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Preparation method of dihydroartemisinin drop pills for treating malaria

A technology for dihydroartemisinin and malaria treatment, which is applied in the direction of pill delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of long disintegration time and difficulty in rapidly reaching blood drug concentration peak value, inconvenient use, etc.

Inactive Publication Date: 2008-11-26
TIANJIN DANXI TCM INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, injections were still used as the main dosage form in the past, and the inconvenience of use was its main disadvantage.
Oral preparations include dihydroartemisinin tablets, the main disadvantage of which is that the disintegration time is long, due to its insoluble nature, it is not easy to absorb, the onset is slow, and it is difficult to quickly reach the peak blood concentration, which greatly affects the oral biomedicine. Utilization, thus also affects the curative effect. Artemisinin-type antimalarial drugs are very competitive in the international market. At present, the focus of competition has changed from raw materials to finished drugs. Occupy a strong advantage in land competition

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] The main drug dihydroartemisinin 100 parts

[0012] Macrogol 4000 50 parts

[0013] Polyethylene glycol 6000 200 parts

[0014] Operation: Melt the prescribed amount of polyethylene glycol 4000 on a water bath at 60-65°C, add the prescribed amount of dihydroartemisinin, stir evenly, add the prescribed amount of polyethylene glycol 6000, and raise the temperature of the water bath to 85-90°C ℃, stir evenly, keep warm for 20 minutes, drop into the methyl silicone oil coolant at 5-10 ℃ with a 0.8-1.1mm caliber dropping pill machine, filter out the methyl silicone oil, shake it off, and dry it in the air. Each pill weighs 35-60mg.

Embodiment 2

[0016] The main drug dihydroartemisinin 100 parts

[0017] Macrogol 400 50 parts

[0018] Polyethylene glycol 6000 250 parts

[0019] Operation: Fully mix the prescribed amount of polyethylene glycol 400 with the prescribed amount of dihydroartemisinin, place it on a water bath at 85-90°C, add the prescribed amount of polyethylene glycol 6000, stir evenly, and keep warm for 15 minutes. Use a 0.8-1.1mm caliber drop pill machine to drop into the liquid paraffin coolant at 5-10°C, filter off the liquid paraffin, shake it off, dry it in the air, and get it. The weight of each pill is 35-60mg.

Embodiment 3

[0021] The main drug dihydroartemisinin 100 parts

[0022] Poloxamer 250 parts

[0023] Operation: Melt the prescribed amount of poloxamer in a water bath at 70-80°C, add the prescribed amount of dihydroartemisinin, stir well, keep warm for 20 minutes, and drop 5 In the methyl silicone oil coolant at -10°C, filter the methyl silicone oil, shake it off, and dry it in air to obtain the product. The weight of each pill is 35-60mg.

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PUM

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Abstract

The invention discloses a preparation method for dihydro artemisinine pill that is a chemical preparation used for curing malaria. The preparation method has the advantages that (1) compared with common-released preparation tablets, capsules and soft capsules, disintegration time limit is greatly shortened and effect taking is fast; (2) water-soluble accessories are used, which completely disperses water-insoluble principal medicine, thus being helpful for the absorption of the principal medicine and being capable of improving peroral biological availability; (3) the pill of the invention can be taken in ways of deglutition and sublingual buccal and can be directly absorbed by the veins of sublingual mucous coat, thus avoiding the first-pass effect of a stomach, achieving the peak value of blood concentration quickly, taking effect fast and improving curative effect; (4) as the pill of the invention has fast absorption and short detention time in the stomach, thereby reducing the occurrence of side effects such as drug resistance, and the like; (5) the pill of the invention has simple production technique and short production period and can lower cost; (6) the pill of the invention overcomes the use inconvenience of intravenous drug administration as well as the defect that the biological availability is low caused by taking other common-released preparations orally.

Description

Technical field: [0001] The invention belongs to a chemical medicine preparation, in particular to a chemical medicine preparation for treating malaria. Background technique: [0002] Malaria is a very old disease with rapid onset and rapid spread, making it difficult to control for a while. In the past, the incidence rate was very high in all parts of the world, especially in tropical and subtropical regions. Now malaria has been basically eliminated in many countries, but it is still a serious epidemic infectious disease in South Asia, the Middle East, Africa and Southeast Asian countries. Hundreds of thousands, if not millions, of people died from malaria. Timely and effective treatment of malaria and effective control of the spread of malaria in these countries and regions is still a top priority, and it is the duty-bound task of the governments of these countries and regions. The United Nations and the World Health Organization also pay great attention to the treatment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/357A61K47/34A61K47/44A61P33/06A61K47/06A61K47/10
CPCY02A50/30
Inventor 孔伶俐魏吉城
Owner TIANJIN DANXI TCM INST
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