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Preparation method for compound artemether dripping pill 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: 2008-12-10
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.
There are only tablets for oral preparations, and its main disadvantage is that the disintegration time is long. Due to its insoluble nature, it is not easy to absorb, and its onset is slow. It is difficult to quickly reach the peak blood concentration, which greatly affects the oral bioavailability. also affected the efficacy of

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Main drug benzefantrine 120 parts

[0012] Main drug artemether 20 parts

[0013] Macrogol 4000 50 parts

[0014] Polyethylene glycol 6000 200 parts

[0015] Operation: Melt the prescribed amount of polyethylene glycol 4000 on a water bath at 60-65°C, add the prescribed amount of benzfluorenol, 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 0.4-0.6mm diameter 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 5-15mg. Take it once a day, 2.5g at a time.

Embodiment 2

[0017] Main drug benzefantrine 120 parts

[0018] Main drug artemether 20 parts

[0019] Macrogol 400 50 parts

[0020] Polyethylene glycol 6000 250 parts

[0021] Operation: Fully mix the prescribed amount of polyethylene glycol 400 with the prescribed amount of benzfluorenol, 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 0.4 - Drop into the liquid paraffin coolant at 5-10°C with a 0.6mm 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 5-15mg. Take 2.5g each time, once a day.

Embodiment 3

[0023] Main drug benzefantrine 120 parts

[0024] Main drug artemether 20 parts

[0025] Poloxamer 250 parts

[0026] Operation: Melt the prescribed amount of poloxamer on a water bath at 70-80°C, add the prescribed amount of benzefantrine, 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, dry it in the air, and get it. The weight of each pill is 5-15mg. Take 2.5g each time, once a day.

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Abstract

The invention relates to the preparation of a chemical medicine preparation, which is a compound artemether methyl ether droping pill used for curing malaria. The present invention has the advantages that: 1. Serving as main ingredients, antimalarial lumefantrine and artemether are sufficiently dispersed by water-soluble auxiliary-ingredient polyethylene glycol or poloxamer, thus being favorable for absorbing the main ingredients. 2. The dropping pill preparation can be taken under tongue and also can be swallowed with very short disintegration (dissolve) time limit. And the invitro dissolve quantities are greatly improved and the peak value of the blood concentration can be reached rapidly, thus being beneficial to the improvement of the curative effect; 3. The main ingredients and the auxiliary ingredients are equably mixed at the temperature of 80 to 90 DEG C and insulated for some time, and then are dropped into methylsilicone oil or liquid paraffin at the temperature ranging from 5 to10 DEG C; 4. The method is simple in production process and short in production cycle. The cost can be decreased; 5. As the medicine is left in stomach for a short time or maybe the first-pass effect of the stomach can be avoided, so the generation of drug resistance and other side effects decreases.

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): A61K31/357A61K9/20A61K47/34A61P33/06A61K31/137A61K47/10
CPCY02A50/30
Inventor 孔伶俐魏吉城
Owner TIANJIN DANXI TCM INST
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