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CompletedNCT02078180Updated Oct 6, 2017Results posted

Pharmacokinetic Study of Bupropion Hydrochloride Products With Different Release Patterns

A Phase 4 interventional study of generic bupropion in Depression, sponsored by University of Michigan. Completed at 1 site in United States. Open to participants aged 25 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2017-10-06.

Sponsored by University of Michigan · Phase 4, Interventional, and Basic science

Phase
Phase 4
Study type
Interventional
Enrollment
34
Allocation
Randomized
Ages
25 Years to 55 Years
Sex
All
01

Study summary

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

02

Conditions studied

  • Depression

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03

In context

Depression

8,057 studies on the registry are indexed under Depression; 1,641 are open to participants now.

This study's enrollment of 34 is below the median of 84 across 6,720 interventional studies indexed under Depression.

Browse Depression studies →

Lead sponsor

University of Michigan is the lead sponsor of 1,475 studies on the registry; 196 are open to participants now.

Of its 162 completed or terminated interventional studies of FDA-regulated products, 128 (79%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
25 Years to 55 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

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

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
05

Study design

Phase
Phase 4
Primary purpose
Basic science
Allocation
Randomized
Intervention model
Crossover assignment
Masking
Single (Outcomes assessor)
Enrollment
34 participants (actual)

Study arms

  • Active comparator
    generic bupropion IR75

    One oral dose of generic bupropion IR75

    Drug: generic bupropion

  • Active comparator
    generic bupropion IR100

    One oral dose of generic bupropion IR100

    Drug: generic bupropion

  • Active comparator
    generic bupropion SR100

    One oral dose of generic bupropion SR100

    Drug: generic bupropion

  • Active comparator
    generic bupropion SR150

    One oral dose of generic bupropion SR150

    Drug: generic bupropion

  • Active comparator
    generic bupropion XL150

    One oral dose of generic bupropion XL150

    Drug: generic bupropion

  • Active comparator
    generic bupropion XL300

    One oral dose of generic bupropion XL300

    Drug: generic bupropion

Interventions

  • Druggeneric bupropion

    We are comparing different formulations of bupropion that release this drug at different rates. The abbreviation IR75 means immediate release and the number is the dose in mg. The other abbreviations represent SR for sustained-release and XL for extended release, which release the drug slower than the IR formulation.

    Also known as: Wellbutrin

06

What researchers measure

Primary outcomes

  1. Comparision of the Buproprion Area Under the Concentration Time Curve (AUC) From Time 0 to 96 Hours by Type of Formulation and Dosage

    Each formulation of buproprion has a different rate of release. Some release the drug immediately while others release the drug slowly. We will compare the exposure of buproprion by formulation and dose by looking at the area under the concentration time curve. The area under the concentration time curve is a mathematical way of looking at drug exposure in the body. The reported values are AUC (0-96 hours).

    Time frame: 4 days

Secondary outcomes

  1. Comparision of the Buproprion Maximum Concentration (Cmax) by Type of Formulation and Dosage

    Each formulation of buproprion has a different rate of release. Some release the drug immediately while others release the drug slowly. We will compare the exposure of buproprion by formulation and dose by looking at the maximum concentration. The maximum concentration depends on the rate of drug release and so looking at this value can help us compare differences between formulation.

    Time frame: 4 days

07

Results

Posted Oct 6, 2017
Limitations and caveats
The small study sample size may have masked the contribution of pharmacogenetics to bupropion metabolism.

Participant flow

Participant flow — Overall Study
MilestoneIR75, IR200, SR100, SR150, XL150, XL300
Started34
Ir7530
Ir10031
Sr10031
Sr15032
Xl 15031
Xl 30032
Completed29
Not completed5

Outcome measures

PrimaryComparision of the Buproprion Area Under the Concentration Time Curve (AUC) From Time 0 to 96 Hours by Type of Formulation and Dosage

Each formulation of buproprion has a different rate of release. Some release the drug immediately while others release the drug slowly. We will compare the exposure of buproprion by formulation and dose by looking at the area under the concentration time curve. The area under the concentration time curve is a mathematical way of looking at drug exposure in the body. The reported values are AUC (0-96 hours).

