This trial is active, not recruiting.

Condition depression
Treatment generic bupropion
Phase phase 4
Sponsor University of Michigan
Start date April 2014
End date November 2016
Trial size 50 participants
Trial identifier NCT02078180, HHSF223201310164C, HUM00081894


The objectives of this project are to determine if the bioavailability and release pattern of bupropion HCl products differ and if the genotype of the metabolic enzymes affects the saturation of intestinal enzymes with different dose strengths within one product line. Findings from this project will help the FDA Center for Drug Evaluation and Research's (CDER) Office of Generic Drugs improve policy development and review practice in the future for similar products, e.g. extended release oral drug products being metabolized in the gut wall and having multiple strengths.

Aim 1: To compare the pharmacokinetics of bupropion and its metabolites in plasma in healthy individuals when they ingest different strengths of bupropion (75-300 mg) with variable release profiles (IR vs XL vs SR) in GI tract.

Working hypothesis: Variation in release rate and mechanism of bupropion formulations in gastrointestinal (GI) tract will impact metabolism and saturation of bupropion in GI tract, which will generate different concentration of bupropion and its metabolites in plasma.

Aim 2: To investigate pharmacogenomics of CYP 2B6 that influences metabolism, saturation, and pharmacokinetics of bupropion

Working hypothesis: The gain of function of CYP2B6 variants (allele *4 and *22) in patients will increase the metabolism of bupropion in the GI tract and liver, reduce both local concentration and plasma concentration of bupropion, and thus cause non-bioequivalence when bupropion is released earlier in GI tract

United States No locations recruiting
Other countries No locations recruiting

Study Design

Allocation randomized
Intervention model crossover assignment
Masking single blind (outcomes assessor)
Primary purpose basic science
(Active Comparator)
One oral dose of generic bupropion IR75
generic bupropion Wellbutrin
(Active Comparator)
One oral dose of generic bupropion IR100
generic bupropion Wellbutrin
(Active Comparator)
One oral dose of generic bupropion SR100
generic bupropion Wellbutrin
(Active Comparator)
One oral dose of generic bupropion SR150
generic bupropion Wellbutrin
(Active Comparator)
One oral dose of generic bupropion XL150
generic bupropion Wellbutrin
(Active Comparator)
One oral dose of generic bupropion XL300
generic bupropion Wellbutrin

Primary Outcomes

PK parameters for bupropion formulations: half-life (t1/2), volume of distribution (Vd/F), oral clearance (CL/F), maximum drug concentration (Cmax), time to reach Cmax (Tmax), area under the concentration vs. time curve (AUC), absorption rate constant
time frame: Pharmacokinetic (PK) data will be collected over time points: 0, 0.5, 1, 2, 3, 4, 6, 8, 12*, 24, 48, 72, and 96 hours post-dose. *XL formulation only.

Eligibility Criteria

Male or female participants from 25 years up to 55 years old.

Inclusion Criteria: - Healthy volunteers 25 to 55 years old. - Volunteers have a Body Mass Index (BMI), calculated from the ratio of height and weight, within a range of 18.5 to 35. - Willing to be medication and supplement free 2 weeks prior to beginning study, and throughout the study. All forms of birth control are okay. Exclusion Criteria: - Individuals unwilling or unable to comply with the study protocol (e.g. unable to remain medication or supplement free during the study). - Individuals unwilling or unable to take bupropion or have an allergy to bupropion - Any medical or surgical conditions which might significantly alter bupropion absorption (e.g., history of malabsorption, liver disease, gastric bypass surgery ) - Individuals with a history of psychiatric or neurological illness, including seizure disorders - Nicotine dependence - Alcohol dependence - Pregnant or nursing women

Additional Information

Official title Pharmacokinetic Study of Bupropion Hydrochloride Products With Different Release Patterns
Principal investigator Duxin Sun, PhD
Trial information was received from ClinicalTrials.gov and was last updated in May 2016.
Information provided to ClinicalTrials.gov by University of Michigan.