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Application of artesunate for preparing medicine to treat fibrosis of liver

An anti-hepatic fibrosis and artesunate technology, applied in the digestive system, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as unsatisfactory and poor therapeutic effect of liver fibrosis drugs

Inactive Publication Date: 2007-01-31
方步武
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] The present invention aims to solve the problems of lack of drugs and unsatisfactory therapeutic effects in clinical treatment of liver fibrosis, and provides an application of artesunate for preventing or reversing liver fibrosis in the preparation of anti-hepatic fibrosis preparations

Method used

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  • Application of artesunate for preparing medicine to treat fibrosis of liver
  • Application of artesunate for preparing medicine to treat fibrosis of liver
  • Application of artesunate for preparing medicine to treat fibrosis of liver

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] According to the methods known to those skilled in the art, the medicine of the present invention is prepared into tablets, which can inhibit HSC proliferation in a dose-dependent and time-dependent manner, and have no cytotoxicity to HSC. Although the positive control drug colchicine can inhibit the proliferation of HSC However, it has obvious cytotoxicity to HSC; at the same time, artesunate can significantly reduce the content of hydroxyproline in the HSC culture supernatant; artesunate can prevent HSC from G 0 / G 1 Phase enters S phase, while for G 2 / M phase has no effect; artesunate can induce the apoptosis of activated hepatic stellate cells.

[0090] Artesunate tablets: Each tablet contains 50.00mg of artesunate, 92.75mg of microcrystalline cellulose, 13.25mg of starch, 105.69mg of anhydrous lactose, 2.65mg of magnesium stearate, and 0.66mg of silicon dioxide.

[0091] Tablets are prepared by direct compression. Usage: 1 tablet each time, 2-3 times a day. 5-...

Embodiment 2

[0093] Prepare the drug of the present invention into artesunate injection according to methods known to those skilled in the art: under sterile conditions, dihydroartemisinin and succinic anhydride are used as raw materials, in chloroform solvent, in weakly alkaline medium triethyl ether In the presence of amine or sodium bicarbonate, through esterification reaction, artesunate is produced, recrystallized with ethanol, crushed to obtain sterile powder, and packed in a sterile room according to the aseptic method, each 60mg. When used, it is dissolved in 0.6ml of 5% sodium bicarbonate, then diluted with 5.4ml of normal saline, and injected slowly intravenously or intramuscularly. Pregnant women are prohibited. Regularly check reticulocytes during medication.

Embodiment 3

[0095] Medicine of the present invention is prepared into artesunate suppository by methods known to those skilled in the art:

[0096] Artesunate 5g, 5% NaHCO3 50ml (artesunate dissolved), glycerin 35g, Pluronic (F68) 10g, stearic acid amount, can be made into 50 capsules.

[0097] Usage: 1 capsule each time, 1-2 times a day, stuffed into the anus. 5-6 days of medication per week, every 3-4 weeks as a course of treatment. Pregnant women are prohibited. Regularly check reticulocytes during medication.

[0098] The suppository is safe and convenient to use, and reduces or avoids enterohepatic circulation.

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Abstract

An application of artesunate in preparing the medicines for preventing and treating the hepatic fibrosis and preventing heptocirrhosis and liver cancer is disclosed.

Description

technical field [0001] The invention relates to the use of a pharmaceutical preparation whose organic active ingredients are lactones, in particular to the use of artesunate in the preparation of anti-hepatic fibrosis preparations. Background technique [0002] Liver fibrosis exists in the pathogenesis of all chronic liver diseases and is a characteristic change of chronic liver diseases. Its outcome is liver cirrhosis and liver cancer, which seriously affects public health. According to statistics, 1 / 3 of patients with chronic hepatitis B and C virus can be transformed into liver cirrhosis, and 1 / 3 of the latter can be transformed into liver cancer; alcoholic liver disease, schistosomiasis and other chronic liver diseases can cause liver fibrosis increased incidence. It is generally believed that liver fibrosis can be reversed, while cirrhosis is not. Thus blocking the pathogenesis of liver fibrosis to liver cirrhosis and liver cancer, but so far no anti-hepatic fibrosis ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P1/16
Inventor 方步武
Owner 方步武
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