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Nanometer clotrimazole emulsion medicine and its prepn process

A nano-emulsion, clotrimazole technology, applied in the direction of emulsion delivery, oil/fat/wax inactive ingredients, antifungal agents, etc. High thermodynamic stability, good solubilization, and improved corrosion resistance

Inactive Publication Date: 2007-03-21
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since clotrimazole is insoluble in the aqueous phase, it affects its bioavailability
At present, there are many medicines for treating skin diseases on the market, but most of them are water preparations or ointments, which are easy to contaminate the clothes when rubbed on the affected area, and the action time is short

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Accurately weigh 4.5g of hydrogenated castor oil polyoxyethylene ether, 1.0g of ethanol (clotrimazole 0.2g is dissolved in it), and 0.5g of olive oil. Add distilled water and stir manually while adding water. At the beginning, the viscosity of the system is small. As the amount of water increases, the system will become viscous. At this time, the system may appear in a liquid crystal state or a water-in-oil nanoemulsion. Continue to add drops and keep stirring. When the system suddenly became thinner, what produced at this moment was the O / W type colorless and transparent clotrimazole nanoemulsion medicine, claiming its weight as 10.0g.

Embodiment 2

[0052] Accurately weigh 4.5 g of castor oil polyoxyethylene ether, 0.5 g of ethanol (clotrimazole 0.1 g is dissolved therein), and 0.5 g of isooctyl palmitate, and at room temperature of 22 ℃, manually stir it to fully mix it, and then Slowly add distilled water, and stir manually while adding water. At the beginning, the viscosity of the system is small. As the amount of water increases, the system will become viscous. At this time, the system may appear liquid crystal or water-in-oil nanoemulsion. Stir, when the system suddenly becomes thinner, what produces this moment is O / W type light yellow transparent clotrimazole nanoemulsion medicine, claims its weight as 10.00g.

Embodiment 3

[0054] Accurately weigh 3.0 g of castor oil polyoxyethylene ether, 1.0 g of 1,3-butanediol (clotrimazole 0.05 g is dissolved therein), 0.44 g of isopropyl myristate, and stir it by hand at room temperature of 23°C Mix well, then add distilled water slowly, and stir manually while adding water. At the beginning, the viscosity of the system is small. As the amount of water increases, the system will become viscous. At this time, the system may appear liquid crystal or water-in-oil nanoemulsion , continue to add dropwise and constantly stir, when the system becomes thinner suddenly, what produces at this moment is the O / W type light yellow transparent clotrimazole nanoemulsion medicine, claims its weight as 10.0g.

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Abstract

The nanometer clotrimazole emulsion medicine consists of surfactant, oil, clotrimazole and distilled water. Its preparation process includes the following steps: weighing surfactant with or without co-surfactant; calculating HLB value and selecting oil for reaching emulsifying HLB value near that of the surfactant phase; dissolving clotrimazole into surfactant; changing the ratio between the surfactant phase and the oil phase regularly; adding distilled water slowly at 20-25 deg.c to form clear and flowing O / W type stable nanometer emulsion liquid. The nanometer clotrimazole emulsion has high skin permeability, no contamination to clothing, high dissolubility of clotrimazole, raised bioavailability of clotrimazole, delayed metabolism time and wide medicine market foreground.

Description

technical field [0001] The invention belongs to the field of drugs, and relates to a new dosage form of clotrimazole, a broad-spectrum antifungal drug for external use, in particular to a clotrimazole nanoemulsion drug and a preparation method thereof. Background technique [0002] Clotrimazole is a broad-spectrum antifungal drug, which is effective against superficial skin fungi such as various ringworms, cryptococcal fungal infections and deep fungi such as Candida neophytes, coccidioides, spores, and British membrane tissue Cytoplasma infection has a strong inhibitory effect. Therefore, it is often used clinically for skin, nail, toenail infection, angular cheilitis, otitis externa and vaginal infection caused by skin fungus. Since clotrimazole is insoluble in the aqueous phase, its bioavailability is affected. There are many medicines for treating skin diseases in the market, but most of them are water preparations and or ointments, which are easy to contaminate clothe...

Claims

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Application Information

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IPC IPC(8): A61K31/4164A61K9/107A61K47/44A61P31/10
Inventor 欧阳五庆吴旭锦杨宝平
Owner NORTHWEST A & F UNIV
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