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Preparation method of econazole nitrate/polyacrylic resin cationic nanoparticles

A technology of polyacrylic acid resin and econazole nitrate, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations. Effect

Inactive Publication Date: 2012-01-11
河南省眼科研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the zeta potential of RS100 nanoparticles prepared by Pignatello et al. is less than +20mV, and some experimental groups are even lower than 5mV, which is not very ideal.

Method used

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  • Preparation method of econazole nitrate/polyacrylic resin cationic nanoparticles
  • Preparation method of econazole nitrate/polyacrylic resin cationic nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: Polyether F-68 was dissolved in phosphate buffer to obtain an aqueous phase, econazole nitrate and polyacrylic resin RS100 were dissolved in a mixed solution of acetone and ethanol to obtain an organic phase, and the organic phase was added to water Reaction in phase to obtain primary econazole nitrate / polyacrylic acid resin nanoparticle colloidal solution, then use vacuum evaporation method combined with ultrafiltration to remove organic solvent and unreacted F-68, then add osmotic pressure regulator and antibacterial agent and a buffering agent, and finally adjust the pH value to 4.5-7.0 to obtain econazole nitrate / polyacrylic acid resin nanoparticles.

[0015] The osmotic pressure regulator is glycerin or mannitol, the bacteriostatic agent is benzalkonium chloride, benzalkonium bromide or ethylparaben, and the buffer is phosphate. The phosphate is NaH 2 PO 3 、Na 2 HPO 3 or KH 2 PO 3 . The aqueous phase is prepared by dissolving 1 gram of F-68 in 50-...

Embodiment 2

[0016] Example 2: Take 1.0 g of polyether F-68 and dissolve it in 80 ml of disodium hydrogen phosphate buffer solution with a pH of 5.85 to obtain an aqueous phase.

[0017] Take 2ml of acetone and 13ml of ethanol and mix evenly, dissolve 0.0613g of econazole nitrate and 0.3635g of RS100 in the above mixture, and shake fully to dissolve the two to obtain the organic phase.

[0018] Take the organic phase, slowly drop it into the water phase under stirring, continue stirring for 30 minutes after injection, and obtain the primary econazole nitrate / polyacrylic acid resin nanoparticle colloid solution A.

[0019] Take liquid A, and remove the organic solvent under vacuum at a constant temperature of 60°C until the volume is reduced to 60ml to obtain liquid B.

[0020] Take liquid B, dilute to 100ml, perform ultrafiltration with vivo-50 ultrafilter, concentrate to 20ml, and then dilute to 100ml, repeat 3 times to obtain liquid C.

[0021] Take 50ml of liquid C, add 0.4g of disodiu...

Embodiment 3

[0024] Example 3: 1.1 g of F-68 was taken and dissolved in 100 ml of disodium hydrogen phosphate buffer solution with a pH of 5.85 to obtain an aqueous phase.

[0025] Mix 4ml of acetone with 20ml of ethanol. Dissolve 0.0635g of econazole nitrate and 0.4756g of RS100 in the above mixed liquid, shake fully to dissolve the two to obtain the organic phase.

[0026] Take the organic phase, stir it, slowly drop it into the water phase, and continue stirring for 30 minutes after injection to obtain the primary econazole nitrate / polyacrylic acid resin nanoparticle colloid solution A.

[0027] Take liquid A, and remove the organic solvent under vacuum at a constant temperature of 60°C until the volume is reduced to 80ml to obtain liquid B.

[0028] Take liquid B, dilute it to 125ml, perform ultrafiltration with a vivo-50 ultrafilter, concentrate to 25ml, and then dilute to 125ml, repeat 3 times to obtain liquid C.

[0029] Take 50ml of liquid C, add 0.25g of disodium hydrogen phosph...

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Abstract

The invention discloses a preparation method of econazole nitrate / polyacrylic resin nanoparticles. The preparation method comprises the steps of: dissolving polyether F-68 in a phosphate buffer solution to obtain an aqueous phase, dissolving econazole nitrate and polyacrylic resin RS100 in a mixed solution of acetone and ethanol to obtain an organic phase, adding the organic phase into the aqueous phase for reaction, then removing an organic solvent and unreacted F-68, then adding an osmotic pressure regulator, a bacteriostat and a buffer, and finally regulating a pH value to be 4.5-7.0. In the invention, a solvent-diffusion method is used for preparing econazole nitrate / RS100 nanoparticles, a vacuum volatilization method is combined with an ultrafiltration method to remove the organic solvent, buffer salt and a free surfactant, and a preservative, the osmotic pressure regulator and a thickener are added after volume metering to prepare an econazole nitrate / RS100 nanoparticle colloidal solution, which has the zeta potential ranging from +26mV to +35Mv, has stronger medicine carrying capacity and is particularly suitable for ocular surface medication.

Description

technical field [0001] The invention belongs to pharmaceutical preparations, in particular to a preparation method of econazole nitrate polyacrylic acid resin nanoparticles. Background technique [0002] Econazole ECZ is an antifungal drug that can be used on the skin, cavities and mucous membranes. According to the in vitro antibacterial test, its bacterial spectrum is suitable for infected patients in my country, and its antibacterial effect on Aspergillus fumigatus and Fusarium fungi is better. According to literature reports, 2% ECZ and 5% natamycin have the same antibacterial efficacy. ECZ is almost insoluble in water, soluble in methanol, slightly soluble in ethanol, slightly soluble in chloroform and dichloromethane, almost insoluble in ether. Due to its special chemical properties, his corneal permeability is extremely poor, which directly limits the clinical application of the drug in ophthalmology. Improving the corneal penetration of ECZ and increasing its resi...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4174A61K47/32A61P31/10
Inventor 周天洋王丽娅张俊杰
Owner 河南省眼科研究所
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