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Intra-ocular release system of voriconazole

A technology of voriconazole ophthalmic and voriconazole, which is applied in the field of long-acting voriconazole intraocular drug delivery system, which can solve the problems of treatment interruption and serious adverse reactions, achieve high local concentration, reduce adverse reactions, and improve compliance

Inactive Publication Date: 2010-12-29
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the application of ocular fungal infection, in order to achieve the effective drug concentration in the eye, a large dose of drug is required for systemic administration, and the adverse reactions are more serious, often leading to treatment interruption

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Take 250 mg of polylactide-glycolide with a molecular weight of 5000 Daltons, dissolve it in 5 ml of dichloromethane, add 250 mg of voriconazole powder, stir and dissolve evenly, inject it into a polytetrafluoroethylene mold, control the airflow speed, and volatilize the dichloromethane. After being completely dried, the polylactide-glycolide drug delivery system containing voriconazole was removed from the polytetrafluoroethylene mold, and kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent to obtain a thickness of 1.5-2 1.5-2 mm thick and 1.5-2 mm thick voriconazole preparations with a 1.5-2 mm pore size die.

Embodiment 2

[0018] According to the method and steps of Example 1, but adopting 500 mg of polylactide-glycolide with a molecular weight of 1,000,000 Daltons, 10 ml of dichloromethane, 250 mg of voriconazole medicine, and 15 mg of a pore-forming agent to make a medicine stick with a diameter of 2 mm, in After removing the pore-forming agent, a drug rod with a diameter of 2 mm and a pore structure of 10 microns was obtained, kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent, and then cut into a voriconazole release preparation with a length of 2 mm. The voriconazole preparation is sterilized and sterilized by fumigation with ethylene oxide for 24 hours, and it can be used after being placed for another week.

Embodiment 3

[0020] Take 0.9 g of polylactide-glycolide with a molecular weight of 35,000 Daltons, dissolve it with 5 ml of dichloromethane, add 0.1 g of voriconazole powder, stir and dissolve evenly, inject it into a polytetrafluoroethylene mold, control the airflow speed, and make the dichloromethane Volatile. After being completely dried, the polylactide-glycolide drug delivery system containing voriconazole was removed from the polytetrafluoroethylene mold, and kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent to obtain a thickness of 1.5-2 1.5-2 mm thick and 1.5-2 mm thick voriconazole preparations with a 1.5-2 mm pore size die.

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PUM

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Abstract

The invention relates to a long-acting voriconazole intraocular medicine release system which contains voriconazole and is characterized in that the intraocular medicine release system also contains biodegradable medicinal high-molecular auxiliary material; voriconazole and biodegradable medicinal high-molecular auxiliary material are mixed to form homogenized mixture; the weight ratio of biodegradable high-molecular auxiliary material and voriconazole is 0.1:0.9-0.9-0.1; the molecular weight of the biodegradable high-molecular auxiliary material is 5000-1000000Dalton. The biodegradable high-molecular auxiliary material is selected from poly(lactide-co-glycolide) and polylactic acid. The release period of the voriconazole intraocular medicine release system is a week to a year, has less medicine dosage, less times of administration, reduces the adverse reaction caused by the repeated injection of vitreous cavity and greatly improve the compliance of patients; if the vitreous body baseis implanted simultaneously during the excision operation of the central vitreous body, the complications of intraocular hemorrhage and retinal detachment caused by the repeated vitreous body puncture medicine-injection.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for intraocular implantation, in particular to a long-acting voriconazole intraocular drug delivery system using a biodegradable polymer material as a drug carrier. 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. [0003] Fungal endophthalmitis is a blinding eye disease that is difficult to treat clinically. The incidence rate is increasing year by year, and it greatly damages the structure of the eyeball and visual function. The existing treatment options include systemic injection or oral antifungal drugs, local ocular surface eye drops, direct injection at the infected site such as anterior cha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/506A61K47/34A61P27/02A61P31/10
Inventor 董晓光吴祥根谢立信杨丽娜
Owner SHANDONG EYE INST
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