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Cyclosporine microball preparation for treating endophthalmitis

A cyclosporine and preparation technology, applied in the directions of cyclic peptide components, bulk delivery, drug combination, etc., can solve the problems of recurrent inflammatory or chronic inflammatory reaction, bleeding, poor intraocular permeability, etc. - Restriction of eye barrier, long-lasting therapeutic effect, effect of good therapeutic effect

Inactive Publication Date: 2006-11-01
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nussenblatt et al. confirmed that direct injection of CsA into the vitreous cavity can prevent experimental autoimmune uveitis, but due to the short maintenance time of CsA in the vitreous cavity after injection, repeated injections may cause intraocular infection, bleeding and other complications
In addition, systemic medication is not only expensive, but also may cause complications such as kidney and liver toxicity damage and high blood pressure, so its application in ophthalmology is limited
At present, the topical application of CsA in the eye is mainly eye drops. Due to the large molecular weight and hydrophobicity of CsA, the intraocular permeability is poor, and it is difficult to achieve the curative effect of topical application in the eye.
[0004] Uveitis is an organ-specific autoimmune ophthalmic disease mediated by T cells, characterized by inflammation that invades the uvea and neural retina, mainly manifested as recurrent or chronic inflammatory reactions , the course of the disease is long, prone to chronicity and relapse, its etiology is complicated, the pathogenesis is not yet fully clear, and there is no ideal preventive and therapeutic measures at present

Method used

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  • Cyclosporine microball preparation for treating endophthalmitis
  • Cyclosporine microball preparation for treating endophthalmitis
  • Cyclosporine microball preparation for treating endophthalmitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] At room temperature, add cyclosporine A and PLGA (75 / 25, MW=15000) to a stoppered test tube to dissolve in dichloromethane. After fully dissolving, the organic phase is quickly poured into the aqueous phase stirred at a certain speed. and continued stirring at this speed for 6 min (800 rpm). Then, the system was dispersed into 200 ml of aqueous solution containing PVA (polyvinyl alcohol, concentration 0.1%), evaporated under magnetic stirring at room temperature for 5 hours, and the dichloromethane was removed to solidify the microspheres. Centrifuge at 4000 rpm for 15 min at 15°C. The supernatant was collected to obtain a microsphere suspension. The obtained microspheres were freeze-dried and stored. In clinical use, water for injection, normal saline for injection or glucose solution for injection is used to prepare microsphere suspension for intravitreal injection.

Embodiment 2

[0057] Preparation method of cyclosporine A-loaded microspheres

[0058] At room temperature, add cyclosporine A and PLGA (75 / 25, MW=15000) (the dosage ratio of drug to carrier material 10%, W / W) in a stoppered test tube to be dissolved in dichloromethane. , the organic phase was quickly poured into the aqueous phase stirred at a certain speed, and the stirring was continued at this speed for 6 min (stirring speed 800 rpm). Then, the system was dispersed in 200 ml of aqueous solution containing PVA (polyvinyl alcohol, concentration 5%), and under magnetic stirring at room temperature, dichloromethane was evaporated and removed to solidify the microspheres. Centrifuge at 4000 rpm for 15 min at 15°C. The supernatant was collected to obtain a microsphere suspension. The obtained microspheres were freeze-dried and stored.

[0059] The particle size distribution range of the prepared cyclosporine-loaded microspheres is 10-70 μm, the microspheres observed by scanning electron mic...

Embodiment 3

[0060] Embodiment 3, the preparation method of cyclosporine A-loaded microspheres

[0061] At room temperature, add cyclosporine A and PLGA (75 / 25, MW=15000) (the dosage ratio of drug to carrier material 20%, W / W) and Pluronic F68 (0.5%) in a stoppered test tube to dissolve together. After fully dissolving in dichloromethane, the organic phase was quickly poured into the aqueous phase stirred at a certain speed, and the stirring was continued at this speed for 6 min (stirring speed 1000 rpm). Then, the system was dispersed in 200 ml of aqueous solution containing PVA (polyvinyl alcohol, concentration 0.5%), and under magnetic stirring at room temperature, dichloromethane was evaporated and removed to solidify the microspheres. Centrifuge at 4000 rpm for 15 min at 15°C. The supernatant was collected to obtain a microsphere suspension. The obtained microspheres were freeze-dried and stored.

[0062] The particle size distribution range of the prepared cyclosporine-loaded micr...

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Abstract

An injection containing suspended microspheres carrying ciclosporin for treating endophthalmitis (such as uveitis) by injecting it into the vitreous body of eyeball is disclosed. Its advantages are slow release, long acting time and high curative effect.

Description

technical field [0001] The present invention relates to a new application of medicine, in particular to a method for administering cyclosporine-loaded microspheres for intravitreal injection, and the method for treating intraocular inflammation. The direct injection into the vitreous of the eyeball enables the slow release of the drug wrapped in the carrier material, and has a good therapeutic effect on intraocular inflammation such as uveitis, especially chronic uveitis. Background technique [0002] The invention relates to a microsphere preparation for ophthalmic injection, in particular to a long-acting cyclosporine intraocular drug delivery system in which a biodegradable polymer material is used as a carrier material. [0003] Cyclosporin A (Cyclosporin A, CsA, also referred to as cyclosporine) is a third-generation immunosuppressant, which is characterized by high efficiency and no bone marrow toxicity. It is a selective immunosuppressant and has been widely used clin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K9/16A61P27/02
Inventor 张强刘瑜玲王坚成何渊张华
Owner PEKING UNIV
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