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Preparation for benflumetol dripping pill for treating malaria

A technology for the treatment of malaria and lumefantrine, applied in pill delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem that it is difficult to quickly reach the peak blood concentration and the long disintegration time limit , Inconvenient use, 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.
Oral preparations include capsules, the main disadvantage of which is the long disintegration time limit. Due to its non-water-soluble nature, it is not easy to absorb, and the 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] The main drug benzefantrine 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 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, 2.0g at a time.

Embodiment 2

[0016] The main drug benzefantrine 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 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 - 0.6mm caliber drop pill machine drop into the liquid paraffin coolant at 5-10 ℃, filter off the liquid paraffin, shake it off, dry it in air, and get it. The weight of each pill is 5-15mg. Take 2.0g each time, once a day.

Embodiment 3

[0021] The main drug benzefantrine 100 parts

[0022] Poloxamer 250 parts

[0023] 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 2.0g each time, once a day.

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Abstract

The invention relates to the preparation of a chemical medicine agent, benflumelol used for curing the malaria. The present invention has advantages that: 1. Compared to the existing preparation capsule agent, the disintegration time limited is greatly shortened with rapid onset; 2. The auxiliary water soluble material sufficiently disperse the main non-water soluble ingredient, which is favorable for absorption of the main ingredient and the oral administration bioavailability can be improved; 3. The dropping pills of the present invention can be taken with water, or taken under tongue. The ingredient can be directly absorbed by the hypoglossis mucous membrane capillary vessel to avoid first pass effect of stomach and rapidly reach peak value of the blood concentration with rapid effect. The curative effect is improved; 4. As dropping pill of the present invention is rapid in absorption, short in detention time in stomach so that the generation of drug resistance and other side effects are decreased; 5. Simple production process and short production cycle can reduce the cost; 6. The invention overcomes not only inconvenience in applying the vein administration but also defects of low biological utilization ratio of other oral administrative regular preparation.

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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IPC IPC(8): A61K31/137A61K9/20A61K47/34A61P33/06A61K47/10
CPCY02A50/30
Inventor 孔伶俐魏吉城
Owner TIANJIN DANXI TCM INST
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