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Cyclosporine A micelle eye drop and preparing method thereof

A technology of cyclosporine and eye drops, applied in the direction of cyclic peptide components, capsule delivery, pharmaceutical formulations, etc., can solve the problems of unsatisfactory safety and economical efficiency, poor intraocular permeability, poor patient compliance, etc., to achieve The effect of prolonging the drug action time, reducing the number of administrations, and reducing the concentration of administration

Active Publication Date: 2013-04-24
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CsA oil eye drops are irritating to the eyes, poor patient compliance, and poor intraocular permeability. Existing conventional preparations require a higher concentration (usually 1% mass concentration) to achieve an effective therapeutic concentration. In terms of safety and Not very economically

Method used

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  • Cyclosporine A micelle eye drop and preparing method thereof
  • Cyclosporine A micelle eye drop and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Put 5 mg of cyclosporine A and 150 mg of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 50,000) in a 100 mL round-bottomed flask, add 10 mL of absolute ethanol, fully dissolve, and evaporate in a water bath at 40°C in a rotary vacuum. Water and ethanol to obtain a uniformly dispersed film of drug and copolymer, then add distilled water to fully wash the film, 300w power water bath ultrasonic 10min, to obtain a micellar solution. The micellar solution was passed through a 0.22 μm microporous membrane, and then freeze-dried to obtain the micellar powder. Then disperse and dissolve the micellar powder with 10 mL of borate buffer solution, add preservative benzalkonium chloride, and isotonic regulator sodium chloride, adjust the pH to 7.3, and then sterile filter and repack. The average particle size of cyclosporine A micelles measured by the laser particle size analyzer is 73nm, the dispersion index PDI=0.067, and the dispersion uniformity i...

Embodiment 2

[0015] Put 10 mg of cyclosporine A and 200 mg of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 100,000) in a 100 mL round bottom flask, add 10 mL of dichloromethane, fully dissolve, and evaporate in a water bath at 40°C in a rotary vacuum for two Chloromethane to obtain a uniformly dispersed film of drug and copolymer, then add distilled water to fully wash the film, 300w power water bath ultrasonic 10min, to obtain a micellar solution. The micellar solution was passed through a 0.22 μm microporous membrane, and then freeze-dried to obtain the micellar powder. Then use 20mL phosphate buffer to disperse and dissolve the micellar powder, add preservative benzalkonium chloride, and isotonic regulator sodium chloride, adjust the pH to 7.3, and then sterile filter and repack. The average particle size of cyclosporin A micelles measured by laser particle size analyzer is 86nm, the dispersion index PDI=0.200, and the dispersion uniformity is good. Th...

Embodiment 3

[0017] Put 25mg of cyclosporine A and 300mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 150,000) in a 500mL round bottom flask, add 30mL of dichloromethane, fully dissolve, and evaporate in a water bath at 40°C for two Chloromethane to obtain a uniformly dispersed film of drug and copolymer, then add distilled water to fully wash the film, 300w power water bath ultrasonic 10min, to obtain a micellar solution. The micellar solution was passed through a 0.22 μm microporous membrane, and then freeze-dried to obtain the micellar powder. Disperse and dissolve the micellar powder with 50 mL of phosphate buffer, add preservative benzalkonium chloride, and isotonicity regulator sodium chloride, adjust the pH to 7.3, and then sterile filter and repack. The average particle size of cyclosporine A micelles measured by the laser particle size analyzer is 110nm, the dispersion index PDI=0.162, and the dispersion uniformity is good. The cyclosporine...

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Abstract

The invention relates to a cyclosporine A micelle eye drop and a preparing method thereof. The cyclosporine A micelle eye drop comprises cyclosporine A used as a main drug, aseptic and isoosmotic adjusting agents, and is characterized by further comprising a copolymer of polythene caprolactam, polyvinyl acetate and polyethylene glycol used as drug auxiliary materials. The preparing method includes: preparing a cyclosporine A micelle through a solvent rotary evaporation film forming method; obtaining cyclosporine A micelle powder after filtering, freezing and drying the cyclosporine A micelle; and dispersing and dissolving the powder into a buffer solution to obtain the cyclosporine A micelle eye drop. According to the cyclosporine A micelle eye drop, the cyclosporine A has good solubility in a water solution, the micelle is small in particle diameter and uniform in distribution range and drug stability is good. The cyclosporine A micelle eye drop not only reduces drug irritation, but also improves drug absorption of a cornea, reduces drug concentration, prolongs drug action time, reduces dosing frequency, improves patient compliance, and has good economical efficiency.

Description

technical field [0001] The invention relates to a novel cyclosporin A eye drop, in particular to a cyclosporine A micellar eye drop and a preparation method thereof. Background technique [0002] Cyclosporin A (Cyclosporin A, CsA) is a third-generation immunosuppressant, which has been widely used in clinical ophthalmology. The efficacy of postoperative immune rejection has been recognized. However, the systemic administration of CsA is affected by the blood-ocular barrier factors, the ocular utilization is low, and it may cause complications such as renal toxicity, central nervous system toxicity, liver toxicity and hypertension, and its application is greatly limited. Such local administration methods can avoid the above-mentioned toxic and side effects. CsA drugs have large molecular weight, strong hydrophobicity, and are almost insoluble in water. Currently, oil eye drops are mainly used for topical administration of CsA in ophthalmology. CsA oil eye drops are irritat...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/51A61K38/13A61K47/34A61P37/06A61P27/02A61K47/32
Inventor 姜皓然史伟云吴祥根
Owner SHANDONG EYE INST
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