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Oil-in-water type compound ketoconazole nano-medicament and preparation method thereof

A compound ketoconazole nanometer, oil-in-water type technology, applied in the field of medicine, can solve the problems of large fluctuations in blood drug concentration, damage and allergic reactions, and low bioavailability, and achieve easy promotion, good invasiveness, good fluidity

Inactive Publication Date: 2013-04-10
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the oral dosage form dissolves in gastric acid and is easy to absorb, it is widely distributed after absorption, and the blood concentration fluctuates greatly, which will bring many adverse reactions such as nausea, vomiting, abdominal pain, headache, etc., and occasionally liver damage and allergic reactions
Although ointment and other external dosage forms can reduce adverse reactions and expand the scope of clinical reference, they have the disadvantages of unsatisfactory transdermal effect, poor stability, and low bioavailability. They need to use azone, DMF, DMSO and other skin penetration to promote enhances transdermal absorption

Method used

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  • Oil-in-water type compound ketoconazole nano-medicament and preparation method thereof
  • Oil-in-water type compound ketoconazole nano-medicament and preparation method thereof
  • Oil-in-water type compound ketoconazole nano-medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] 1) Weigh 0.77g of 2-phenylethanol, 0.23g of eugenol, 0.166g of ketoconazole, 0.01g of clobetasol propionate, 9g of Tween-80, 14.000g of distilled water, and set aside;

[0092] 2) Add ketoconazole and clobetasol propionate into 2-phenylethanol and stir evenly, then add eugenol and stir until completely dissolved;

[0093] 3) Add Tween-80 to the solution prepared in step 2) and stir evenly;

[0094] 4) Stir the solution prepared in step 3) rapidly at room temperature, slowly add distilled water dropwise while stirring, and keep stirring the system to form a transparent and clear liquid, which is the compound nanoemulsion drug.

Embodiment 2

[0096] It consists of 8.000g of Tween-80, 0.500g of ketoconazole, 1.000g of 2-phenylethanol, 0.100g of IPM, 0.300g of clobetasol propionate, 0.300g of eugenol, 2.000g of absolute ethanol, and 12.000g of distilled water.

Embodiment 3

[0098] It consists of 7.000g of EL40, 0.840g of ketoconazole, 0.900g of 2-phenylethanol, 0.060g of vitamin E oil, 0.012g of clobetasol propionate, 0.240g of eugenol, and 13.750g of distilled water.

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Abstract

The invention discloses an oil-in-water compound ketoconazole nano-medicament. The grain diameter of the medicament is 1-100nm. The oil-in-water compound ketoconazole nano medicament comprises the following raw materials in percentage by weight: 0.01-8.0 percent of ketoconazole, 0.01-10 percent of eugenol, 0.001-5.0 percent of clobetasol propionate, 25.0-45.0 percent of surfactant, 0-10.0 percentof cosurfactant, 0.1-25.0 percent of oil and the balance of distilled water. The oil-in-water compound ketoconazole nano-medicament can be used for treating stubborn skin mycotic infection, mycodermatitis, chronic mucocutaneous candidiasis, dermatitis blastomycosis, coccidioidomycosis, histoplasmosis, chromoblastomycosis and paracoccidioidomycosis, and dermatomycosis and tinea versicolor caused by dermatophyte and microzyme as well as trichophyton disease, scytitis and pruritus. The oil-in-water compound ketoconazole nano-medicament has the advantages of strong osmosis, favorable stability, favorable infiltrating property, durable acting time, remarkable effect, low cost, simple preparation method and convenience in popularization and application.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new compound dosage form of ketoconazole, eugenol and clobetasol propionate, in particular to an oil-in-water compound ketoconazole nano-medicine and a preparation method thereof. Background technique [0002] At present, the medicines for the clinical treatment of skin diseases mainly include compound ointment, injections, and oral dosage forms, but most of them are only for fungal diseases, mite diseases or eczema, and these diseases often occur at the same time, and there are few reports on the medicines for treating these skin diseases at the same time. Although the oral dosage form dissolves in gastric acid and is easily absorbed, it is widely distributed after absorption, and the blood concentration fluctuates greatly, which will bring many adverse reactions such as nausea, vomiting, abdominal pain, headache, etc., and occasionally liver damage and allergic reactions. Although ointme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/573A61K31/496A61K31/085A61K9/107A61P17/00A61P31/10A61P31/04A61P17/04A61P33/14A61P29/00
Inventor 欧阳五庆兰莹欧阳伸雨
Owner NORTHWEST A & F UNIV
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