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Microemulsion gel preparation of oxiconazole nitrate

A technology of oxyconazole nitrate and oxyconazole microemulsion, which is applied in the field of topical antifungal preparations and the topical targeted microemulsion gel preparations of imidazole antifungal oxyconazole nitrate, which can solve the problem of emulsions. The cream becomes thick, rough, difficult to apply, etc., to achieve the effect of fast onset, improved adhesion, and no pollution to clothes

Active Publication Date: 2013-05-29
湖南中威制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 3) In terms of stability, long-term storage will cause the cream to become thicker, difficult to apply, and feel rough with hands

Method used

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  • Microemulsion gel preparation of oxiconazole nitrate
  • Microemulsion gel preparation of oxiconazole nitrate
  • Microemulsion gel preparation of oxiconazole nitrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Prescription composition:

[0059]

[0060] Preparation process: 1) Weigh 0.57g of oxiconazole nitrate, 15.0g of polyoxyethylene hydrogenated castor oil, 5.00g of isopropanol, and 5.00g of GTCC, mix well at room temperature and stir, slowly add distilled water to 80.0g, stir And equilibrate for 22 minutes to obtain a uniform and transparent oxiconazole nitrate microemulsion; 2) Weigh 0.90 g of carbomer and 0.20 g of benzoic acid, add water to 20.0 g, fully swell overnight, and disperse evenly to obtain a blank gel; 3) Mix 1) with the oxiconazole nitrate microemulsion and blank gel in 2) and grind evenly, adjust the pH to neutral with triethanolamine, and obtain the oxiconazole nitrate microemulsion with a weight content of 0.50% of oxyconazole nitrate Glue preparation.

Embodiment 2

[0062] Prescription composition:

[0063]

[0064] Preparation process: 1) Weigh 1.15g of oxiconazole nitrate, 24.0g of caprylic glyceride of coconut oil, 16.0g of polyethylene glycol 400, and 5.00g of castor oil, mix well at room temperature and stir, and slowly add distilled water to 80.0g , stirred and equilibrated for 18 minutes to obtain uniform and transparent oxiconazole nitrate microemulsion; 2) Weigh 0.80 g of carbomer and 0.30 g of benzalkonium bromide, add water to 20.0 g, fully swell and disperse overnight to obtain a blank gel Gel; 3) 1) and 2) Oxiconazole nitrate microemulsion and blank gel are mixed and developed evenly, and the pH is adjusted to neutral with triethanolamine, and the obtained Oxiconazole nitrate with a weight content of 1.00% is Oxiconazole nitrate azole microemulsion gel preparation.

Embodiment 3

[0066] Prescription composition:

[0067]

[0068] Preparation process: 1) Weigh 1.15g of oxiconazole nitrate, 12.8g of polyoxyethylene hydrogenated castor oil, 6.40g of propylene glycol, and 4.80g of GTCC, mix well at room temperature and stir, slowly add distilled water to 80.0g, stir and balance 20min to obtain uniform and transparent oxiconazole nitrate microemulsion; 2) Weigh 1.20g of carbomer, 0.20g of benzoic acid, add water to 20.0g, fully swell and disperse overnight to obtain a blank gel; 3) mix 1 ) mixed with the oxiconazole nitrate microemulsion and blank gel in 2) and prepared evenly, and the pH was adjusted to neutral with triethanolamine to obtain an oxiconazole nitrate microemulsion gel preparation with a weight content of 1.00% of oxyconazole nitrate .

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Abstract

The invention relates to an external targeting microemulsion gel preparation of oxiconazole nitrate which is an antifungal medicament, and belongs to the field of pharmaceutical preparation. The preparation is mainly composed of oxiconazole nitrate, a surfactant, a cosurfactant, an oil phase, gel matrix, a preservative, a pH regulator and distilled water. The average particle size of the oxiconazole nitrate microemulsion is below 50nm and the polydipersity index (PDI) of particle size distribution is below 0.2. The preparation uses the new carrier-microemulsion for percutaneous administration; compared with the commercially available oxiconazole nitrate emulsifiable paste, the percutaneous transport time lag of the external targeting microemulsion gel preparation is short and the preparation takes effect quickly, has high penetration efficiency and high remainder ratio in epidermis and dermis and good targeting effect in epidermis and can release the medicament stably, thus the curative effect of the medicament can be increased and toxic or side effects and adverse reactions can be both reduced. The form of the microemulsion oxiconazole nitrate preparation is not limited to gel and the preparation can be an external preparation such as patch, paste, spray, ointment, cataplasm, cream and the like.

Description

technical field [0001] The invention relates to an external preparation of an antifungal drug, in particular to an external targeted microemulsion gel preparation of an imidazole antifungal drug oxiconazole nitrate, which belongs to the field of pharmaceutical preparations. Background technique [0002] Oxiconazole nitrate (Oxiconazole nitrate) is a new generation of imidazole broad-spectrum antifungal drugs. It was first launched in Switzerland for clinical use in 1983, and then its external creams and lotions were launched in the United States, Britain, Japan and other countries. At present, it is mainly used clinically for tinea pedis, jock itch, tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes or Epidermophyton flocculus infection, and pityriasis caused by Microsporum pityriasis. Treatment of fungal diseases. [0003] Oxiconazole nitrate inhibits the growth of fungi and is related to preventing the synthesis of ergosterol: ergosterol is the main...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/06A61K9/70A61K31/4164A61K47/32A61K47/34A61K47/38A61K47/44A61P31/10
Inventor 谭剑平常坦然蒋立新周志文
Owner 湖南中威制药有限公司
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