Time frame:
4 days
Reported as:
Mean · h*nanogram/milliliter
Comparision of the Buproprion Area Under the Concentration Time Curve (AUC) From Time 0 to 96 Hours by Type of Formulation and Dosage
h*nanogram/milliliterGeneric Bupropion IR75Generic Bupropion IR100Generic Bupropion SR100Generic Bupropion SR150Generic Bupropion XL150Generic Bupropion XL300
Comparision of the Buproprion Area Under the Concentration Time Curve (AUC) From Time 0 to 96 Hours by Type of Formulation and Dosage469 ± 177667 ± 418706 ± 3041002 ± 516740 ± 4491356 ± 637
SecondaryComparision of the Buproprion Maximum Concentration (Cmax) by Type of Formulation and Dosage

Each formulation of buproprion has a different rate of release. Some release the drug immediately while others release the drug slowly. We will compare the exposure of buproprion by formulation and dose by looking at the maximum concentration. The maximum concentration depends on the rate of drug release and so looking at this value can help us compare differences between formulation.

Time frame:
4 days
Reported as:
Mean · nanogram/milliliter
Comparision of the Buproprion Maximum Concentration (Cmax) by Type of Formulation and Dosage
nanogram/milliliterGeneric Bupropion IR75Generic Bupropion IR100Generic Bupropion SR100Generic Bupropion SR150Generic Bupropion XL150Generic Bupropion XL300
Comparision of the Buproprion Maximum Concentration (Cmax) by Type of Formulation and Dosage93 ± 36136 ± 7061 ± 2978 ± 4061 ± 34111 ± 44

Adverse events

Collected over Varied per person from 3 months to 10 months based on their randomization sequence and the time that it took to complete all phases of the study with washout between each formulation.. Non-serious events are listed at a 0% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
IR 75, IR 100, SR 100, SR 150, XL 150 and XL 3000/34 (0%)0/34 (0%)10/34 (29.4%)
Most frequent other events
Most frequent other events
EventIR 75, IR 100, SR 100, SR 150, XL 150 and XL 300
HeadacheNervous system disorders5/34
NauseaGastrointestinal disorders2/34
Peripheral vision lossEye disorders1/34
DizzynessNervous system disorders1/34
RashSkin and subcutaneous tissue disorders1/34

Baseline characteristics

Age, Customized
Age, Customized(Participants)IR 75, IR 100, SR 100, SR 150, XL 150 and XL 300
<25 years0
25-65 years34
>65 years0
Sex: Female, Male
Sex: Female, Male(Participants)IR 75, IR 100, SR 100, SR 150, XL 150 and XL 300
Female18
Male16
Race (NIH/OMB)
Race (NIH/OMB)(Participants)IR 75, IR 100, SR 100, SR 150, XL 150 and XL 300
American Indian or Alaska Native0
Asian2
Native Hawaiian or Other Pacific Islander0
Black or African American6
White24
More than one race0
Unknown or Not Reported2
Region of Enrollment
Region of Enrollment(Participants)IR 75, IR 100, SR 100, SR 150, XL 150 and XL 300
United States34
08

Study locations

1 site
  • University of Michigan
    Ann Arbor, Michigan 48109-2700, United States
09

References and documents

Individual participant data

Plan to share: No

No publications or documents are linked to this record.

10

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Oct 6, 2017, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT02078180
Lead sponsor
University of Michigan
Responsible party
Duxin Sun (Professor of Pharmaceutical Sciences, University of Michigan) — Principal investigator
First posted
Mar 5, 2014
Start date
Apr 2014
Primary completion
Nov 2016
Completion
Nov 2016
Results posted
Oct 6, 2017
Last update
Oct 6, 2017

Study contacts

Duxin Sun, PhD
principal investigator · University of Michigan

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

Not currently enrolling

This study is completed, as verified in Sep 2017. You cannot join it, but the record below documents what was studied.

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