Biodegradable alpha-2 agonist polymeric implants and therapeutic uses thereof

• US 9,095,506 B2
• Filed: 11/17/2008
• Issued: 08/04/2015
• Est. Priority Date: 11/17/2008
• Status: Active Grant

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Spada, Lon T., Ghebremeskel, Alazar N., Robinson, Michael R.
• Primary Examiner(s): PACKARD, BENJAMIN J
• Application Number:
  US12/272,548
• Publication Number:
  US 20100124565A1
• Time in Patent Office: 2,451 Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/498 Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics

Abstract

Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants can be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, including reduction of an elevated intraocular pressure.

Claims

1. A biodegradable implant adapted for intraocular use, the implant comprising:

(a) about 40 weight % brimonidine free base;

(b) about 10 weight % brimonidine tartrate;

(c) about 20 weight % first ester end-capped poly (D,L-lactide) polymer having an inherent viscosity of about 0.3 dL/g;

(d) about 20 weight % second ester end-capped poly (D,L-lactide) polymer; and

(e) about 10 weight % acid end-capped poly (D,L-lactide) polymer having an inherent viscosity of about 0.2 dL/g; and

wherein the implant exhibits a substantially linear release of brimonidine over a period of time from about 20 days to about 50 days.

2. A method for treating glaucoma comprising the step of intraocular administration of a biodegradable intraocular implant comprising:

(a) about 40 weight % brimonidine free base;

(b) about 10 weight % brimonidine tartrate;

(c) about 20 weight % first ester end-capped poly (D,L-lactide) polymer having an inherent viscosity of about 0.3 dL/g;

(d) about 20 weight % second ester end-capped poly (D,L-lactide) polymer; and

(e) about 10 weight % acid end-capped poly (D,L-lactide) polymer having an inherent viscosity of about 0.2 dL/g; and

wherein the implant exhibits a substantially linear release of brimonidine over a period of time from about 20 days to about 50 days.