SBIR-STTR Award

Opiate antagonist therapy is an important treatment for recently withdrawn narcotic addicts. Buprenorphine is a drug with mixed agonist-antagonist properties, which eliminates physiological reinforcement by preventing any subjective reward from morphine-like drugs. Buprenorphine is very effective and is preferred by subjects to either methadone or naltrexone. BIOTEK proposes to improve buprenorphine therapy by developing a 3-day transdermal delivery system. A buprenorphine patch would avoid the inconvenience of frequent clinical visits, and steady maintenance of the agonist action of buprenorphine should motivate compliance by providing more positive reinforcement. BIOTEK has previously demonstrated high transdermal delivery rates for buprenorphine. Recent results from a study of human subjects using BIOTEK's injectable buprenorphine microcapsules suggest that effective opiate blockade can be maintained by a much lower buprenorphine dose rate than previously thought necessary. It is the purpose of the proposed program to develop an effective antagonist patch containing too little buprenorphine to be an attractive target for subversion or abuse.

Thesaurus Terms:
buprenorphine, drug administration rate /duration, drug design /synthesis /production, narcotic antagonist, opiate alkaloid, transdermal drug delivery pharmacokinetics, reinforcer, skin irritation /irritant human tissue, laboratory rabbit

Opiate antagonist therapy is an important treatment for recently withdrawn opiate addicts. Buprenorphine is a mixed agonist-antagonist which eliminates physiological reinforcement by blocking subjective opiate reward. Recently marketed as sublingual tablets, buprenorphine is very effective and is preferred by subjects to methadone or naltrexone. BIOTEK proposes to improve buprenorphine therapy by developing a 3-day transdermal delivery system. Such a patch would provide steady maintenance of agonist therapy to foster compliance. If such a patch can be made to contain relatively little buprenorphine, the motivation for subversion and abuse will be minimal. In vitro results on human skin obtained during Phase I strongly support the feasibility of such a patch, and rabbit irritation studies suggest that it will be non-irritating. Phase II will establish patch specifications suitable for GMP manufacture, confirm the in vitro performance of the selected formulation, prepare and characterize GMP clinical samples, initiate stability studies, submit an IND, and conduct an initial human study of safety and pharmacokinetics.

Thesaurus Terms:
buprenorphine, drug abuse, drug abuse chemotherapy, drug administration rate /duration, drug design /synthesis /production, human therapy evaluation, narcotic antagonist, psychopharmacology, transdermal drug delivery chemical stability, clinical trial phase I, drug adverse effect, pharmacology, skin irritation /irritant clinical research, human subject, human tissue, laboratory rabbit, patient oriented research, residential care facility