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Antifungal medicine composition

A technology of antifungal drugs and compositions, applied in the direction of antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as liver toxicity, anemia, paresthesia, etc., to reduce toxic reactions and reduce development , the effect of reducing the dose of the drug

Active Publication Date: 2014-01-29
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of ketoconazole can cause a series of adverse reactions such as liver toxicity, gastrointestinal reactions such as nausea and vomiting, drug eruption, itching, dizziness, headache, abdominal pain, lethargy, photophobia, paresthesia, white blood cells and Thrombocytopenia, anemia, hair loss, allergies, etc.

Method used

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  • Antifungal medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1, the interactive antifungal activity test of spinosad and ketoconazole

[0030] The interactive antifungal (Candida albicans, Candida albicans SC5314) activity of spinosad and ketoconazole was tested by the checkerboard method.

[0031] 1. Put Candida albicans SC5314 in RPMI1640 medium, 35°C, humidity 80%, 5% CO 2 Incubate under conditions.

[0032] 2. Dissolve spinosad and ketoconazole in DMSO respectively to a concentration of 1 mg / mL, and store in the refrigerator for use.

[0033] 3. Determination of minimum inhibitory concentration (MIC)

[0034] (1) Refer to the M-27A protocol of the National Committee for Clinical Laboratory Standards (NCCLS), that is, the "Yeast Liquid Medium Dilution Method for Antifungal Drug Susceptibility Test Protocol". Prepare the stored 1 mg / mL spinosyn and ketoconazole solution with liquid medium (RPMI1640 medium) to make a series of diluted spinosad and ketoconazole solutions.

[0035] (2) Inoculate Candida albicans cel...

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PUM

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Abstract

The invention discloses an antifungal medicine composition composed of A and B. The A is any one of the substances of: macrolide antibiotic, analogue thereof, derivative thereof, prodrug thereof, metabolite thereof, and pharmaceutically active salt thereof. B is any one of the substances of: triazole compound, analogue thereof, derivative thereof, prodrug thereof, metabolite thereof, and pharmaceutically active salt thereof. As a result of in-vitro antifungal experiments, when ketoconazole and spinosad are applied in combination, high synergetic activity can be developed. The composition disclosed by the invention is effective against intractable invasive fungal infections. With the composition, ketoconazole dose can be reduced, such that patient economic burden can be reduced, ketoconazole toxic reaction can be reduced, and fungal drug resistance development can be effectively reduced.

Description

technical field [0001] The invention relates to an antifungal pharmaceutical composition. Background technique [0002] The increasing incidence of fungal infections, especially opportunistic fungal infections in immunocompromised patients, poses a serious challenge to the treatment of fungal infections. Although some fungal drugs have come out one after another, which has brought new opportunities for the treatment of fungal infections, but at the same time, reports of drug resistance to drug treatment have gradually increased. Therefore, there is a need to develop new antifungal treatments. [0003] Ketoconazole can be used to treat superficial and deep mycoses, such as skin and nail ringworm, vaginal candidiasis, gastrointestinal fungal infections, etc. Infect. However, the use of ketoconazole can cause a series of adverse reactions such as liver toxicity, gastrointestinal reactions such as nausea and vomiting, drug eruption, itching, dizziness, headache, abdominal pai...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P31/10A61K31/496
Inventor 张立新白超弦任彪刘梅
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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