Assessment of the Pharmacokinetics of a Sustained Release Formulation of a Tramadol/Acetaminophen Combination

Phase 1

Completed

• Conditions: Pain
• Interventions: Drug: Tramadol HCI/Acetaminophen

• Registration Number: NCT01880125
• Lead Sponsor: Yungjin Pharm. Co., Ltd.

Brief Summary

1. Objective: To evaluate the pharmacokinetic profiles of an SR 75 mg tramadol/650 mg acetaminophen formulation compared with an immediate release (IR) 37.5 mg tramadol/325 mg acetaminophen formulation after a single dose and at steady state

2. Subjects: Healthy subject

3. Methods: A phase I study to evaluate the pharmacokinetic sustained release and immediate release treatment profiles at steady state.

Detailed Description

This study was open, randomized, 2-period, 2-treatment multiple-dose crossover study of immediate release treatment and sustained release treatment was designed to assess the pharmacokinetics after a 2-day repeated administration in which the steady state was achieved.

Study Timeline

• Study Start: 2012-01
• Primary Completion: 2012-05
• Study Completion: 2012-05
• Study First Submitted: 2013-06-13
• Study First Submitted QC: 2013-06-17
• Study First Posted: 2013-06-18
• Status Verified: 2021-04
• Last Update Submitted: 2021-04-29
• Last Update Posted: 2021-05-05

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 24

Inclusion Criteria

• Subjects between the ages of 20 and 45 years
• Subjects weighed ≥ 45 kg and were within 20% of their ideal body weight
• No clinically relevant abnormalities identified by vital sign measurement, 12-lead electrocardiography and routine laboratory test

Exclusion Criteria

• Hypersensitivity or histories of sensitivity to either tramadol or acetaminophen
• Evidence or histories of clinically significant renal, digestive, respiratory, musculoskeletal, endocrine, psychiatric, neurological, hematological or cardiovascular diseases
• Taking any prescription or herbal medicines within 2 weeks before the study or any over-the-counter medication within 1 week before the study
• Systolic blood pressure (SBP) ≥ 160 mmHg or ≤ 100 mmHg or diastolic blood pressure (DBP) ≥ 95 mmHg or ≤ 60 mmHg
• Any surgical or medical conditions that could affect drug absorption

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Group B	Tramadol HCI/Acetaminophen	Period 1: Tramadol HCI/Acetaminophen 75/650mg PO once once with water 240ml at fasted state Period 2: Tramadol HCI/Acetaminophen 37.5/325mg PO once with water 240ml at fasted state
Group A	Tramadol HCI/Acetaminophen	Period 1: Tramadol HCI/Acetaminophen 37.5/325mg PO once with water 240ml at fasted state Period 2: Tramadol HCI/Acetaminophen 75/650mg PO once once with water 240ml at fasted state

Primary Outcome Measures

Name	Time	Method
Evaluate the pharmacokinetic profiles of tramadol and acetaminophen at steady state	0 to 36 hour	Bio-equivalence of AUC at steady state of tramadol and acetaminophen

Secondary Outcome Measures

Name	Time	Method
Evaluate the pharmacokinetics profiles of tramadol, acetaminophen and O-desmethyltramadol at steady state	0 to 36 hour	Half-life of O-desmethyltramadol at steady state