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Application of Chukrasone A for preparing antifungal drugs for human body

A technology against human fungi and drugs, applied in the directions of antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of digestive tract irritation, strong accumulation of toxicity, etc. active effect

Inactive Publication Date: 2013-11-20
JIANGSU KEHUA MEDICAL INSTR TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The spread of pathogenic bacteria and the enhancement of drug resistance seriously threaten human health and life. Antibacterial drugs have been widely used as routine drugs in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) Treatment, although antibacterial agents currently used clinically (such as ketoconazole, amikacin, gentamicin, vigorconazole, itraconazole, terbinafine, amphotericin, fluconazole, etc.) The curative effect on skin and superficial infection is good, but these antibacterial drugs have strong cumulative toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc. one of the hotspots

Method used

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  • Application of Chukrasone A for preparing antifungal drugs for human body
  • Application of Chukrasone A for preparing antifungal drugs for human body
  • Application of Chukrasone A for preparing antifungal drugs for human body

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of the compound ChukrasoneA tablet involved in the present invention:

[0014] Take 20 grams of compound Chukrasone A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press machine.

Embodiment 2

[0015] Embodiment 2: the preparation of the compound ChukrasoneA capsule involved in the present invention:

[0016] Get 20 grams of compound Chukrasone A, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

[0017] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example

[0018] Experimental example: ChukrasoneA anti-human fungal activity

[0019] Anti-human fungus activity experiment is the method of concentration dilution, each determination is repeated three times, the test pathogens are Trichophyton rubrum, Microsporum lanoides and Trichophyton aureus, and the concentration of bacteria solution is 10 5 individual / mL. The initial concentration of ChukrasoneA is 50.0μg / mL (5% dimethyl sulfoxide DMSO), serially diluted to 0.098μg / mL, the equal volume of bacteria liquid and test samples are mixed and cultured in a 96-well plate, and the culture temperature of human fungi is respectively 28°C, observe after 24 hours of incubation time, if no colonies are found, it is the lowest anti-human fungal concentration of the sample, that is, the MIC value. The positive control of this experiment is ketoconazole, and the results of Chukrasone A against human fungi are shown in Table 1.

[0020] Table 1 ChukrasoneA anti-human fungal MIC value (μg / mL)

...

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PUM

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Abstract

The invention relates to an application of Chukrasone A for preparing antifungal drugs for a human body. Chukrasone A has strong inhibition effect on trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, so the Chukrasone A can be used as an anti human body fungal compound, and can be applied for preparing relative medicament. The application of Chukrasone A for preparing antifungal drugs for human body is firstly disclosed. Because a matrix type belongs to a new matrix type, and Chukrasone A has unexpectedly strong inhibition activity on human body fungus without possibility of any enlightenment given by other compounds, Chukrasone A has significantly substantive characteristics, and simultaneously has substantial progress for preventing human body infection fungus.

Description

technical field [0001] The present invention relates to the use of Chukrasone A, in particular to the application of Chukrasone A in the preparation of anti-fungal drugs for human body. Background technique [0002] The spread of pathogenic bacteria and the enhancement of drug resistance seriously threaten human health and life. Antibacterial drugs have been widely used as routine drugs in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) Treatment, although antibacterial agents currently used clinically (such as ketoconazole, amikacin, gentamicin, vigorconazole, itraconazole, terbinafine, amphotericin, fluconazole, etc.) The curative effect on skin and superficial infection is good, but these antibacterial drugs have strong accumulation toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc. one of the hotspots. [0003] The compound ChukrasoneA involved in th...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P31/10
Inventor 丁圣雨
Owner JIANGSU KEHUA MEDICAL INSTR TECH CO LTD
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