Anti-excititoxic sustained release intracular implants and related methods

A technology of neurotoxicity and internal implants, which is applied in the device of the present invention for treating patients' eyes and, according to the field of the present invention, can solve the problems of heart symptom deterioration, side effects, etc., and achieve the effect of stable treatment and prolonged treatment effect

Inactive Publication Date: 2007-04-18
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Topical beta-blockers such as Timolol  Can cause systemic side effects such as fatigue, confusion, or wheezing, with worsening of cardiac symptoms after rapid discontinuation of beta-blockers
Oral carbonic anhydrase inhibitors such as acetazolamide can also be used, but these agents can have systemic side effects including chronic metabolic acidosis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Preparation and testing of implants containing NMDA receptor antagonist and biodegradable polymer matrix

[0113] A biodegradable implant is prepared by combining memantine and a biodegradable polymer composition in a stainless steel mortar. The composition was mixed by Turbula shaker, setting conditions: 96RPM, 15 minutes. Scrape off the powder mixture from the walls of the mortar and mix for another 15 minutes. The mixed powder mixture is heated to a semi-molten state at a specific temperature for a total of 30 minutes to form a polymer / drug melt.

[0114] The drug strip is prepared by the following process: using a No. 9 polytetrafluoroethylene (PTFE) tube to pellet the polymer / drug melt into a barrel, and extrude the material at a specific core extrusion temperature to form filaments. The filament is then cut into an implant or drug delivery system with a size of approximately 1 mg. The size of the medicine strip is about 2mm (length)×0.72mm (diameter). The weight of th...

Embodiment 2

[0120] Treatment of glaucoma with intraocular implants containing memantine

[0121] A 68-year-old female patient told her doctor that seeing things became difficult. The doctor determined that her intraocular pressure level was elevated and diagnosed her with glaucoma. An implant containing a combination of 400 μg of memantine and 600 μg of PLGA and PLA was placed in the vitreous of the patient's eyes using a trocar. The vision loss was prevented about 5 months after the implantation procedure.

Embodiment 3

[0123] Method for preparing intraocular implants of memantine active agent

[0124] Conduct an experiment to study the effect of molecular weight (MW), lactide-glycolide (LG) ratio, and drug load on poly(D,L-lactide-co-glycolide) polymer implants containing memantine The influence of the release curve. The implants were prepared by melt extrusion on a small pilot scale extruder.

[0125] Memantine is an N-methyl-D-aspartate (NMDA) receptor antagonist and has been shown to have potential efficacy as a neuroprotective agent in many neurodegenerative diseases. Specifically, memantine can also protect the optic nerve and retina in many eye diseases. The use of sustained-release polymer implants to deliver memantine directly into the vitreous can be an effective way to deliver the drug close to the retina (which can be the most effective here), avoiding the complications of more conventional delivery methods.

[0126] This experiment describes our work to prepare poly(lactide-co-glycol...

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Abstract

Biocompatible intraocular implants include an anti-excitotoxic agent and a polymer that is effective to facilitate release of the anti-excitotoxic agent into an eye for an extended period of time. The therapeutic agents like NMDA receptor anragonists like adamantine or memantine may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.

Description

[0001] Cross reference [0002] This application is a partial continuation of application 10 / 837142 filed on April 30, 2004, and the entire content of which is incorporated into the present invention by reference. Background technique [0003] The present invention relates to a device and method for treating the eye of a patient, and more specifically to an intraocular implant that provides extended release of a therapeutic agent to the eye in which the implant is placed, and a method of preparing and using the implant, such as treating or alleviating one One or more symptoms of glaucoma, such as proliferative vitreoretinopathy and cell damage or death. [0004] Glaucoma affects approximately 5% of people over 65 years of age and 14% of people over 80 years of age. The vision loss caused by glaucoma has been attributed to the progressive damage of the optic nerve and the loss of retinal ganglion cells mediated by increased intraocular pressur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/13A61K9/00
CPCA61K9/0051A61P27/02A61P27/06A61K9/20A61K9/48A61K31/13
Inventor P·M·休斯L·T·斯帕达H·杉本W·M·布兰达J·N·张
Owner ALLERGAN INC
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