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Terbinafine nano milk-like liquid antifungal medicine and its preparation

The technology of an antifungal drug, terbinafine, is applied in the field of medicine, which can solve the problems of low concentration, high risk of taking, and poor water solubility, and achieve the effects of uniform distribution, simple preparation method, and low surface tension

Inactive Publication Date: 2009-10-14
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example: its water solubility is poor, and the drug concentration of the dosage form currently used in clinical practice is generally low; it is mainly metabolized in the liver, and the risk of taking it is relatively high for those with liver and kidney insufficiency; the common adverse reactions are mainly nausea, diarrhea, anorexia, mild Abdominal pain, loss of taste, and skin reactions (rash, hives, etc.)

Method used

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  • Terbinafine nano milk-like liquid antifungal medicine and its preparation
  • Terbinafine nano milk-like liquid antifungal medicine and its preparation
  • Terbinafine nano milk-like liquid antifungal medicine and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Accurately weigh 4.5g of polyoxyethylene ether (40) hydrogenated castor oil, 1.0g of ethanol (in which 0.02g of terbinafine is dissolved), 0.5g of olive 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 terbinafine nanoemulsion, claiming its weight is 10.0g.

Embodiment 2

[0065] Accurately weigh 4.5g of castor oil polyoxyethylene ether, 1.0g of ethanol (dissolving 0.06g of terbinafine in it), 0.5g of isooctyl ester, and stir and mix well at 22°C, then slowly add distilled water therein, while Stir while adding, the viscosity of the system is small at the beginning, 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 colorless and transparent characteristic is produced at this time. Binafine nanoemulsion claims its weight as 10.0g.

Embodiment 3

[0067] Accurately weigh 4.5g of polyoxyethylene ether (40) hydrogenated castor oil, 1.0g of ethanol (in which 0.10g of terbinafine is dissolved), 0.5g of castor oil, stir and mix well at 24°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 terbinafine nanoemulsion, claiming its weight is 10.0g.

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Abstract

The invention discloses a terbinafine nanometer antifungal which is prepared by terbinafine, oil, surfactant, water according to the following method: First, the said raw materials are unloaded and weighed and reserved, then surfactants and oil is blended and mixed; terbinafine is added into cosurfactant and completely dissolved; the solution with terbinafine dissolved in it is added to the homogeneous mixed surfactant and oil, stirring uniform, finally, distilled water is slowly added dropwise, dropwising and stirring until the stable, homogeneous, transparent terbinafine nanometer antifungal is obtained. The drug with small particles, small viscosity, good fluidity and good nature stability, can reach through the skin and get into the blood circulation, inhibit squalene cycloxygenase, so as to treat the dermatophyte infection and many deep mycotic infection with a drastic therapeutic effect, and what is more the preparation of the invented products is simple, low energy consumption and without special equipment the drug can be mass produced.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of an antifungal drug terbinafine, in particular to a terbinafine nanoemulsion antifungal drug and a preparation method thereof. Background technique [0002] Terbinafine is an allylamine broad-spectrum antifungal drug that can be taken orally or externally. )-N-methyl-1-naphthalene-methylamine, white or off-white crystalline powder, slightly soluble in water. Metabolized in the liver, distribution phase t 1 / 2 About 1.1 hours to eliminate phase t 1 / 2 About 16 hours. It is suitable for the treatment of tinea corporis, jock itch, tinea pedis, tinea unguium and skin candida infection caused by superficial fungi. In recent years, it has been found that it also has a strong therapeutic effect on many deep fungal infections. It selectively inhibits the squalene epoxidase of fungi, causing the accumulation of squalene in fungal cells, the lack of ergosterol, and the fat deposi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/135A61K9/107A61K47/30A61P31/10
Inventor 欧阳五庆杨宝平吴旭锦
Owner NORTHWEST A & F UNIV
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