Opiate antagonist therapy is an important treatment for recently withdrawn narcotic addicts. Buprenorphine is a drug with mixed agonist-antagonist properties which prevents any high from morphine-like drugs, thereby eliminating physiological reinforcement. BIOTEK proposes to improve antagonist therapy by developing a transdermal delivery system for buprenorphine, a very effective drug preferred by subjects to either methadone or naltrexone. Transdermal buprenorphine would avoid the inconvenience of frequent clinical visits, and steady maintenance of the secondary agonist action of buprenorphine should provide more positive reinforcement and improve compliance. Because buprenorphine is susceptible to abuse, BIOTEK proposes to protect the patches against subversion by adding a transdermally inactive form of naloxone, a drug which counteracts the mild euphoria of buprenorphine and precipitates withdrawal from other opiates if taken intravenously. BIOTEK has previously demonstrated high transdermal delivery rates for buprenorphine. In Phase I we will attempt to achieve similar rates for buprenorphine from a formulation which contains transdermally inactive naloxone, with the goal of developing an abuse-resistant 48 hour buprenorphine patch.
