An ophthalmic film formulation containing voriconazole

A voriconazole and ophthalmic technology, applied in the field of ophthalmic films containing voriconazole, can solve the problems of low drug loading, difficulty in making eye drops, and low water solubility of voriconazole, and achieve high bioavailability, easy operation, The effect of simple preparation method

Active Publication Date: 2019-01-29
ZHEJIANG UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility of voriconazole is low, and it is not easy to make eye drops, while the drug loading of ordinary ophthalmic films is relatively low

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • An ophthalmic film formulation containing voriconazole
  • An ophthalmic film formulation containing voriconazole
  • An ophthalmic film formulation containing voriconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] prescription:

[0031] Voriconazole 500mg

[0032] Polyvinyl alcohol-124 2.5g

[0033] Preparation method: Dissolve voriconazole in 6mL of ethanol, dissolve polyvinyl alcohol in 20mL of water, then slowly add the voriconazole solution into the polyvinyl alcohol solution and mix. Inject part of the mixed liquid into a 10mL medical syringe, and control the flow rate of 0.4ml / h through a micro-injection pump; set the spinning voltage to 18-19kv, lift the iron stand to adjust the distance between the collection device and the nozzle to 19-20cm, and wrap the receiving plate on it Aluminum foil, to collect the nanofibrous membrane. The collected nanofiber membrane was placed in a vacuum drying oven at room temperature to evaporate the solvent for 3 days. Then remove the film and cut it into 6mg films.

Embodiment 2

[0035] prescription:

[0036] Voriconazole 500mg

[0037] Polyacrylic resin EPO 15g

[0038] Triethyl citrate 3g

[0039] Preparation method: Dissolve voriconazole, polyacrylic resin EPO, and triethyl citrate in ethanol, then add it into a medical syringe, and control the flow rate of 0.4ml / h through a micro-injection pump; set the spinning voltage to 18-19kv, and lift the iron stand To adjust the distance between the collection device and the nozzle to 19-20cm, wrap the receiving plate with aluminum foil, and collect the nanofiber membrane. The collected nanofiber membrane was placed in a vacuum drying oven at room temperature to evaporate the solvent for 3 days. Then remove the film and cut it into 3.5mg films.

Embodiment 3

[0041] prescription:

[0042] Voriconazole 500mg

[0043] Polyvinylpyrrolidone K30 4.5g

[0044] Ethylparaben 0.045g

[0045]Preparation method: Dissolve voriconazole in 6mL of ethanol, dissolve polyvinylpyrrolidone K30 and ethylparaben in tetrahydrofuran, then slowly add voriconazole solution to polyvinylpyrrolidone K30 solution and mix. Inject the mixed liquid into a 10mL medical syringe, and control the flow rate to 0.4ml / h through a micro-injection pump; set the spinning voltage to 18-19kv, lift the iron stand to adjust the distance between the collection device and the nozzle to 19-20cm, and wrap the receiving plate with aluminum foil , to collect nanofibrous membranes. The collected nanofiber membrane was placed in a vacuum drying oven at room temperature to evaporate the solvent for 3 days. Then remove the film and cut it into 1mg films each.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
diameteraaaaaaaaaa
diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to an ocular insert containing voriconazole. The ocular insert is composed of nanometer polymer fiber comprising 1 part of voriconazole, 1-200 parts of film-forming material and 0-50 parts of auxiliary materials. The ocular insert is obtained through electrostatic spinning, the diameter of the nanometer polymer fiber is 10-1000 nm, and voriconazole is of an amorphous state in the ocular insert. The ocular insert containing voriconazole is composed of the fiber with a nanoscale diameter, has a large specific surface area, high porosity and high biocompatibility, and also has the remarkable advantages of being high in drug loading capacity, capable of releasing drugs in a sustained mode, high in bioavailability and the like.

Description

technical field [0001] The invention relates to ophthalmic preparations, in particular to an ophthalmic film containing voriconazole. Background technique [0002] Fungal keratitis is a common eye disease that seriously endangers visual function. With the widespread use of broad-spectrum antibiotics and corticosteroids, its incidence has increased year by year. Fungal keratitis has the characteristics of insidious onset, long course of disease, lack of specific therapy, and easy recurrence. It has become one of the diseases with a high clinical blinding rate. At present, for the treatment of fungal keratitis, systemic administration and local administration are the main clinical methods, supplemented by surgical treatment, but insensitivity to antifungal drugs during the treatment process is the main difficulty in the treatment of the disease at present. [0003] Voriconazole is an effective option for the treatment of ophthalmic fungal infectious diseases. The mechanism o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & AuthorityPatents(China)
IPC IPC(8): A61K9/70A61K31/506A61K47/32A61K47/38A61K47/36A61P31/10A61P27/02D01D5/00
CPCA61K9/0048A61K9/7007A61K31/506A61K47/32A61K47/36A61K47/38D01D5/0015
Inventor俞振伟孙晓译俞凌燕
OwnerZHEJIANG UNIV