25g

[0070] Hard fat 630g

[0071] Polyoxyethylene [40] 300g,

[0072] A total of 1000 capsules (2g per capsule) were made, specification: 75mg: 25mg.

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Abstract

The invention relates to a compound abrotanum formulation, in particular to an amodiaquine hydrochloride and artesunate three section suppository, which has the formulation that: amodiaquine hydrochloride and stearin are arranged at the upper layer; food dye red color No. 40 and stearin are arranged in the middle layer; artesunate and stearin are arranged in the lower layer. The combination of the amodiaquine hydrochloride and the artesunate prevents the generation of drug resistance of malarial parasite and greatly improves the healing efficiency and cure rate. Besides, with the advantage of fast absorption and quick effect in suppository, the invention can be best applied to children and patients suffering from dysphagia. By avoiding the first-pass effect in rectal administration and realizing fast effect, the suppository is usually taken as first-aid medicine for patients suffering from serious malaria. Therefore, the suppository can be promoted in remote area to ensure timely and effective anti-malaria treatment, thus realizing outstanding advantage for countries in the third world.

Description

technical field [0001] The invention relates to a compound artemisinin preparation, specifically a three-section suppository compounded with amodiaquine hydrochloride and artesunate. Background technique [0002] Compound artemisinin preparation is currently the most effective antimalarial drug, its cure rate for malaria treatment can reach 95%, and its onset time is shorter than artemisinin single preparation. [0003] Humans have had the painful lesson of being defeated by malaria parasites. For example, the once-popular antimalarial drug chloroquine is now ineffective in most parts of the world. Sulfadoxine-pyrimethamine has been widely used since it entered Thailand in 1977, but its efficacy has dropped by 90% within 5 years. The antimalarial drug atovaquone has been on the market since 1997, and it took only one year for drug resistance to develop. [0004] Kochi, director of WHO's malaria treatment department, said: "We can't repeat the mistakes of the past. The onl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/4706A61K31/357A61P33/06
CPCY02A50/30
Inventor 江浩舟孙松刘斐罗传国曹玉明
Owner FRONT PHARM PLC
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