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Fukinanclide K-containing antifungal composition for external use

A technology of butterbur lactone and external composition, which is applied in the direction of medical preparations containing active ingredients, antifungal agents, and medical preparations without active ingredients, which can solve the problems of stimulating drug resistance of pathogenic bacteria and achieve Good antibacterial effect, improved therapeutic effect, high therapeutic effect

Inactive Publication Date: 2018-11-09
泮宝峰 +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bifonazole (CAS: 60628-96-8), as a broad-spectrum antifungal drug, is widely used in the treatment of fungal skin diseases, and with its widespread use, bifonazole, etc. The problem of drug resistance of existing topical antifungal drugs is becoming more and more prominent, and the simple method of increasing the dose is more likely to stimulate the drug resistance of pathogenic bacteria, forming a vicious circle

Method used

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  • Fukinanclide K-containing antifungal composition for external use
  • Fukinanclide K-containing antifungal composition for external use
  • Fukinanclide K-containing antifungal composition for external use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Pharmacological Example 1. Preparation of drug-resistant strains

[0015] Preparation

[0016] 1) Standard strain Trichophyton rubrum (No.: ATCC228188) was used as the standard strain, and the standard strain of Trichophyton rubrum was inoculated on potato dextrose agar (PDA) medium, and activated in an incubator at 28°C for 7 to 14 days , select the colonies with good growth status and no pollution as the test strains, select the colonies with good growth status and no pollution as the test strains, drop an appropriate amount of 0.85% sterile saline on the colonies, and gently repeat with a sterile cotton swab Scrape the surface of the colony to mix the spores well with the normal saline. Filter the bacterial suspension with two layers of gauze into a centrifuge tube, and then place it in a vortex shaker for about 15s. Count with a hemocytometer, and adjust the bacterial concentration to 2-6×10 with sterile saline. 5 cfu / mL, and finally diluted 10 times with PRMI-16...

Embodiment 2

[0019] Pharmacological Example 2. In vitro antibacterial effect test

[0020] 1. Preparation of culture medium

[0021] Potato dextrose agar medium (PDA), the mass fraction is 20% potato, 2% glucose, and 1.8% agar. Add 5ml of medium to each test tube to prepare a slant medium; add 20ml of medium to a plate with a diameter of 90mm to prepare a plate medium

[0022] 2. Experimental method

[0023] 2.1 Treatment of strains

[0024] 1. The artificially induced drug-resistant Trichophyton rubrum strain and standard strain prepared in Pharmacological Example 1 were transferred to the PDA medium activation strain on a plate using a sterilization inoculation loop respectively, placed in a 28°C constant temperature incubator, and cultivated for 7 days.

[0025] 2.2 Making bacterial suspension

[0026] Pick an appropriate colony mass and dissolve it in 1 mL of 0.9% sterile saline with Tween 80 added. Shake with a micro-shaker for 2 minutes, fully shake to wash out the spores, and u...

Embodiment 3

[0050] Butterolide K 8.4g, bifonazole 7g

[0051] Sodium carboxymethyl cellulose 60g, glycerol 150g

[0052] Add 2g of ethyl paraben to distilled water to 1000g

[0053] Mix CMC-Na and glycerol to obtain CMC-Na slurry, dissolve ethyl paraben in hot water, then add CMC-Na slurry, stir to form gel, and then add bifonazole and bee bucket. The vegetable lactone K is dissolved in an appropriate amount of ethanol, gradually added and stirred, and the remaining amount of water is added and stirred to obtain a transparent gel.

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Abstract

Fukinanclide K-containing antifungal composition for external use is prepared from bifonazole and fukinanclide K as active ingredients, and at least one accessory suitable for external application toskin; the mass ratio of the fukinanclide K to the bifonazole in the composition for external use is (0.8-1.2):1, and the mass percentage of bifonazole is 0.7%-0.9%. The composition is formed into a gel, and the accessory of the gel is selected from one or more of a cellulose derivative, a humectant, a solvent, a surfactant, a pH adjuster, and excess water. The cellulose derivative is selected fromone or more of sodium carboxymethylcellulose (CMC-Na), methylcellulose (MC), and hydroxypropyl methyl cellulose (HPMC); the solvent is selected from one or more of ethanol, propylene glycol, dimethylsulfoxide, and N, N-dimethylformamide; the humectant is glycerol, and the amount is 10% to 15%.

Description

Technical field: [0001] The present invention provides an antifungal composition for external use. Background technique: [0002] Butterolide K is a sesquiterpene lactone extracted from Asteraceae Butterfly, and its structure is as follows [0003] [0004] According to reports, butterburide derivatives such as butterburide K have anticoagulant effects and certain anticancer activities, but no antifungal effects are mentioned. Fungal skin disease refers to a large class of infectious diseases of human skin and skin appendages such as mucous membranes, hair and nails caused by pathogenic fungi. . Bifonazole (CAS: 60628-96-8), as a broad-spectrum antifungal drug, is widely used in the treatment of fungal skin diseases. The problem of drug resistance of existing topical antifungal drugs is becoming more and more prominent, and simply by increasing the dose, it is easier to stimulate the drug resistance of pathogenic bacteria, forming a vicious circle. In our study, we fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4174A61K31/365A61K9/00A61P31/10A61P17/00
CPCA61K9/0014A61K31/365A61K31/4174A61K47/38A61P17/00A61P31/10A61K2300/00
Inventor 赵振燕董芳梅童小丽王文坤
Owner 泮宝峰
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