Nanometer itraconazole external preparation and preparation method and use thereof

A technology of itraconazole and external preparations, applied in the field of medicine, can solve the problems of difficult absorption, low absorption rate of itraconazole, low skin penetration, etc., achieve bioavailability improvement, avoid liver toxicity, enhance The effect of curative effect

Inactive Publication Date: 2011-06-08
江苏小林制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Itraconazole is currently clinically mainly administered orally or intravenously, but the disadvantage is that it has certain liver toxicity. We have changed itraconazole from intravenous or oral administration to topical administration. The key is to use itraconazole The original systemic administration of conazole was changed to local topical administration, using the skin tissue as a penetration barrier to limit the absorption of itraconazole in the huma

Method used

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  • Nanometer itraconazole external preparation and preparation method and use thereof
  • Nanometer itraconazole external preparation and preparation method and use thereof
  • Nanometer itraconazole external preparation and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The raw material of itraconazole is pulverized into an average particle size of 150nm by nanotechnology materials, and itraconazole cream is prepared according to the following prescription:

[0017] Itraconazole 10g

[0018] Octadecanol 75g

[0019] Glyceryl monostearate 30g

[0020] White Vaseline 50g

[0021] Liquid paraffin 100g

[0022] Glycerin 75g

[0023] Sodium Lauryl Sulfate 10g

[0024] Methylparaben 1g

[0025] Add water to 1000g

[0026] The raw material of itraconazole is pulverized into an average particle size of 150nm by nanotechnology material, and it is set aside. Take stearyl alcohol, glyceryl monostearate, white petrolatum, and liquid paraffin and heat and melt to form an oil phase, and keep warm at 80-85°C. In addition, the water is heated to 80-85°C, and the prescribed amount of sodium lauryl sulfate and methyl paraben are added to dissolve into the water phase. Pour the water phase into the oil phase, stir while adding, stop heating afte...

Embodiment 2

[0028] The raw material of itraconazole is pulverized into an average particle size of 600nm by nanotechnology materials, and itraconazole cream is prepared according to the following prescription:

[0029] Itraconazole 50g

[0030] Stearic acid 50g

[0031] Glyceryl monostearate 40g

[0032] Octadecanol 55g

[0033] White Vaseline 50g

[0034] Liquid paraffin 55g

[0035] Glycerin 60g

[0036] Tween 80 35g

[0037] Span 60 5g

[0038] EDTA 1g

[0039] Methylparaben 1g

[0040] Add water to 1000g

[0041] The raw material of itraconazole is pulverized into an average particle size of 600nm by nanotechnology material, and it is set aside. Take stearic acid, stearyl alcohol, glyceryl monostearate, white petrolatum, liquid paraffin, and Span 60 and heat and melt to form an oil phase, and keep warm to 80-85°C. In addition, the water is heated to 80-85°C, and then the prescribed amount of Tween 80, methylparaben and EDTA are added to dissolve into the water phase. Pour ...

Embodiment 3

[0043] The itraconazole raw material is pulverized into an average particle size of 150nm by nanotechnology material, and itraconazole ointment is prepared according to the following prescription:

[0044] Itraconazole 50g

[0045] White Vaseline 850g

[0046] Liquid paraffin 50g

[0047] Solid paraffin 50g

[0048] The raw material of itraconazole is pulverized into an average particle size of 150nm by nanotechnology material, and it is set aside. Take white vaseline and solid paraffin and heat to melt, and stir to room temperature. Add the main ingredient into the prescribed amount of liquid paraffin, stir to disperse evenly, pour into the ointment base, and stir evenly. Measure the content, fill and package to obtain itraconazole ointment.

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Abstract

The invention provides a nanometer itraconazole external preparation and a preparation method and a use thereof, and the nanometer itraconazole external preparation comprises components of nanometer itraconazole and a matrix, wherein the matrix is selected from the multiple components of octodecyl alcohol, cetyl alcohol, stearic acid, isostearic acid, glyceryl monostearate, white vaseline, sodium lauryl sulfate, glycerin, liquid paraffin, solid paraffin, tween-80, tween-60, span-60, span-80, polyethylene glycol 4000, polyethylene glycol 400, polyethylene glycol 200, carbomer, propylene glycol, ethanol, benzyl alcohol, triethanolamine, carboxylation methyl cellulose, EDTA (ethylenediamine tetraacetic acid) or methyl hydroxybenzoate, and the content of the nanometer itraconazole is 0.1% by weight-10% by weight. By adopting the nanometer itraconazole external preparation, the shortcomings that the itraconazole is difficult to absorb in the external preparation, the skin penetration is not high and the percutaneous absorption rate of the itraconazole is not high are solved, the hepatotoxicity of the itraconazole during metabolism process of a human body is avoided, the bioavailability is improved, and a new administration way is provided for a patient.

Description

field of invention [0001] The invention relates to the technical field of medicine, in particular to a nano-scale itraconazole external preparation, its preparation method and its application. Background technique [0002] Itraconazole is a second-generation triazole synthetic antifungal drug with a broad antibacterial spectrum. These fungi mainly include dermatophytes (Trichophyton, Microsporum, and Epidermophyton floccosum), Yeasts (Candida species include Candida albicans, Candida glabrata, and Candida krusei; Cryptococcus neoformans; Malassezia; Trichosporum; Geotrichum), Aspergillus, Histoplasma, Paramecia brasiliensis Coccidioides, Sporothrix schenckii, Dusky fungi, Cladosporium, Blastomyces dermatitidis, Pseudoarishia bordetii, Penicillium manefei and many other yeasts and molds. [0003] Itraconazole is currently clinically mainly administered orally or intravenously, but the disadvantage is that it has certain liver toxicity. We have changed itraconazole from intra...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/06A61K31/496A61K47/12A61K47/14A61K47/16A61K47/20A61K47/22A61K47/32A61K47/34A61K47/38A61K47/44A61P31/10A61K47/10
Inventor 殷雨林郭尊武邓建华周玉琢王福东
Owner 江苏小林制药有限公司
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