Ocular implant made by a double extrusion process

• US 8,048,445 B2
• Filed: 07/15/2008
• Issued: 11/01/2011
• Est. Priority Date: 01/09/2003
• Status: Expired due to Fees

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Nivaggioli, Thierry, Peng, Lin, Shiah, Jane-Guo, Blanda, Wendy M., Weber, David A., Bhagat, Rahul, Chou, David
• Primary Examiner(s): Foley; Shanon A
• Application Number:
  US12/173,746
• Publication Number:
  US 20080286336A1
• Time in Patent Office: 1,204 Days
• Field of Search: None
• US Class Current: 424/426
• CPC Class Codes: A61F 9/0017 implantable in, or in contact with, the eye, e.g. ocular inserts
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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: A61K 9/1647 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/204 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The invention provides biodegradable implants sized for implantation in an ocular region and methods for treating medical conditions of the eye. The implants are formed from a mixture of hydrophilic end and hydrophobic end PLGA, and deliver active agents into an ocular region without a high burst release.

Claims

1. A method for making an ocular bioerodible implant for treating a condition of the eye, the method comprising performing a plurality of heat extrusions of a biodegradable polymer and at least one corticosteroid thereby forming a filament including a homogeneous distribution of the at least one corticosteroid, wherein the ocular bioerodible implant has a reduced in-batch variability relative to a single extrusion implant.

2. The method of claim 1 further comprising the step of milling the biodegradable polymer prior to a first extrusion.

3. The method of claim 1, wherein the biodegradable polymer comprises poly(lactic-co-glycolic)acid (PLGA) copolymer.

4. The method of claim 3 wherein the ratio of lactic to glycolic acid monomers is about 50/50 weight percentage.

5. The method of claim 3 wherein the PLGA copolymer is about 20 to about 90 weight percent of the bioerodible implant.

6. The method of claim 5 wherein the PLGA copolymer is about 40 percent by weight of the bioerodible implant.

8. A bioerodible implant for treating an ocular condition made by the method of claim 1.

7. A method for making a bioerodible implant for treating an ocular condition, the method comprising the steps of:

(a) milling a biodegradable polymer;

(b) blending the milled biodegradable polymer and particles of an active agent, to thereby obtain a blended mixture of the milled biodegradable polymer and the particles of the active agent, wherein at least about 75% of the particles of the active agent have a diameter of less than about 201 Jm;

(c) carrying out a first heat extrusion of the blended mixture, to thereby obtain a first extrusion product;

(d) pelletizing the first heat extrusion product, and;

(e) carrying out a second heat extrusion of the pelletized first extrusion product, thereby obtaining a bioerodible implant for an ocular condition including a homogeneous distribution of the active agent,

wherein the bioerodible implant has a reduced in-batch variability relative to a single extrusion implant.