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Nanometer antifungal econazole nitrate emulsion medicine and its prepn process

A technology of econazole nitrate nano- and antifungal drugs, which is applied in the field of medicine, can solve the problems of poor blood-brain barrier penetration, increased drug toxicity, and poor oral absorption, so as to avoid the first-pass effect of the liver, reduce adverse reactions, and surface low tension effect

Inactive Publication Date: 2009-01-07
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Econazole nitrate has remarkable curative effect, but also has many deficiencies: oral absorption is poor, and the peak plasma concentration after oral administration of 1g is only 1mg / L; T1 / 2β) is about 2.1 hours, the terminal half-life (T1 / 2) is 20 to 24 hours, and the serum protein binding rate is 90%. Poor permeability; mainly inactivated by liver metabolism into inactive metabolites, 14% to 22% of the oral dose is excreted from the urine, mainly inactive metabolites, of which less than 1% is the original substance, and 50% of the oral dose excreted in feces
Interaction with multiple drugs can increase drug toxicity

Method used

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  • Nanometer antifungal econazole nitrate emulsion medicine and its prepn process

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Accurately weigh castor oil polyoxyethylene ether 4.5g, dimethyl sulfoxide 0.5g (dissolving econazole nitrate 0.02g in it), isooctyl palmitate 0.5g, under 20 ℃ of conditions, stir and mix, then to Slowly add distilled water and stir while adding. At the beginning, the viscosity of the system is small. As the amount of water increases, the system becomes viscous. Continue to add distilled water and stir continuously. When the system suddenly becomes thinner, what is produced at this time is O / W type colorless transparent econazole nitrate nanoemulsion, claiming its weight is 10.0g.

Embodiment 2

[0058] Accurately weigh 4.0 g of castor oil polyoxyethylene ether, 0.5 g of dimethyl sulfoxide (dissolving econazole nitrate 0.07 g in it), 1.0 g of almond oil, stir and mix well at 20 ° C, and then slowly add Add distilled water while stirring. At the beginning, the viscosity of the system is small. As the amount of water increases, the system becomes viscous. Continue to add distilled water and stir continuously. When the system suddenly becomes thinner, the O / W type no Color transparent econazole nitrate nanoemulsion, claims its weight as 10.0g.

Embodiment 3

[0060] Accurately weigh 2.5g of castor oil polyoxyethylene ether, 0.75g of dimethyl sulfoxide (dissolving 0.12g of econazole nitrate in it), 0.5g of snake oil, stir and mix well at 20°C, and then slowly add Add distilled water while stirring. At the beginning, the viscosity of the system is small. As the amount of water increases, the system becomes viscous. Continue to add distilled water and stir continuously. When the system suddenly becomes thinner, the O / W type no Color transparent econazole nitrate nanoemulsion, claims its weight as 10.0g.

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Abstract

The nanometer antifungal econazole nitrate emulsion medicine consists of econazole nitrate, surfactant, oil and distilled water. Its preparation process includes the following steps: weighing the materials; mixing the surfactant and oil and dissolving econazole nitrate in dimethyl sulphoxide; mixing the solution of econazole nitrate with the surfactant and oil; and final adding distilled water slowly while stirring to form stable homogeneous transparent nanometer antifungal econazole nitrate emulsion medicine. The medicine is used in treating candidal tinea corporis, tinea cruris and tinea pedis, aural mycosis, seborrheic dermatitis, etc. The medicine is absorbed through skin to enter into blood circulation, and this avoids the first pass effect of liver, prolongs the medicine release and prevents stimulation to gastrointestinal tract. The preparation process is simple and low in power consumption.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of an antifungal drug econazole nitrate, in particular to a nanoemulsion antifungal drug of econazole nitrate and a preparation method thereof. Background technique [0002] Econazole nitrate is a broad-spectrum antifungal drug for external use of imidazoles, which has antibacterial activity against deep and superficial fungi, and its chemical name is 1-[2,4-dichloro-β(4-chlorobenzyloxy)phenethyl] Imidazole nitrate, white or yellowish crystal or crystalline powder, odorless, very slightly soluble in water. Econazole nitrate is metabolized in the liver and is mainly excreted by bile. It is effective against dermatophytes, yeasts and molds, and has antibacterial effects on some Gram-positive bacteria; it is suitable for tinea corporis, jock itch, tinea pedis, and ear Treatment of fungus, seborrheic dermatitis, etc. Econazole nitrate inhibits the biosynthesis of ergosterol,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4164A61K9/107A61K47/44A61P31/10
Inventor 欧阳五庆杨宝平吴旭锦
Owner NORTHWEST A & F UNIV
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