Clonidine and GABA compounds in a biodegradable polymer carrier

Patent metadata

Field	Value
Publication number	US-9968572-B2
Application number	US-201615087363-A
Country	US
Kind code	B2
Filing date	Mar 31, 2016
Priority date	Dec 3, 2010
Publication date	May 15, 2018
Grant date	May 15, 2018

Abstract

Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a gamma-aminobutyric acid compound at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

First claim

What is claimed is:

1. A method for treating acute pain, wherein said method comprises implanting a drug depot in an organism to reduce, prevent or treat pain, wherein said drug depot comprises clonidine and at least one gamma-aminobutyric acid (GABA) compound comprising gabapentin in an amount from about 0.1 wt. % to about 30 wt. % of the drug depot and baclofen, vigabatrin, pregabalin, gamma-amino-phosphinic acid or 1-{[(alpha isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, and at least one biodegradable polymer, wherein the drug depot is configured to have a burst release of about 5% to about 25% of the clonidine within 24 hours, and the weight ratio of gabapentin to clonidine is 100:1.

2. A method according to claim 1 , wherein said clonidine comprises from about 5 wt. % to about 15 wt. % of the drug depot.

3. A method according to claim 1 , wherein said biodegradable polymer comprises at least 70 wt. % of the drug depot.

4. A method according to claim 1 , wherein said biodegradable polymer comprises at least 90 wt. % of the drug depot.

5. A method according to claim 1 , wherein (i) the at least one biodegradable polymer comprises polylactide (PLA) or (ii) the at least one biodegradable polymer comprises one or more of poly(lactide-co-glycolide) (PLGA), polylactide (PLA), polyglycolide (PGA), D-lactide, polyorthoester (POE), D,L-lactide, L-lactide, D,L-lactide-co-caprolactone, L-lactide-co-ε-caprolactone, D,L-lactide-co-glycolide-co-caprolactone or a combination thereof.

6. A method according to claim 5 , wherein the at least one biodegradable polymer comprises poly(lactic-co-glycolide) and said poly(lactic-co-glycolide) comprises a mixture of polyglycolide and polylactide.

7. A method according to claim 6 , wherein said mixture comprises more polylactide than polyglycolide.

8. A method according to claim 1 , wherein said clonidine is in the form of clonidine hydrochloride or a mixture of clonidine and a hydrochloride salt or an insoluble fatty acid salt.

9. A method according to claim 1 , wherein said implanting comprises applying said pharmaceutical composition at a plurality of sites that triangulate a pain generator.

Assignees

• Warsaw Orthopedic Inc

Inventors

• Wilsey Jared T
• Clay Danielle L
• Marx Jeffrey C
• Mckay William F
• Roy Josee
• Zanella John Myers

Classifications

• A61K31/195 Primary

  having an amino group · CPC title

• A61K47/34

  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 title

• A61K31/662

  Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K9/0024

  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 title