steady-state pharmacokinetics of bia 2-093 and oxcarbazepine in healthy volunteers

Conditions: Epilepsy

Summary: 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.

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.

Eligibility criteria:
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.

Keywords: epilepsy oxcarbazepine eslicarbazepine acetate bia 2-093