Cyclosporine microball preparation for treating endophthalmitis

A technology of cyclosporine and microspheres, which is applied in the direction of cyclic peptide components, bulk delivery, drug combination, etc., can solve the problems of recurrent or chronic inflammatory reactions, poor intraocular permeability, easy recurrence, etc., and achieve Overcome the limitation of the blood-ocular barrier, good therapeutic effect, no toxic and side effects

Inactive Publication Date: 2008-11-12
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

[0054] At room temperature, add cyclosporin A and PLGA (75 / 25, MW=15000) into a stoppered test tube and dissolve in dichloromethane. After fully dissolving, pour the organic phase into the water phase stirred at a certain speed In, and continue stirring at this speed for 6min (800rpm). Then the system was dispersed into 200 ml aqueous solution containing PVA (polyvinyl alcohol, concentration 0.1%), and was volatilized for 5 hours under magnetic stirring at room temperature to remove dichloromethane to solidify the microspheres. Centrifuge at 4000rpm at 15°C for 15min. Collect the supernatant to obtain microsphere suspension. The obtained microspheres were stored freeze-dried. For clinical use, use water for injection, normal saline for injection or glucose solution for injection to make a microsphere suspension, and inject it into the vitreous of the eyeball.

Embodiment 2

[0056] The preparation method of cyclosporin A microsphere

[0057] At room temperature, add cyclosporine A and PLGA (75 / 25, MW=15000) (10% ratio of drug to carrier material, W / W) in dichloromethane in a stoppered test tube, and after fully dissolving , the organic phase was quickly poured into the aqueous phase stirred at a certain speed, and continued to stir at this speed for 6min (stirring speed 800rpm). Then this system was dispersed in 200ml aqueous solution containing PVA (polyvinyl alcohol, concentration 5%), and under magnetic stirring at room temperature, dichloromethane was volatilized and removed to solidify the microspheres. Centrifuge at 4000rpm at 15°C for 15min. Collect the supernatant to obtain microsphere suspension. The obtained microspheres were stored freeze-dried.

[0058] The prepared cyclosporine-loaded microspheres have a particle size distribution range of 10-70 μm, and the microsphere particles are observed by a scanning electron microscope to sho...

Embodiment 3

[0059] Embodiment 3, the preparation method of carrying cyclosporin A microsphere

[0060] At room temperature, add cyclosporin A and PLGA (75 / 25, MW=15000) (drug to carrier material ratio 20%, W / W) and pluronic F68 (0.5%) co-dissolved in a stoppered test tube In dichloromethane, after fully dissolving, the organic phase was quickly poured into the aqueous phase stirred at a certain speed, and continued to stir at this speed for 6 minutes (stirring speed 1000rpm). Then the system was dispersed into 200 ml aqueous solution containing PVA (polyvinyl alcohol, concentration 0.5%), and under magnetic stirring at room temperature, dichloromethane was volatilized and removed to solidify the microspheres. Centrifuge at 4000rpm at 15°C for 15min. Collect the supernatant to obtain microsphere suspension. The obtained microspheres were stored freeze-dried.

[0061] The prepared cyclosporine-loaded microspheres have a particle size distribution range of 10-70 μm, and the microsphere pa...

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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 Patents(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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