Formulation for controlled release of drugs by combining hydrophilic and hydrophobic agents

• US 5,869,079 A
• Filed: 06/02/1995
• Issued: 02/09/1999
• Est. Priority Date: 06/02/1995
• Status: Expired due to Term

• Current Assignee: Allergan Incorporated (Abbvie Incorporated)
• Original Assignee: Oculex Pharmaceuticals, Inc. (Abbvie Incorporated)
• Inventors: Wong, Vernon, Kochinke, Frank
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US08/459,134
• Time in Patent Office: 1,348 Days
• Field of Search: 424/422, 424/423, 424/426, 424/486, 424/488, 514/953
• US Class Current: 424/426
• CPC Class Codes: A61F 2210/0004 bioabsorbable
• CPC Class Codes: A61F 9/0017 implantable in, or in contact with, the eye, e.g. ocular inserts
• 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 9/0024 Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/204 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• 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 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

Combinations of hydrophilic and hydrophobic entities in a biodegradable sustained release implant are shown to modulate each other'"'"'s rate of release. Formulations of a therapeutically active agent and modulator provide controlled, sustained drug release for an extended period of time.

Claims

1. An semi-rigid implant for sustained release comprising:

a polyester of lactic acid and glycolic acid in from 10 to 50 weight percent of said implant;

hydroxylpropylmethylcellulose in from 10 to 50 weight percent of said implant; and

dexamethasone, wherein said dexamethasone is released within a therapeutic dosage which does not vary by more than about 100% for a period of at least about 3 days.