Long-acting sustained-release preparation for treating fungal keratitis, preparation method and application thereof

A technology for fungal keratitis and sustained-release preparations, which is applied in the directions of antifungal agents, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of unsatisfactory long-acting sustained-release effect and poor patient compliance. , low bioavailability and other problems, to achieve the effect of improving drug bioavailability, large drug loading, and simple preparation method

Active Publication Date: 2018-07-31
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese invention patent CN201110380218 reports the use of polyethylene glycol 400, lecithin and other auxiliary materials to make nano-micro composite powder. Although the auxiliary materials used are safe, the particle size of the obtained drug is small and the dispersion is transparent, but the drug is easy to burst when it is released. , the long-term sustained-release effect is not ideal
[0004] At present, the commonly used ophthalmic antifungal preparations in clinical practice are mostly eye drops, which are made of water or buffer solution, have low bioavailability, require frequent administration, and have poor patient compliance

Method used

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  • Long-acting sustained-release preparation for treating fungal keratitis, preparation method and application thereof
  • Long-acting sustained-release preparation for treating fungal keratitis, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) Dissolve 2g of chitosan in 200mL of 2% (v / v) acetic acid solution, mechanically stir, transfer to a three-necked flask after 2 days, and prepare chitosan-acetic acid solution; take 7.6mL of 2mg / mL Graphene dispersion, 300W ultrasonic 30min, make it fully dispersed;

[0036] (2) Add the graphene dispersion liquid fully dispersed by ultrasound in step (1) to the chitosan-acetic acid solution prepared in step (1), and continue to stir for 5 hours at 60° C. to obtain chitosan electrostatically bonded graphite vinyl composites;

[0037] (3) Get the injection of voriconazole and dilute it with normal saline, and add it dropwise in the composite material of chitosan electrostatically bonded graphene prepared in step (2) under stirring state, so that the final concentration of voriconazole in the composite material is 5mg / mL, kept stirring at 30°C for 12h; put it into a dialysis bag (cut-off size 800Da), put it in deionized water to remove unloaded medicine, and after 12h...

Embodiment 2

[0039] (1) get 2g chitosan quaternary ammonium salt and be dissolved in the 1% (v / v) acetic acid solution of 200mL, mechanically stir, transfer in the there-necked flask after 1 day, prepare chitosan quaternary ammonium salt-acetic acid solution; Take 10mL of 2mg / mL graphene dispersion, 300W ultrasonic for 1h, to fully disperse;

[0040] (2) Add dropwise the graphene dispersion liquid after step (1) ultrasonically fully dispersed in the chitosan quaternary ammonium salt-acetic acid solution prepared in step (1), and continue stirring for 3 hours at 20° C. to obtain chitosan A composite material of quaternary ammonium salt electrostatically bonded to graphene;

[0041] (3) Get the injection of voriconazole and dilute it with normal saline, and add it dropwise in the composite material of chitosan quaternary ammonium salt electrostatically bound graphene prepared in step (2) under stirring, so that the final concentration of voriconazole in the composite material 8mg / mL, kept s...

Embodiment 3

[0043] (1) Dissolve 2g of chitosan in 200mL of 1.5% (v / v) acetic acid solution, mechanically stir, transfer to a three-necked flask after 3 days, and prepare chitosan-acetic acid solution; take 20mL of 2mg / mL carboxyl Graphene dispersion, 300W ultrasonic 1h, make it fully dispersed;

[0044] (2) Add the carboxygraphene dispersion liquid fully dispersed by ultrasound in step (1) to the chitosan-acetic acid solution prepared in step (1), and continue stirring for 1 hour at 80°C to obtain chitosan electrostatic binding Graphene composites;

[0045](3) Get the injection of voriconazole and dilute it with normal saline, and add it dropwise in the composite material of chitosan electrostatically bound carboxyl graphene prepared in step (2) under stirring, so that the final concentration of voriconazole in the composite material is 10mg / mL, continuously stirred for 8h at 50°C; put into a dialysis bag (cut-off size 800Da), place in deionized water to remove unloaded medicine, and af...

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Abstract

The invention relates to a preparation for treating antifungal drugs, in particular to a long-acting slow-release preparation for treating fungal keratitis and its preparation method and application. The matrix of the long-acting sustained-release preparation for the treatment of fungal keratitis according to the present invention is composed of graphene-like materials electrostatically combined with drug-loaded chitosan substances, and the drug is loaded on the sheet-like structure of graphene-like materials, and the structure is stable. Large load. The preparation has good antibacterial activity against fungi and bacteria, and has good cell compatibility, flexibility and tensile strength. The preparation can be easily and conveniently applied to the cornea, and has no toxic effect on normal tissues while achieving excellent antibacterial activity. As an ophthalmic dosage form, it can adhere to the patient's cornea for long-term sustained release to achieve an effective drug concentration, and the preparation is simple, the drug-loaded material itself has excellent antibacterial activity, good mechanical properties, and has no irritation to eye tissues. And toxic and side effects, easy to use and so on.

Description

technical field [0001] The invention relates to a preparation for treating antifungal drugs, in particular to a long-acting slow-release preparation for treating fungal keratitis and its preparation method and application. Background technique [0002] Fungal keratitis is a serious blinding eye disease. The main pathogens causing fungal keratitis are mainly saprophytic fungi, such as Fusarium and Aspergillus. With the general abuse of broad-spectrum antibiotics, corticosteroids and antiviral drugs clinically, the drug resistance of bacteria has been enhanced. In recent years, the incidence of fungal keratitis has gradually increased, and the condition has become more serious. [0003] Voriconazole (UK-109, 496) is a second-generation triazole broad-spectrum antifungal drug. Compared with traditional antifungal drugs such as amphotericin B and itraconazole, its antifungal spectrum is wider and its efficacy is stronger. for exact. However, because of its solubility difficult...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K47/36A61K9/06A61K31/506A61P27/02A61P31/10
Inventor 蒋刚彪袁进陈国普黄健菲阮仲航
Owner SOUTH CHINA AGRI UNIV
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