Preparation of cyclosporine A nano-particle eye drop

A technology of cyclosporine and eye drops, which is applied in the directions of inactive medical preparations, cyclic peptide components, sensory diseases, etc., can solve the problems of low bioavailability, poor water solubility, large toxic and side effects, etc. Convenience, reduce toxic and side effects, and reduce production costs

Inactive Publication Date: 2011-10-12
BEIJING INST OF OPHTHALMOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to provide a preparation method of cyclosporine A nano eye drops, to overcome the existing defects of cyclosporine A such as poor water solubility, low bioavailability, and large toxic and side effects

Method used

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  • Preparation of cyclosporine A nano-particle eye drop
  • Preparation of cyclosporine A nano-particle eye drop
  • Preparation of cyclosporine A nano-particle eye drop

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Experimental program
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specific Embodiment approach

[0049] Using the emulsified solvent evaporation method, polyethylene glycol-polylactic acid copolymer was used to encapsulate cyclosporine A drug, and spherical nanoparticles with a particle size of about 296.9±32.06nm were obtained, the drug loading was 17.02%, and the encapsulation efficiency is 85.10%. The specific implementation is as follows:

[0050] (1) Dissolve 50mg of polyethylene glycol-polylactic acid copolymer in 6mL of dichloromethane solution, 10mg of cyclosporine A in 0.5mL of dichloromethane, mix the two, and add the mixed solution to the solution containing 0.6% surfactant 20mL water of polyvinyl alcohol (PVA), at room temperature, magnetically stirred for 10min;

[0051] (2) The above solution is mixed with a high-pressure homogenizer to form an emulsion;

[0052] (3) the emulsion removes methylene chloride with a rotary evaporator;

[0053] (4) Centrifuge at 12,500 rpm for 6 minutes, redissolve in normal saline, and obtain cyclosporine A polyethylene glyc...

Embodiment 2

[0057] Using the emulsified solvent evaporation method, the polyethylene glycol-polylactic acid copolymer was used to encapsulate the cyclosporine A drug to obtain spherical nanoparticles with a particle size of about 252.7±27.29nm, the drug loading was 6.98%, and the encapsulation efficiency is 69.80%. The specific implementation is as follows:

[0058] (1) Dissolve 50mg of polyethylene glycol-polylactic acid copolymer in 6mL of dichloromethane solution, 5mg of cyclosporin A in 0.5mL of dichloromethane, mix the two, and add the mixed solution to the solution containing 0.6% surfactant 20mL water of polyvinyl alcohol (PVA), at room temperature, magnetically stirred for 10min;

[0059] (2) The above solution is mixed with a high-pressure homogenizer to form an emulsion;

[0060] (3) the emulsion removes methylene chloride with a rotary evaporator;

[0061] (4) Centrifuge at 12,500 rpm for 6 minutes, redissolve in normal saline, and obtain cyclosporine A polyethylene glycol-p...

Embodiment 3

[0063] Using the nanoprecipitation method, polyethylene glycol-polylactic acid copolymer was used to encapsulate cyclosporine A drug, and spherical nanoparticles with a particle size of about 99.27±18.31nm were obtained, the drug loading was 0.84%, and the encapsulation efficiency 42.26%. The specific implementation is as follows:

[0064] (1) Dissolve 20 mg of polyethylene glycol-polylactic acid copolymer in 3 mL of acetone solution, and 0.4 mg of cyclosporine A in 2 mL of acetone solution as the oil phase;

[0065] (2) Add 5 mL of the oil phase dropwise to 10 mL of mechanically stirred water, and stir for 30 min;

[0066] (3) the emulsion removes the organic solvent with a rotary evaporator;

[0067] (4) Centrifuge at 13,000rpm for 10min, redissolve in normal saline, and obtain cyclosporine A polyethylene glycol-polylactic acid copolymer nano eye drops;

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Abstract

The invention relates to cyclosporine A-carrying polyethylene glycol-polylactic acid copolymer nano eye drop, prepared by the following two methods: method 1: dissolving a polymer and cyclosporine A in an organic solvent, magnetically stirring the organic solvent with a water solution containing a surfactant, breaking by a high pressure homogenizer to prepare an emulsion, then removing the organic solvent by a rotary evaporator, centrifuging, and re-dissolving in normal saline to obtain the cyclosporine A-carrying polyethylene glycol-polylactic acid copolymer nano eye drop; and method 2: dissolving a polymer and cyclosporine A in an organic solvent, and slowly dropwise adding into water while magnetically stirring to prepare the cyclosporine A-carrying polyethylene glycol-polylactic acid copolymer nano eye drop. The drug-carrying nano eye drop prepared by the methods can obviously improve the water solubility of cyclosporine A.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a preparation method of cyclosporin A-loaded polyethylene glycol-polylactic acid copolymer nanometer eye drops. technical background [0002] Cyclosporin A (CsA), as a potent immunosuppressant, can effectively inhibit immune rejection after keratoplasty, but because it is insoluble in water, it cannot be formulated into water-soluble preparations for local ocular use. The method of systemic administration has been adopted, such as oral administration of cyclosporine A. According to the monitoring of the concentration of cyclosporine A in the blood, the effective drug concentration cannot be reached 2 hours and 24 hours after administration. At the same time, the drug has a strong inhibitory effect on the activation of T cells, which can lead to a decrease in systemic immunity, and can also cause serious side effects such as hypertension, liver and kidney toxicity, or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K9/00A61K47/34A61P37/06A61P27/02
Inventor 马科吴雁张海娟韩东徐清游玉霞
Owner BEIJING INST OF OPHTHALMOLOGY
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