Entecavir medicinal composition and uses thereof

A technology of eltecavir and composition, which is applied in the field of eltecavir pharmaceutical composition, can solve the problems of viral rebound, the emergence of patients, and the comparison of short-term effects of eltecavir, etc., and achieves far-reaching social benefits and broad application. Foreground effect

Inactive Publication Date: 2008-01-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for some patients who failed lamivudine treatment, the dose of etecavir should be increased. After two years of treatment trials, it was found that 10% of patients developed drug resistance
Therefore, the toxicity of nucleoside drugs after long-term use, the drug resistance and the relatively high rebound of the virus after drug withdrawal are an unresolved problem
However, so far, the short-term effect of inhibiting the virus of a single traditional Chinese medicine is still not comparable to that of etecavir

Method used

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  • Entecavir medicinal composition and uses thereof
  • Entecavir medicinal composition and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The composition of embodiment 1 etecavir silymarin and its derivatives

[0024] Etecavir is mixed with silymarin and its derivatives (extracted from Compositae Silybum marianum L. Gaertn) in a certain ratio to prepare a composition.

[0025] The duck hepatitis B model test was carried out, and the results showed that it had an obvious effect of inhibiting DHBV, and the DHBV DNA was inhibited by 80% on the 10th day of administration, and the edema of the liver pathology section was significantly reduced;

[0026] The results of various animal experimental liver injury tests show that the above pharmaceutical composition has a protective effect on experimental liver injury, can resist necrosis of liver cells, reduce fatty degeneration, and restore the damage of mitochondria and endoplasmic reticulum in liver cells.

Embodiment 2

[0027] Embodiment 2, the composition of etecavir glycyrrhizic acid and its derivatives

[0028] Etecavir and glycyrrhizic acid are extracted from the dry rhizome of leguminous plant Glycyrrhiza uralensis Fisch or Glycyrr-hiza Glabra) in a certain ratio to obtain the composition, and the duck hepatitis B model test is carried out. The results show that animal experiments show that its anti- Hepatitis B virus is strong. The composition has a protective effect on the rat liver injury model of experimental animals, can reduce ALT, alleviate histological lesions, and can obviously improve the deep jaundice of experimental animals.

Embodiment 3

[0029] Embodiment 3, etecavir matrine and etecavir oxymatrine composition

[0030] Etecavir is mixed with matrine and oxymatrine (extracted from Sophorae flavescentis Ait, Sophora alopecuroids L and Sophorae tonkinensis Gapnep) in a certain ratio to prepare a composition. According to the in vitro HepG2 2.215 cell test, it can inhibit HBsAg by 80.5% and HBeAg by 68.0% after 10 days of administration; the duck hepatitis B model test shows that it has obvious inhibitory effect on DHBV-DNA, and the DHBV DNA is inhibited by more than 70% on the 10th day of administration After liver cell injury and liver fibrosis caused by carbon tetrachloride, galactosamine, ethanol, etc. in rats, 90% of serum bilirubin returned to normal, and 80% of ALT decreased, especially for jaundice.

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Abstract

The present invention pertains to the pharmaceutical field and relates to an antiviral compound drug, in particular to an entecavir drug composition and the anti-HBV usage. The present invention is composed of entecavir, (1s-(1 Alpha, 3 Alpha, 4 Beta))-2-amino-1, 9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purine-6-ketone, monocase compound which is extracted from one or more traditional Chinese medicines and the pharmaceutical excipients. The results of the in vitro and the duck hepatitis B animal model tests show that the present invention has obvious anti-HBV efficacy; at the same time, the present invention also has good hepatoprotective effect. The entecavir drug composition becomes the more safe and effective drug for treating hepatitis B and thus having very broad application prospect and far-reaching social benefits.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to an antiviral compound drug, in particular to an etecavir pharmaceutical composition and its anti-hepatitis B virus application. Background technique [0002] Hepatitis B is an infectious disease that seriously endangers people's lives and health. It has a wide range of prevalence and a high incidence rate, which is unmatched by other infectious diseases. According to relevant reports, as many as 15% of the populations in Asia, Africa and southern Europe are carriers of hepatitis B virus. According to statistics, there are 1 million newly increased hepatitis B patients every year in Europe alone, and China is a high-incidence area for hepatitis B virus. Relevant studies have confirmed that hepatitis B is closely related to liver cirrhosis and primary liver cancer. Around the world, about 1-2 million people die from liver cancer caused by HBV every year. Viral hepatitis B has long been an i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/899A61K31/522A61K47/40A61K9/20A61K9/08A61K9/48A61K9/16A61P31/14A61P1/16
Inventor 周珮林国强冯美卿孙智华李继扬史训龙黄海戴培兴
Owner FUDAN UNIV
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