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Antifungal activity ophthalmopathy slow-release microparticle and use thereof

A nanoparticle and fungal technology, applied in the field of slow-release nanoparticles for antifungal ophthalmopathy, can solve problems such as serious adverse reactions and treatment interruption, and achieve the effects of improved medication economy and less medication dosage

Inactive Publication Date: 2009-03-25
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the application of ocular fungal infection, in order to achieve the effective drug concentration in the eye, a large dose of drug is required for systemic administration, and the adverse reactions are more serious, often leading to treatment interruption

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Take 175mg of voriconazole, take 7350mg of polylactide-glycolide with a molecular weight of 5000 Daltons and a polymerization ratio of lactide and glycolide of 40:60, dissolve it in 10ml of acetonitrile, and use oil-in-oil (O / O) Type emulsification-solvent evaporation method to prepare nanoparticles: drip into 400ml of 20% Span liquid paraffin solution under 800rpm stirring condition, after stirring for 10min, add cyclohexane to precipitate and settle the nanoparticles, and finally collect the nanoparticles by After repeated washing, the obtained nanoparticles are decompressed to remove the organic solvent, sterilized, and packaged. The nanoparticle prepared by this method has a drug load of 2%, an encapsulation rate of about 85.7%, a particle size of about 40 μm, and a daily release in vitro of about 3%.

Embodiment 2

[0022] By increasing the stirring at 800 rpm in Example 1 to 7500 rpm, voriconazole nanoparticles with a particle size of 100 nm can be prepared, and the drug loading and encapsulation efficiency have no obvious changes.

Embodiment 3

[0024] Take 175 mg of voriconazole, take 7350 mg of polylactide-glycolide with a molecular weight of 35,000 Daltons, and a polymerization ratio of lactide and glycolide of 40:60, dissolve it in 10 ml of acetonitrile, and use oil-in-oil (O / O) Voriconazole nanoparticles can be prepared by emulsification-solvent evaporation method, and the daily release in vitro can be controlled at about 1.8%.

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PUM

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Abstract

The invention relates to an anti-fungal ophthalmopathy sustained-release milli-microcapsule and the application thereof. The anti-fungal ophthalmopathy sustained-release milli-microcapsule contains voriconazole and is characterized in that the sustained-release milli-microcapsule also contains biodegradable pharmaceutical high-molecular auxiliary material; the voriconazolen and the biodegradable pharmaceutical high-molecular auxiliary material construct homogenized milli-microcapsule with the diameter of 100nm-100um; wherein, the voriconazolen accounts for 2%-50% of the total weight of the milli-microcapsule; the molecular weight of biodegradable pharmaceutical high-molecular auxiliary material is 5000-1000000Dolton. The pharmaceutical high-molecular auxiliary material is selected from poly(lactide-co-glycolide), polylactic acid, polylactic acid-glycolic acid. The anti-fungal ophthalmopathy sustained-release milli-microcapsule is widely applicable to the direct medicine delivery treatment in vitreous cavity or the ocular fungal infection prevention. The anti-fungal ophthalmopathy sustained-release milli-microcapsule treats fungal endophthalmitis through direct sustained-release vitreous cavity medicine delivery, needs less medicine dosage and effectively maintains the medicine concentration for 3 months after once medicine delivery so that the medicine economy is greatly improved. The medicine dosage applied on the ocular part is less when common voriconazolen injection is delivered systematically; patients cannot endure if the direct vitreous cavity injection needs to be conducted 3 times a day.

Description

technical field [0001] The present invention relates to an antifungal ophthalmic sustained-release nanoparticle and its application. Background technique [0002] In recent years, with the gradual increase in the application of antibiotics, glucocorticoids, immunosuppressants, corneal contact lenses, and vegetative trauma, the incidence of ocular fungal infections is on the rise, and it has become a difficult disease to treat and has a high rate of blindness. Infectious eye disease. [0003] Fungal endophthalmitis is a blinding eye disease that is difficult to treat clinically. The incidence rate is increasing year by year, and it greatly damages the structure of the eyeball and visual function. The existing treatment options include systemic injection or oral antifungal drugs, local ocular surface eye drops, direct injection at the infected site such as anterior chamber injection, intravitreal injection, etc. Systemic administration has problems such as poor curative effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/506A61K47/34A61P27/02A61P31/10
Inventor 谢立信董晓光吴祥根于常红
Owner SHANDONG EYE INST
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