Food Effect in Healthy Volunteers, Healthy Volunteers, Pharmacokinetics
Conditions
Keywords
Pelubiprofen, DW-1021, Tramadol, Food effect
Brief summary
This is a Phase 1, open-label, single-dose crossover study designed to evaluate the effect of food on the pharmacokinetics of DW-1021, a fixed-dose combination tablet containing pelubiprofen 45 mg and tramadol 45.9 mg. Fourteen healthy adult Vietnamese males will each receive DW-1021 once under fasting conditions and once under fed conditions, with a 14-day washout period in between. Blood samples will be collected to assess how food intake affects the absorption and exposure levels of both active ingredients. Safety, including adverse events, laboratory results, vital signs, and ECGs, will be closely monitored throughout the study.
Detailed description
DW-1021 is a fixed-dose combination tablet containing pelubiprofen, a nonsteroidal anti-inflammatory drug (NSAID), and tramadol, a centrally acting analgesic. Combining these two agents is expected to provide multimodal pain relief by targeting both peripheral and central pain pathways while potentially reducing opioid-related side effects. This Phase 1 study is being conducted to evaluate how a standard high-fat meal affects the rate and extent of absorption of pelubiprofen and tramadol when administered together in DW-1021. A randomized, open-label, two-period, two-sequence crossover design is used to allow each subject to serve as his own control, improving the reliability of the pharmacokinetic comparison between fasting and fed states. Each of the 14 healthy adult male volunteers will receive a single dose of DW-1021 under fasting conditions in one period and under fed conditions in the other, with a sufficient washout period to prevent carryover effects. Intensive blood sampling will be performed after each dose to measure plasma concentrations of pelubiprofen, its active metabolite (trans-OH-pelubiprofen), tramadol, and O-desmethyl-tramadol. Safety will be monitored throughout, including recording of adverse events, laboratory tests, vital signs, and ECGs. The data generated will help determine whether food intake has a clinically significant impact on the pharmacokinetic profile of DW-1021 and will support future dosing recommendations and product labeling.
Interventions
DRUGDW-1021
A fixed-dose combination controlled release film-coated tablet containing pelubiprofen 45 mg and tramadol 45.9 mg (salt form), administered as a single oral dose under fasting and fed conditions in a two-period, two-sequence crossover design. Each subject receives the intervention once under each condition with a 14-day washout period.
Sponsors
Daewon Pharmaceutical Co., Ltd.
Big Leap Research
Haiphong University of Medicine and Pharmacy
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Intervention model description
A randomized, open-label, two-period, two-sequence crossover design. Each subject will receive DW-1021 once under fasting conditions and once under fed conditions, with a 14-day washout period between periods.
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy male subjects aged 20 to 40 years at screening visit 2. Body Mass Index (BMI) between 18.5 and 24.9 kg/m² 3. Body weight greater than 50 kg 4. Systolic blood pressure between 100 mmHg and 129 mmHg; diastolic blood pressure less than 84 mmHg 5. Regular heart rate ranging from 60 to 90 beats per minute 6. No clinically significant medical history or evidence of congenital or chronic diseases, including but not limited to: hypertension, orthostatic hypotension, hypoglycemia when fasting, swallowing difficulties, diabetes, cardiovascular diseases, pulmonary diseases, gastrointestinal diseases, liver insufficiency, renal insufficiency, endocrine disorders, neurological or psychiatric disorders, immunological, hematological, or hereditary diseases, tuberculosis, or infectious diseases 7. Suitable laboratory test results (hematology, urinalysis, blood chemistry, HCV/AIDS, HBsAg, anti-HCV) and electrocardiogram (ECG) at screening: no pathological findings; clinical laboratory parameters within the normal range or, if outside the normal range, not clinically significant as judged by the investigator 8. Willing and able to provide written informed consent after being fully informed about the study objectives and possible adverse effects 9. Agree to use effective contraception from initial administration until 7 days after the last dose of test or reference drugs
Exclusion criteria
1. Use of drugs that induce or inhibit drug-metabolizing enzymes (e.g., barbiturates) within 30 days prior to administration, or use of any medication that might affect the study within 10 days prior to administration 2. Participation in any other clinical trial within 3 months prior to screening 3. Blood donation within 8 weeks prior to drug administration 4. History of gastrointestinal surgery that may affect drug absorption 5. History of drug abuse, or use of alcohol, drugs, or tobacco products within 1 year before participation 6. Known hypersensitivity or allergy to the test or reference drug or their components 7. Known genetic disorders such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption, which are characterized by symptoms like diarrhea and bloating after consuming dairy products 8. Suffering from dysphagia
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Plasma Concentration (Cmax) | Up to 48 hours post-dose in each period | Cmax of pelubiprofen, tramadol will be assessed following a single oral administration of DW-1021 under fasting and fed conditions to evaluate the effect of food on systemic exposure. |
| Area Under the Concentration-Time Curve (AUC₀-t) | Up to 48 hours post-dose in each period | AUC₀-t of pelubiprofen,tramadol will be assessed following a single oral administration of DW-1021 under fasting and fed conditions to evaluate the effect of food on systemic exposure. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Tmax of trans-OH-pelubiprofen and O-desmethyl-tramadol | Up to 48 hours post-dose in each period | Time to reach maximum plasma concentration (Tmax) of trans-OH-pelubiprofen and O-desmethyl-tramadol following single oral administration of DW-1021 under fasting or fed condition. |
| Cmax of trans-OH-pelubiprofen and O-desmethyl-tramadol | Up to 48 hours post-dose in each period | Maximum observed plasma concentration (Cmax) of trans-OH-pelubiprofen and O-desmethyl-tramadol following single oral administration of DW-1021 under fasting or fed condition |
| CL/F of trans-OH-pelubiprofen and O-desmethyl-tramadol | Up to 48 hours post-dose in each period | Apparent oral clearance (CL/F) of trans-OH-pelubiprofen and O-desmethyl-tramadol following single oral administration of DW-1021 under fasting or fed condition |
| t½ of trans-OH-pelubiprofen and O-desmethyl-tramadol | Up to 48 hours post-dose in each period | Terminal elimination half-life (t½) of trans-OH-pelubiprofen and O-desmethyl-tramadol following single oral administration of DW-1021 under fasting or fed condition. |
| AUC₀-t of trans-OH-pelubiprofen and O-desmethyl-tramadol | Up to 48 hours post-dose in each period | Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC₀-t) for trans-OH-pelubiprofen and O-desmethyl-tramadol following single oral administration of DW-1021 under fasting or fed condition |
Countries
Vietnam
Contacts
Primary ContactPhuong Nguyen Thi Thu Phuong, MD, PhD
Outcome results
None listed