Steady-state Pharmacokinetics of BIA 2-093 and Oxcarbazepine in Healthy Volunteers

Overview

To investigate the steady-state pharmacokinetics of once-daily and twice-daily regimens of BIA 2-093 and twice-daily regimen of Oxcarbazepine (Trileptal®) in healthy subjects and to assess the tolerability of such regimens in healthy subjects.

Study Type

  • Study Type: Interventional
  • Study Design
    • Allocation: Randomized
    • Intervention Model: Crossover Assignment
    • Primary Purpose: Treatment
    • Masking: None (Open Label)
  • Study Primary Completion Date: December 2003

Detailed Description

Single centre, open-label, randomised, three-way crossover study in 12 healthy volunteers. The study consisted of three 8-day treatment periods separated by washout periods of 10-15 days. On each of the treatment periods the volunteers received either a daily oral dose of BIA 2-093 900 mg once-daily (od), BIA 2-093 450 mg twice-daily (bid), or Oxcarbazepine (Trileptal®) 450 mg bid.

Interventions

  • Drug: BIA 2-093
  • Drug: Oxcarbazepine

Arms, Groups and Cohorts

  • Experimental: Group A
    • BIA 2-093 900 mg once-daily period followed by BIA 2-093 450 mg twice-daily period followed by oxcarbazepine 450 mg twice-daily period BIA 2-093 450 mg od – BIA 2-093 450 mg bid – OXC 900 mg bid
  • Experimental: Group B
    • BIA 2-093 450 mg twice-daily period followed by oxcarbazepine 450 mg twice-daily period followed by BIA 2-093 900 mg once-daily period BIA 2-093 450 mg bid – OXC 450 mg bid – BIA 2-093 900 mg od
  • Experimental: Group C
    • oxcarbazepine 450 mg twice-daily period followed by BIA 2-093 900 mg once-daily period followed by BIA 2-093 450 mg twice-daily period OXC 450 mg bid – BIA 2-093 900 mg od – BIA 2-093 450 mg bid

Clinical Trial Outcome Measures

Primary Measures

  • Cmax – Maximum Observed Plasma Drug Concentration
    • Time Frame: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 h post-dose
    • Cmax – maximum observed plasma drug concentration for BIA 2-093 metabolites: BIA 2-194 BIA 2-195 Oxcarbazepine

Secondary Measures

  • AUC – Area Under the Plasma Concentration Versus Time Curve
    • Time Frame: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 h post-dose
    • AUC – Area Under the Plasma Concentration Versus Time Curve for BIA 2-093 metabolites: BIA 2-194 BIA 2-195 Oxcarbazepine
  • Number of of Subjects Reporting at Least One Adverse Event
    • Time Frame: 8 weeks
    • Number of of subjects reporting at least one adverse event.

Participating in This Clinical Trial

Inclusion Criteria

  • Subjects were eligible for entry into the study if they fulfilled the following inclusion criteria:

  • Male or female subjects aged between 18 and 45 years, inclusive. – Subjects of body mass index (BMI) between 19 and 28 kg/m2, inclusive. – Subjects who were healthy as determined by pre-study medical history, physical examination, neurological examination, and 12-lead ECG. – Subjects who had clinical laboratory tests clinically acceptable. – Subjects who were negative for HBsAg, anti-HCV Ab and HIV-1 and HIV-2 Ab tests at screening. – Subjects who were negative for alcohol and drugs of abuse at screening and first admission. – Subjects who were non-smokers or who smoked less than 10 cigarettes or equivalent per day. – Subjects who were able and willing to give written informed consent. – If case of female subjects, subjects who were not of childbearing potential by reason of surgery or, if of childbearing potential, who used one of the following methods of contraception: double-barrier, intrauterine device or abstinence. – If case of female subjects, subjects who had a negative pregnancy test at screening and first admission. Exclusion Criteria:

  • Subjects who did not conform to the above inclusion criteria. – Subjects who had a clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders. – Subjects who had a clinically relevant surgical history. – Subjects who had a clinically relevant family history. – Subjects who had a history of relevant atopy. – Subjects who had a history of hypersensitivity to carbamazepine or oxcarbazepine or any other relevant drug hypersensitivity. – Subjects who had a history of alcoholism or drug abuse. – Subjects who consumed more than 14 units of alcohol a week. – Subjects who had a significant infection or known inflammatory process on screening and/or first admission. – Subjects who had acute gastrointestinal symptoms at the time of screening and/or first admission (e.g., nausea, vomiting, diarrhoea, heartburn). – Subjects who had used prescription or over-the-counter medication within two weeks of first admission. – Subjects who had used any investigational drug and/or participated in any clinical trial within four months of their first admission. – Subjects who had previously received BIA 2-093. – Subjects who had donated and/or received any blood or blood products within the previous 4 months prior to screening. – Subjects who were vegetarians, vegans and/or have medical dietary restrictions. – Subjects who could not communicate reliably with the investigator. – Subjects who were unlikely to co-operate with the requirements of the study. – Subjects who were unwilling or unable to give written informed consent. – In case of female subjects, subjects who were pregnant or breast-feeding. – In case of female subjects, subjects who were of childbearing potential and did not use an approved effective contraceptive method or used oral contraceptives.

Gender Eligibility: All

Minimum Age: 18 Years

Maximum Age: 45 Years

Are Healthy Volunteers Accepted: Accepts Healthy Volunteers

Investigator Details

  • Lead Sponsor
    • Bial – Portela C S.A.
  • Provider of Information About this Clinical Study
    • Sponsor
  • Overall Official(s)
    • Manuel Vaz-da-Silva, MD, PhD, Principal Investigator, BIAL – Portela & Cª S.A.

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