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Preparation method of artemether drop pills for treating malaria

A technology for treating malaria and artemether, which is applied in the directions of pill delivery, medical preparations with non-active ingredients, and medical preparations containing active ingredients, 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 artemether tablets, artemether capsules, and artemether soft capsules (capsules). The peak value of blood drug concentration greatly affects the oral bioavailability, and thus also affects the competition of curative effect. The competition of artemisinin antimalarial drugs in the international market is very fierce. At present, the focus of competition has changed from raw materials to Transformed into finished medicine, the characteristics of drop pills have a strong advantage in the competition of finished medicine

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] The main drug artemether 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 artemether, stir evenly, add the prescribed amount of polyethylene glycol 6000, raise the temperature of the water bath to 85-90°C, Stir evenly, keep warm for 20 minutes, use a 0.8-1.1mm caliber dropping pill machine, drop into the methyl silicone oil coolant at 5-10°C, filter the methyl silicone oil, shake it off, and dry it in the air. Each pill weighs 35-60mg.

Embodiment 2

[0016] The main drug artemether 100 parts

[0017] Macrogol 400 50 parts

[0018] Polyethylene glycol 6000 250 parts

[0019] Operation: Fully mix the prescribed amount of polyethylene glycol 400 and the prescribed amount of artemether, place it on a water bath at 85-90°C, add the prescribed amount of polyethylene glycol 6000, stir evenly, keep warm for 15 minutes, and use 0.8 - Drop into the liquid paraffin coolant at 5-10°C with a 1.1mm caliber dropping pill machine, 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 artemether 100 parts

[0022] Poloxamer 250 parts

[0023] Operation: Melt the prescribed amount of poloxamer on a 70-80°C water bath, add the prescribed amount of artemether, stir well, keep warm for 20 minutes, and drop 5-10 ℃ in the methyl silicone oil coolant, 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 relates to a preparation method of a chemical drug preparation for treating malaria which is artemether dropping pills. The preparation method has the advantages that: 1. compared with tablets, capsules and soft capsules of the normal-release preparations, the disintegration time limit is greatly shortened, and the onset of action is rapid; 2. water-soluble excipients are used for the full dispersing non-water-soluble main drug, thus being conductive to the absorption of the main drug and improving the oral bioavailability; 3. the dropping pills of the invention can be swallowed, carried out the sublingual administration and directly absorbed by sublingual mucosal veins, thus avoiding the first-pass effect of the stomach, rapidly achieving the peak value of the plasma-drug concentration, having rapid onset of action and improving the efficacy; 4. as the dropping pills of the invention have rapid absorption, the stagnation time in the stomach is short, and the dropping pills can further reduce the generation of drug resistance and other side effects; 5. the production process is simple, the production period is short, and the cost can be lowered; 6. the dropping pills can not only overcome the inconvenient usage of the intravenous drug delivery, but also can overcome the shortcoming of low bioavailability of other oral normal-release preparations.

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): A61K31/357A61K9/20A61K47/34A61P33/06A61K47/10
CPCY02A50/30
Inventor 孔伶俐魏吉城
Owner TIANJIN DANXI TCM INST
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