Oil-in-water compound fluconazole nano-emulsion and preparation method thereof

A fluconazole nanometer, oil-in-water type technology, applied in the field of medicine, can solve the problems of difficult body absorption, low drug loading in aqueous solution, and low bioavailability, so as to improve bioavailability, increase drug loading, The effect of improving solubility

Inactive Publication Date: 2012-07-18
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are mainly several dosage forms of fluconazole tablets, capsules, powder injections and injections on the market, but because fluconazole is insoluble in water, its aqueous solution The drug loading is extremely low, and the bioavailability is low, it is not easy to be absorbed by the body, and the therapeutic effect is poor

Method used

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  • Oil-in-water compound fluconazole nano-emulsion and preparation method thereof
  • Oil-in-water compound fluconazole nano-emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 A kind of oil-in-water type compound fluconazole nanoemulsion drug, the quality of each component:

[0050] RH-40 25.00g, ethanol 10.00g, butyl acetate 15.00g, fluconazole 1.00g, magnolol 0.35g, distilled water 48.65g.

[0051] Above-mentioned each component is made compound recipe fluconazole nanoemulsion medicine, comprises the following steps:

[0052] 1) Add the above amount of fluconazole into the oil to make it fully dissolved, as the oil phase;

[0053] 2) Mix the amount of magnolol with the co-surfactant to fully dissolve it;

[0054] 3 adding the amount of surfactant and co-surfactant into the oil phase and mixing;

[0055] 4) Use distilled water as the water phase, stir the oil phase quickly at room temperature, slowly add the water phase dropwise while stirring, and keep stirring until the system becomes a transparent liquid, and the oil-in-water compound fluconazole nanoemulsion is obtained.

Embodiment 2

[0056] Example 2 A kind of oil-in-water type compound fluconazole nanoemulsion drug, the quality of each component:

[0057] Tween-80 35.00g, polyethylene glycol 600 3.00, ethanol 2.00g, ethyl acetate 3.00g, fluconazole 0.05g, magnolol 0.70g, distilled water 56.25g.

Embodiment 3

[0058] Example 3 A kind of oil-in-water type compound fluconazole nanoemulsion drug, the quality of each component:

[0059] 40.00 g of RH-40, 1.80 g of ethanol, 2.00 g of 1,2-propanediol, 15.00 g of carvacrol, 2.50 g of fluconazole, 0.01 g of magnolol, and 38.69 g of distilled water.

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Abstract

The invention discloses an oil-in-water compound fluconazole nano-emulsion antifungal drug, wherein the drop diameter of the nano-emulsion is between 1 and 100nm. The nano-emulsion comprises the following raw materials in percentage by mass: 25.00 to 40.00 percent of surfactant, 3.80 to 10.00 percent of cosurfactant, 3.00 to 25.00 percent of oil, 0.05 to 2.50 percent of fluconazole, 0.01 to 0.70 percent of magnolol, and the balance of distilled water. The nano-emulsion preparation is clear transparent liquid, and has good stability, so that the dissolubility of the fluconazole is improved, the defect of low bioavailability of the fluconazole in a body is overcome, the medicinal metabolizing time of the fluconazole in the body is delayed, the assistant dosage is reduced, and the product cost is reduced. The nano-emulsion has wide market prospect in pharmacy field.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to an oil-in-water type compound fluconazole nanoemulsion drug for treating superficial and deep infection of animals caused by candida and cryptococcus and skin mycosis and a preparation method thereof. Background technique [0002] Fluconazole, also known as Diflucan, is a drug for the treatment of fungal infections, and has therapeutic effects on fungal infections in humans and animals. Fluconazole is a fluorinated triazole antifungal drug. Its mechanism of action is to inhibit ergosterol synthase, an essential component of fungal cell membrane, to block ergosterol synthesis, destroy the integrity of fungal cell wall, and inhibit its growth and reproduction. This product has strong antibacterial activities against Candida albicans, Microsporum, Cryptococcus neoformans, Epidermophyton and Capsular Histoplasma. Oral absorption is good, widely distributed in the body, and can penetrate into t...

Claims

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Application Information

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IPC IPC(8): A61K31/4196A61K9/107A61K47/44A61P31/10A61K31/05
Inventor 欧阳五庆郑星星欧阳伸雨
Owner NORTHWEST A & F UNIV
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