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Cation adhesion type natamycin nano eye drops

A technology of natamycin and eye drops, which is applied in the field of cation-adhesive natamycin nano-eye drops, can solve the problems of limited application and difficulty in achieving sustained release of ordinary suspensions, and achieve improved safety and Efficacy, prolonging the duration of action of the drug, altering the effect of corneal resorption characteristics

Active Publication Date: 2010-06-09
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the solubility and dissolution rate of the drug in tears are affected by the secretion of tears, it is difficult for ordinary suspensions to achieve sustained release, which greatly limits the clinical application of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 1.5g natamycin and 0.03mg phospholipids are dissolved in 50ml ether, and the ether is fully removed by rotary evaporation to obtain a uniformly dispersed film of medicine and phospholipids, then add 0.6% chitosan (molecular weight 5000, deacetylation degree 85%) solution 0.5ml and 0.5% F-68 solution 6ml, fully wash the membrane, ultrasonically disperse evenly to obtain an emulsion, pass the emulsion through a high-pressure homogenizer, first use 500bar pressure cycle for 5 times for initial crushing, and then use 1500bar pressure cycle for 15 times Further finely pulverized, then the homogeneous emulsion was fixed to 30ml with water for injection, the osmotic pressure was adjusted to isotonicity with sodium chloride, and the pH value of dilute hydrochloric acid was adjusted to 6.5 to obtain cationic adhesion type natamycin nanosuspension drops. eye drops. The particle size of the nanosuspension measured by the laser particle size potential analyzer is 480nm±131nm, and t...

Embodiment 2

[0024] 1.5g natamycin and 0.6g phospholipids were dissolved in 50ml ether, and the ether was fully removed by rotary evaporation to obtain a uniformly dispersed film of medicine and phospholipids, and then 1.2g chitosan and F Dissolve -686g in 25ml of water for injection and fully dissolve, fully wash the membrane with the solution of chitosan and F-68, and obtain an emulsion after ultrasonic dispersion, pass the emulsion through a high-pressure homogenizer, and first use 500bar pressure cycle 5 times for initial Pulverize, and then use 1500bar pressure cycle for 15 times to further finely pulverize, then dilute the homogeneous emulsion to 30ml with water for injection, adjust the osmotic pressure to isotonic with sodium chloride, and adjust the pH value of dilute hydrochloric acid to 6.5 to obtain cationic adhesion Natamycin Nanosuspension Eye Drops. The particle size of the nanosuspension measured by the laser particle size potential analyzer is 480nm±131nm, and the particle...

Embodiment 3

[0026] The present invention can also be obtained by replacing the chitosan in Example 1 with a chitosan with a molecular weight of 300,000 and a deacetylation degree of 85%. The particle size of the nanosuspension measured by the optical particle size potential analyzer is 530nm±186nm, and the particle surface potential is +47mV. The obtained nano-suspension was kept at 4° C. in the dark for 6 months without substantial change in particle size and potential.

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PUM

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Abstract

A cationic adhesive-type natamycin nanometer eye drop comprises natamycin, a proper amount of osmoregulator and pH regulator. The eye drop is characterized by further comprising chitosan, pluronic F-68 and phospholipid, wherein, the mass percent concentration of the phospholipid in the eye drop is 0.01-2%, the mass percent concentration of the pluronic F-68 in the eye drop is 0.1-20%, and the masspercent concentration of the chitosan in the eye drop is 0.01-4%. The molecular weight of the chitosan is 5000-300000, and the deacetylation degree of the chitosan is greater than 85%. The natamycinnanometer eye drop is characterized by making a common natamycin suspension into suspension particles with the diameter ranging from 10nm to 1000nm, thus increasing solubility of the eye drop and enhancing safety and effectiveness. The natamycin particles of the common suspension are modified by the phospholipid and the chitosan to cause the particles to be positively charged, which is helpful toimprove absorption of the eye drop by cornea, enhances drug effect and prolongs the action time of the eye drop. And the chitosan has bioadhesion function, which enhances the adhesiveness between medicinal particles and the cornea.

Description

[0001] The invention relates to a novel natamycin eye drop, in particular to a cationic adhesion type natamycin nano eye drop. Background technique [0002] In recent years, with the gradual increase in the application of antibiotics, glucocorticoids, immunosuppressants, corneal contact lenses, and vegetative trauma, the incidence of ocular fungal infections is on the rise, and it has become a difficult disease to treat and has a high rate of blindness. Infectious eye disease. The main pathogenic bacteria are Fusarium and Aspergillus, and the pathogenic genera present diversity. The most common fungal infection of the eye is fungal keratitis. [0003] Fungal keratitis (fungal keratitis) is a common blinding eye disease worldwide, and it is more common in developing countries dominated by agricultural populations. In recent years, fungal keratitis has been increasing year by year in China, and has become the leading cause of corneal blindness in some areas. At present, due t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P27/02A61K47/36A61P31/10A61K31/7048A61K47/24A61K9/08
Inventor 史伟云吴祥根
Owner SHANDONG EYE INST
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