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Pharmaceutical composition of clofazimine and medical application of composition

A technology of clofazimine and its composition, which is applied in the field of biomedicine, can solve the problems that have not yet been reported about clofazimine and its pharmaceutical composition, and achieve the effect of protecting the liver and improving the protective effect

Inactive Publication Date: 2016-06-22
贺玉皓
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, there has been no report on the correlation between clofazimine and its pharmaceutical composition and liver protection

Method used

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  • Pharmaceutical composition of clofazimine and medical application of composition
  • Pharmaceutical composition of clofazimine and medical application of composition
  • Pharmaceutical composition of clofazimine and medical application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0021] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0022] Separation method: (a) Grind hemp seed (2kg), extract with 85% ethanol under heat reflux (15L×3 times), combine the extracts, concentrate until no alcohol smell (3L), and successively use petroleum ether (3L×3 times), ethyl acetate (3L × 3 times) and water-saturated n-butanol (3L × 3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract and n-butanol extract respectively; (b) step ( a) Use D101 type macroporous resin to remove impurities from the ethyl acetate extract in the medium, first elute with 30% ethanol for 6 column volumes, then use 85% ethanol for 12 column volumes, collect 85%...

Embodiment 2

[0025] Embodiment 2: pharmacological action

[0026] 1. Materials and methods

[0027] 1.1 Materials and Instruments

[0028] Clofazimine was purchased from China National Institute for the Control of Pharmaceutical and Biological Products. Compound (I) is self-made, and the preparation method is shown in Example 1. ICR female mice weighing (25 ± 5) g, Shanghai Slack Laboratory Animal Co., Ltd.; Coomassie brilliant blue G-250, triglyceride kit, malondialdehyde test kit, glutathione peroxide kit, Alcohol dehydrogenase assay kit Nanjing Jiancheng Bioengineering Research Institute; Neptune Jinzun, Shenzhen Neptune Pharmaceutical Co., Ltd.; 56° Red Star Erguotou Liquor, Beijing Red Star Brewery. Alpha-D2 lyophilizer, Christ Company, Germany; electronic balance, Shanghai Tianping Instrument Factory; UV752N ultraviolet-visible spectrophotometer, Shanghai Yidian Analytical Instrument Co., Ltd.

[0029] 1.2 Animal grouping

[0030] 72 ICR mice were adaptively fed for one week und...

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Abstract

The invention discloses a pharmaceutical composition of clofazimine and its medical application. The pharmaceutical composition of clofazimine provided by the invention contains clofazimine and a natural product compound (I) with a novel structure, chlorine When fazimine and compound (I) act alone, they can increase the content of GSH in mouse liver tissue, reduce the content of MDA, inhibit the accumulation of TG, and have a certain hepatoprotective effect; when clofazimine and compound (I) act in combination, The hepatoprotective effect is better, and it can be developed into a liver-protective drug. Compared with the prior art, it has outstanding substantive features and significant progress.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of clofazimine, in particular to a pharmaceutical composition of clofazimine and its application in protecting the liver. Background technique [0002] Many metabolites, such as acetaldehyde and free radical ions, are produced during alcohol metabolism. The damage of these metabolites to the body is greater than that of alcohol itself, which can cause inflammation, cause liver cell damage, reduce immune function, and lead to death. After the body ingests a large amount of ethanol, it is mainly oxidized to acetaldehyde under the catalysis of alcohol dehydrogenase (ADH), and then oxidized to acetate substances by acetaldehyde dehydrogenase. Therefore, it is considered that ADH is an important enzyme in the process of ethanol metabolism, and maintaining its activity can accelerate the catabolism of ethanol in the body and reduce the accumulation of ethanol in the body. A ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/93A61K31/365A61K31/498A61P1/16
CPCC07D307/93A61K31/365A61K31/498
Inventor 贺玉皓
Owner 贺玉皓
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