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Azithromycin-containing slow-released eye drops and preparation method thereof

A technology for azithromycin and eye drops, applied to medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of low water solubility, instability, and unfavorable drug corneal penetration of azithromycin, and improve storage stability Sexuality, easy operation, and the effect of improving drug bioavailability

Inactive Publication Date: 2014-08-20
WUHAN WUYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The present invention is a sustained-release eye drop of azithromycin, which has the main advantage of encapsulating azithromycin in solid lipid nanoparticles, solving the problems of low water solubility and instability of azithromycin, and utilizing biodegradable, non-toxic, biological Water-soluble chitosan with good compatibility can modify the surface of solid lipid nanoparticles to construct an ocular drug delivery system with high stability and sustained release, which overcomes the surface charge of unmodified solid lipid nanoparticles. Negative charge, not conducive to the disadvantages of drug corneal penetration

Method used

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  • Azithromycin-containing slow-released eye drops and preparation method thereof
  • Azithromycin-containing slow-released eye drops and preparation method thereof
  • Azithromycin-containing slow-released eye drops and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0056] Prescription: 1000ml

[0057]

[0058] Preparation method: Weigh the prescribed amount of phospholipids, cholesterol and azithromycin, add them to 100mL of absolute ethanol, heat at 70°C, vortex to dissolve completely, keep them in a water bath, and use them as the organic phase; take another polysorbate 80 and The mixed solution of PEG400 is 300mL, which constitutes the inner water phase; the organic phase is slowly dropped into the inner water phase at the same temperature under stirring at 1200rpm with a 5# needle, and the stirring is continued to completely evaporate the organic solvent and concentrate the system to 100mL to obtain the initial phase. milk;

[0059] The resulting colostrum was quickly poured into 500 mL of continuous phase (0-4° C.) under stirring at 1000 rpm, and the continuous phase was chitosan, propylene glycol, mannitol and phosphate buffer (pH 6.5). Stir and continue to solidify for 2 hours, return to room temperature, add water for injecti...

Embodiment 2

[0061] Prescription: 1000ml

[0062]

[0063] Preparation method: Weigh the prescribed amount of phospholipids, cholesterol, vitamin E and azithromycin, add them to 100mL of methanol, heat at 70°C, vortex to dissolve completely, keep them in a water bath, and use them as the organic phase; The mixed solution of sesame oil and PEG2000 is 300mL, which constitutes the inner water phase; the organic phase is slowly dropped into the inner water phase at the same temperature under 1200rpm stirring with a 5# needle, and the stirring is continued to completely evaporate the organic solvent and concentrate the system to 100mL. Colostrum was obtained; the obtained colostrum was quickly poured into 500 mL of continuous phase (0-4° C.) under stirring at 1000 rpm, and the continuous phase was chitosan, sodium chloride, and sodium citrate buffer solution (pH 6.3). Stir and continue to solidify for 2 hours, return to room temperature, add water for injection to the full amount, and pass t...

Embodiment 3

[0065] Prescription: 1000ml

[0066]

[0067] Preparation method: Weigh the prescribed amount of phospholipids, cholesterol and azithromycin, add them to 100mL of absolute ethanol, heat at 70°C, vortex to dissolve completely, keep them in a water bath, and use them as the organic phase; 300mL of the mixed solution with butylated hydroxytoluene constitutes the internal water phase; the organic phase is slowly dropped into the internal water phase at the same temperature under 1200rpm stirring with a 5# needle, and the stirring is continued to completely evaporate the organic solvent and concentrate the system to 100mL to obtain colostrum; quickly pour the resulting colostrum into 500mL of 1000rpm stirring in the continuous phase (0-4 ° C), the continuous phase is chitosan, PEG6000, borax and phosphate buffer (pH6.8). Stir and continue to solidify for 2 hours, return to room temperature, add water for injection to the full amount, and pass through a 0.45 μm microporous membra...

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Abstract

The invention relates to slow-released eye drops with azithromycin as an effective ingredient and a preparation method thereof, and aims at solving the problems of poor water solubility of azithromycin and unstable physicochemical property of lipidosome. According to the preparation method, the emulsification evaporation-low-temperature curing method is used to prepare chitosan modified azithromycin solid lipid nanoparticles, so that the stability of lipid nanoparticles in storage is improved, slow release of azithromycin in eyes is also realized, and thus the medicine can fully act to realize the optimal treatment effect. The eye drops are mainly used for treating bacterial conjunctivitis.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an antibacterial slow-release eye drop with azithromycin as an active ingredient. technical background [0002] Bacterial conjunctivitis is the most common ophthalmic disease, accounting for about 5% of all conjunctivitis. It often causes damage to eye tissue in varying degrees, and sometimes has serious consequences and endangers vision. It is one of the main blinding eye diseases. Bacterial conjunctivitis is self-healing, but anti-infection treatment can shorten the disease process, prevent infection, and reduce complications. There are many types of pathogenic bacteria in bacterial conjunctivitis, Gram-positive Staphylococcus pneumoniae, Streptococcus pneumoniae, and Haemophilus influenzae are the most common pathogens. Antibiotics are currently the main means of treating bacterial conjunctivitis, and are widely used clinically because of their rapid action and obvi...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/08A61K31/7052A61K47/36A61P27/02A61P31/04A61P31/02
Inventor 祁梅芳杨波耿海明于艳春
Owner WUHAN WUYAO SCI & TECH
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