Implantable polymeric device for sustained release of buprenorphine

Abstract

The present invention provides compositions, methods, and kits for treatment of opiate addiction and pain. The invention provides a biocompatible nonerodible polymeric device which releases buprenorphine continuously with generally linear release kinetics for extended periods of time. Buprenorphine is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with buprenorphine.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Patent Application Ser. No. 60 / 384,733, filed May 31, 2002, the disclosure of which is incorporated herein by reference in its entirety.STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT [0002] This invention was made in part during work supported by a grant from the National Institute of Mental Health (1R43 MH60037-01). The government has certain rights in the invention.TECHNICAL FIELD [0003] The invention provides a nonbioerodible, polymeric device for subcutaneous implantation and sustained release of buprenorphine for treatment of opiate addiction or pain. BACKGROUND OF THE INVENTION [0004] Buprenorphine, a semi-synthetic opiate classified as a “partial agonist” behaves very much like classical mu agonists such as morphine, exerting an analgesic effect through high affinity binding to mu subclass opiate receptors in the central nervous system. [0005] Buprenorphine ...

AI Technical Summary

Benefits of technology

"The invention provides implantable devices for treating opiate addiction and pain. These devices contain buprenorphine, a drug that is continuously released in vivo over a sustained period of time through pores that open to the surface of a nonerodible polymeric matrix. The buprenorphine is encapsulated within the matrix and is released at a steady state rate that results in a steady state plasma buprenorphine level of at least 0.1 ng / ml. The devices can be implanted subcutaneously and can provide long-term treatment for opiate addiction and pain. The method of treatment involves administering at least one implantable device containing buprenorphine. The invention also provides methods for producing the implantable devices."

Problems solved by technology

For this reason, oral buprenorphine formulations have the potential for misuse (i.e., diversion for recreational, rather than therapeutic, purposes), making them unsuitable for use as a take-home medication.

Compliance with this dosing scheme is often poor.

Further, enteral drug delivery is poorly tolerated or prohibited in patients with particular indications, such as some patients with cancer-related pain in whom continuous drug delivery is a necessity.

However, continuous parenteral delivery of opiate analgesics is expensive, cumbersome, and dependent upon the availability of refrigeration, catheters, pumps, and trained personnel.

Further, concerns over drug diversion for illicit use often limits availability of opiate analgesics.

If an opiate addict attempts to abuse the combination tablet by dissolving it and injecting it intravenously, unpleasant withdrawal symptoms brought on by the naloxone component will result.

However, opiate antagonists such as naloxone may reduce the analgesic effectiveness of buprenorphine to those who are using it therapeutically for pain relief and such antagonists may cause undesirable side effects.

Opiate addiction is a major societal problem throughout the world.

Often, poor compliance with dosing regimens complicates treatment.

Further, the cost of such therapy is significant, a large portion of the cost relating to frequent clinic visits and the monitoring of urine tests to assure compliance with drug dosing, as well as pharmacy charges relating to dispensing of methadone.

Another problem with oral dosage forms such as powders or tablets is that they can be dissolved in water and concentrated to provide a solution which may be injected by the addict in lieu of the drug of abuse.

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