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Intraocular nano particle freeze-dried powders and preparation method thereof

A freeze-dried powder and nanoparticle technology, applied in the field of medicine, can solve the problems of short duration of drug effect, increase the incidence of complications such as intraocular hemorrhage, cataract and retinal detachment, etc., and achieve the effects of prolonging the action time, small volume, and prolonging the release rate.

Inactive Publication Date: 2010-05-26
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after a single administration in the vitreous, the drug metabolism is faster and the drug effect is short-lived; multiple administrations will increase the incidence of intraocular hemorrhage, cataract, retinal detachment and other complications

Method used

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  • Intraocular nano particle freeze-dried powders and preparation method thereof
  • Intraocular nano particle freeze-dried powders and preparation method thereof
  • Intraocular nano particle freeze-dried powders and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A freeze-dried powder of nanoparticles for intraocular use, which comprises the following components:

[0021] The mass percent of polylactic acid polyglycolic acid copolymer PLGA is 80.8%;

[0022] The mass percent of dexamethasone acetate DA is 19.2%.

[0023] A preparation method for intraocular nanoparticle freeze-dried powder, comprising the steps of:

[0024] First, dissolve 50 mg of the glucocorticoid dexamethasone acetate DA in 1 ml of acetone as the inner water phase; dissolve 200 mg of poly(lactic-co-polyglycolic acid) PLGA in 9 ml of dichloromethane, and the concentration of PLGA is 2.0%, as the oil phase; the two are mixed under ice-bath conditions, while stirring at a high speed, the stirring speed is 30000 rpm for emulsification for 60 seconds to form water-in-oil type colostrum, internal water phase: oil phase=1: 9;

[0025] Next, under ice-bath conditions, the above-mentioned water-in-oil colostrum was added dropwise to 2.5% (w / v) polyvinyl alcohol PV...

Embodiment 2

[0037] A freeze-dried powder of nanoparticles for intraocular use, which comprises the following components:

[0038] The mass percent of polylactic acid polyglycolic acid copolymer PLGA is 54.7%;

[0039]The mass percent of dexamethasone acetate DA is 45.3%.

[0040] A freeze-dried powder of nanoparticles for intraocular use and a preparation method thereof, comprising the steps of:

[0041] First, dissolve 200 mg of the glucocorticoid dexamethasone acetate DA in 3 ml of acetone as the inner aqueous phase; dissolve 200 mg of polylactic acid polyglycolic acid copolymer PLGA in 9 ml of dichloromethane, and the concentration of polylactic acid polyglycolic acid copolymer PLGA is 2.2%, as the oil phase; the two are mixed under ice bath conditions, while stirring at a high speed, the stirring speed is 30000 rpm, forming water-in-oil colostrum, internal water phase: oil phase=1:3;

[0042] Next, under ice-bath conditions, the above-mentioned water-in-oil colostrum was added dropw...

Embodiment 3

[0054] A freeze-dried powder of nanoparticles for intraocular use, which comprises the following components:

[0055] The mass percent of polylactic acid PLA is 70%;

[0056] The mass percent of dexamethasone acetate DA is 30%.

[0057] A freeze-dried powder of nanoparticles for intraocular use and a preparation method thereof, comprising the steps of:

[0058] First, the glucocorticoid dexamethasone acetate DA 50mg was dissolved in 1ml acetone as the inner water phase; 100mg polylactic acid PLA was dissolved in 4.5ml methylene chloride, and the weight ratio concentration of polylactic acid PLA was 2.0%, as the oil phase; Mix the two under ice bath conditions, and at the same time, stir at a high speed of 30,000 rpm for emulsification for 60 seconds to form water-in-oil colostrum, the inner water phase: oil phase = 1:5;

[0059] Next, under ice-bath conditions, the above-mentioned water-in-oil type colostrum was added dropwise to 2.5% (v / w) polyvinyl alcohol PVA 40ml, and 40...

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Abstract

The invention relates to intraocular nano particle freeze-dried powders, which comprises polylactic acid (PLA) or polylactic-co-glycolic acid (PLGA) and glucocorticoids. The powders are prepared by the following steps: firstly, dissolving the glucocorticoids in acetone to serve as an inner water phase; dissolving the biodegradable polymer PAL or PLGA in methylene dichloride to serve as an oil phase; under the ice-bath condition, mixing the two mixtures, and stirring at high speed to form a water-in-oil type primary emulsion; secondly, under the ice-bath condition, dropwise adding polyvinyl alcohol (PVA) serving as an outer water phase in the primary emulsion to form a water-in-oil-in-water type multiple emulsion through the action of ultrasonication; and finally, stirring the water-in-oil-in-water type multiple emulsion in a stink cupboard and volatilizing an organic phase under reduced pressure, collecting and washing the sediments after centrifuging the product, removing the dissociative glucocorticoids and PVA by washing with distilled water, and then preparing and storing the freeze-dried powders. The intraocular nano particle freeze-dried powders have the characteristics of having large medicament-loading rate and uniform size distribution and capacities of slowly releasing the glucocorticoids, reducing times of repeated medicament administration for the vitreous cavity and reducing the generation of ocular complications.

Description

technical field [0001] The invention of the method relates to the technical field of medicine, in particular to a freeze-dried powder of nanoparticles for intraocular use and a preparation method thereof. Background technique [0002] Glucocorticoid (GS) drugs are commonly used in ophthalmology clinics, and have definite curative effects on intraocular proliferative lesions such as retinal choroidal neovascularization and intraocular inflammatory diseases such as uveitis and retinal vasculitis. In view of its systemic toxicity and side effects, as well as the unique barrier structure of the eyeball, it is generally believed that the intravitreal route of administration is superior to oral or intravenous administration. However, after a single administration in the vitreous, the drug metabolism and elimination are quicker, and the drug effect is short-lived; multiple administrations will increase the incidence of complications such as intraocular hemorrhage, cataract, and ret...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/34A61K31/573A61P27/02
Inventor 王雨生宋存先李越徐建锋王满燕杨菁张涛杨秀梅张鹏侯慧媛石圆圆张自峰朱洁惠延年
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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