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Anti-drug-resistant fungus pharmaceutical composition and preparation thereof

A technology of antifungal drugs and compositions, applied in the field of medicine, can solve the problems of aggravating the drug resistance of Candida albicans to fluconazole, and achieve the effect of anti-drug-resistant fungi

Active Publication Date: 2020-08-07
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

During long-term treatment, repeated administration aggravates the occurrence of fluconazole resistance in Candida albicans, and most fungi that are resistant to fluconazole also have cross-resistance to other antifungal drugs. A large number of drug-resistant strains have emerged, and the current antifungal drugs have fallen into a bottleneck in the treatment of fungal infectious diseases

Method used

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  • Anti-drug-resistant fungus pharmaceutical composition and preparation thereof
  • Anti-drug-resistant fungus pharmaceutical composition and preparation thereof
  • Anti-drug-resistant fungus pharmaceutical composition and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Wash the screen side notoginseng, dry it, and beat it into a coarse powder. Take 1100g coarse powder, add 95% ethanol to reflux twice, the first time is 2h, the second time is 1.5h, and the amount of 95% ethanol is 22L each time. After reflux, filter, combine the filtrates, and obtain 342.8g extract after vacuum distillation. Dissolve the extract in 1L of water, extract 4 times with petroleum ether and n-butanol respectively, and use 0.3L of solvent each time; combine the n-butanol extracts and distill under reduced pressure to obtain n-butanol part extract: 151.90g, That is Pingbian Panax notoginseng n-butanol extract.

Embodiment 2

[0059] (1) Wash the panax notoginseng, dry it, and grind it into coarse powder.

[0060] (2) Add ethanol to the coarse powder and reflux twice, each time the amount is 5-15 times the mass volume (kg / L) of Pingbian Sanqi coarse powder, 1-3 hours each time, filter after reflux, combine the filtrates, and depressurize Concentrate the extract until there is no alcohol smell to obtain the Pingbian Sanqi ethanol extract;

[0061] (3) Suspend Pingbian Sanqi ethanol extract with water, extract with petroleum ether and n-butanol in sequence, and extract 3-6 times with each solvent; combine the n-butanol extract, concentrate the extract under reduced pressure until it has no alcohol smell Get Pingbian notoginseng n-butanol extract.

[0062] The mass concentration of ethanol described in step (2) is 80-90%; the amount of suspension water described in step (3) is 1-3 times that of Pingbian Panax notoginseng ethanol extract. , The amount of n-butanol is 1 / 6-1 / 2 of the water phase volume ...

Embodiment 3

[0073] Anti-drug-resistant Candida albicans effect detection in vitro

[0074] 1-fold ratio microdilution method

[0075] Dissolve 0.1g of Panax notoginseng n-butanol extract in 1mL dimethyl sulfoxide (DMSO) to make a storage solution with a concentration of 100mg / mL, and store it in a refrigerator at 4°C; take a fluconazole dispersible tablet and grind it into powder Add 1mL DMSO to make a stock solution with a concentration of 50mg / mL, and store it in a refrigerator at 4°C.

[0076] Dilute the prepared Pingbian notoginseng n-butanol extract storage solution (100mg / mL) and fluconazole storage solution (50mg / mL) to 1mg / mL and 0.5mg / mL respectively, as the initial concentration, use 5-fold dilution by the micro-doubling dilution method, and 6 concentration gradients are set for each experiment [19] , set Pingbian notoginseng n-butanol extract single use group, fluconazole single use group and Pingbian notoginseng n-butanol extract combined with fluconazole group, respectively...

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Abstract

The invention belongs to the technical field of biological medicines, and discloses a pharmaceutical composition with drug-resistant fungi resistance, which is composed of panax stipuleanatus n-butylalcohol extract and antifungal drugs. The panax stipuleanatus n-butyl alcohol extract is obtained by cleaning panax stipuleanatus, drying the panax stipuleanatus in the sun, crushing the panax stipuleanatus, extracting the panax stipuleanatus with n-butyl alcohol and distilling under reduced pressure. The panax stipuleanatus n-butyl alcohol extract can obviously reduce the efflux function of a fungal cell efflux pump, so that the expression level of drug resistance related genes is obviously reduced, and the mitochondrial membrane potential level in fungal cells is reduced; the pharmaceuticalcomposition composed of the panax stipuleanatus n-butyl alcohol extract and the antifungal drug has a good inhibition effect on drug-resistant fungi.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an anti-drug-resistant fungal pharmaceutical composition and a preparation thereof, which are composed of Pingbian Panax notoginseng n-butanol extract and antifungal medicines. Background technique [0002] Candida albicans ( Candida albicans ) is an opportunistic fungus that exists in human skin, mucous membranes, etc., and generally does not cause disease in normal organisms. In recent years, due to the extensive application of radiotherapy and chemotherapy in cancer patients, the application of a large number of immunosuppressants in organ transplant patients, and the large-scale use of broad-spectrum antibiotics, the incidence of systemic Candida albicans infection has increased rapidly, and the infection rate is as high as 46.36%. [0003] At present, there are few drugs available for clinical anti-Candida albicans deep infection, mainly amphotericin B, miconaz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/258A61P31/10A61K125/00
CPCA61K36/258A61P31/10A61K2236/333A61K2236/39A61K2236/53A61K2236/51
Inventor 王睿睿苏刘艳倪广惠李莉张祎刘潇祎
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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