Applications of pegylated artesunate in preparing medicines capable of resisting hepatic pathological changes

A technology of polyethylene glycol artesunate and artesunate, which is applied in the direction of antineoplastic drugs, drug combinations, and pharmaceutical formulations, and can solve the problem of anti-hepatic fibrosis of polyethylene glycol artesunate that has not yet been seen

Active Publication Date: 2017-04-26
KPC PHARM INC
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Evidence has shown that liver fibrosis and early liver cirrhosis are reversible. Blocking or reversing liver fibrosis is an important goal in the treatment of chronic liver diseases, but t

Method used

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  • Applications of pegylated artesunate in preparing medicines capable of resisting hepatic pathological changes
  • Applications of pegylated artesunate in preparing medicines capable of resisting hepatic pathological changes
  • Applications of pegylated artesunate in preparing medicines capable of resisting hepatic pathological changes

Examples

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Effect test

Embodiment 1

[0027] Example 1 Study on the Effect of Polyethylene Glycol Artesunate on Rat Hepatic Fibrosis

[0028] 1. Test material

[0029] Polyethylene glycol artesunate, made by Kunming Pharmaceutical Research Institute according to the method disclosed in Example 1 of Chinese patent CN103450468B, has a structure of formula 1; artesunate, Chongqing Huafang Wulingshan Pharmaceutical Co., Ltd.; colchicine tablets , Kunming Pharmaceutical Group Co., Ltd.; hyaluronidase (HA), laminin (LN), type III procollagen (PC-III) kits, Zhongsheng Beikong Biotechnology Co., Ltd.; serum alanine transamination Enzyme (ALT), aspartate aminotransferase (AST), serum albumin (ALB), malondialdehyde (MDA), superoxide dismutase (SOD), hydroxyproline (HyP) kit, HE Dye solution, Nanjing Jiancheng Biological Engineering Co., Ltd.; carbon tetrachloride (AR), Chongqing Chuanjiang Chemical Reagent Factory; precision electronic balance, Beijing Sartorius Balance Co., Ltd.; TDL-5 centrifuge, Shanghai Anting Scientif...

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Abstract

The invention provides applications of pegylated artesunate shown as the formula (I) in preparing medicines capable of resisting hepatic pathological changes. According to the applications, pegylated artesunate can obviously reduce the hepatic fibrosis condition and abnormal liver function of hepatic fibrosis rats caused by carbon tetrachloride, reduce the amount of the serum fibrosis markers such as hyaluronidase (HA), laminin (LN) and procollagen III (PC-III), reduce the amount of alamine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum, reduce the contents of malondialdehyde (MDA) and hydroxyproline (Hyp) of the liver tissue, and effectively prevent the development of liver fibrosis and promote the reversion of liver fibrosis, and has the significant differences compared with artesunate under the same dosage. In addition, the pegylated artesunate is good in water solubility, high in bioavailability, and long in half-life period, and the administration times can be reduced. The formula (I) is shown as follows.

Description

technical field [0001] The invention relates to the technical field of artesunate derivatives, in particular to the application of polyethylene glycol artesunate in the preparation of anti-hepatic lesions drugs. Background technique [0002] Hepatic fibrosis is the pathological basis of liver cirrhosis. Various etiologies (such as viral hepatitis, alcoholic liver disease, non-alcoholic liver disease, drug and chemical factors, etc.) cause liver damage and inflammation, leading to liver fibrosis , and eventually develop into liver cirrhosis. Liver fibrosis is the result of excessive deposition of extracellular matrix, and it is also the main intermediate link in the further development of liver cirrhosis and liver cancer. [0003] Liver cirrhosis has a high morbidity and mortality rate. According to statistics, domestic patients hospitalized due to liver cirrhosis accounted for 0.36% to 0.64% of the hospitalizations in the same period. Chronic liver diseases such as parasit...

Claims

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Application Information

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IPC IPC(8): A61K31/785A61P1/16A61P35/00
Inventor 黄照昌宋立明刘国光朱泽曾涛李鹏辉
Owner KPC PHARM INC
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