Oil-in-oil emulsified polymeric implants containing a hypotensive lipid and related methods

• US 7,993,634 B2
• Filed: 12/15/2005
• Issued: 08/09/2011
• Est. Priority Date: 04/30/2004
• Status: Active Grant

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Sarrazin, Christian, Do, Marina, Hughes, Patrick M., Boix, Michele
• Primary Examiner(s): Azpuru; Carlos A
• Application Number:
  US11/303,462
• Publication Number:
  US 20070224246A1
• Time in Patent Office: 2,063 Days
• Field of Search: None
• US Class Current: 424/78.04
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/216 of acids having aromatic rings, e.g. benactizyne, clofibrate
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• 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 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• 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 9/5031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/5089 Processes
• CPC Class Codes: A61L 2/081 Gamma radiation
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: B01J 13/02 Making microcapsules or microballoons for medical preparations A61K9/50
• CPC Class Codes: B01J 13/04 by physical processes, e.g. drying, spraying
• CPC Class Codes: B01J 13/06 by phase separation

Abstract

Biocompatible intraocular implants, such as microparticles, include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the prostamide component may be encapsulated by the polymeric component. The present implants include oil-in-oil emulsified implants or microparticles. Methods of producing the present implants are also described. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma.

Claims

1. A method of treating an ocular condition in an eye of a patient, comprising the step of placing a population of microparticles comprising a polymeric component encapsulating a prostamide component in the form of oil-in-oil emulsified microparticles in an eye of a patient.

2. The method of claim 1 which is effective to treat glaucoma.

3. The method of claim 1 which is effective to decrease intraocular pressure.

4. The population of claim 1, wherein the polymeric component comprises a poly (lactide-co-glycolide) copolymer, and the prostamide component comprises at least one prostamide derivative selected from the group consisting of bimatoprost, salts thereof, and mixtures thereof.

5. The population of claim 1 which is terminally sterilized.

6. The population of claim 5, wherein at least 80% of the prostamide component remains stable after the sterilization.

7. The population of claim 1 having a mean particle diameter from about 30 μ

m to about 50 μ

m.

8. The population of claim 1, wherein the maximum particle diameter is less than about 200 μ

m.

9. The population of claim 1, wherein the microparticles have a release rate of the prostamide component of about 0.7% per day in vitro.

10. The population of claim 1, wherein the prostamide component comprises about 10% wt/wt of the microparticles.

11. The population of claim 1, wherein the prostamide component comprises about 5% wt/wt of the microparticles.