Epilepsy
Conditions
Keywords
BIA 2-093, Eslicarbazepine acetate
Brief summary
The purpose of this study is to investigate the effect of food on the pharmacokinetics of a single 800 mg oral dose of BIA 2-093 in healthy volunteers.
Detailed description
Single centre, open label, randomized, two-way crossover study in 12 healthy male volunteers. The study consisted of 2 periods separated by a washout period of 14 days or more. On each of the study periods the volunteers received a single 800 mg oral dose of BIA 2-093 following either a standard high fat content breakfast or 10 hours of fasting.
Interventions
DRUGBIA 2-093
Sponsors
Bial - Portela C S.A.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
Subjects were eligible for entry into the study if they fulfilled the following inclusion criteria: * Male 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, EEG, and 12-lead ECG. * Subjects who had clinical laboratory tests clinically acceptable to the investigator. * 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 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.
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, 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 relevant drug hypersensitivity. * Subjects who had a history of alcoholism or drug abuse. * Subjects who consumed more than 21 units of alcohol a week. * Subjects who had a significant infection or known inflammatory process on screening and/or admission. * Subjects who had acute gastrointestinal symptoms at the time of screening and/or admission (e.g., nausea, vomiting, diarrhoea, heartburn). * Subjects who had an acute infection such as influenza at the time of screening and/or admission. * Subjects who had used prescription drugs within four weeks of first dosing. * Subjects who had used over-the-counter medication excluding oral routine vitamins but including mega dose vitamin therapy within one week of first dosing. * Subjects who had used any investigational drug and/or participated in any clinical trial within two months of their first admission to this study. * Subjects who had previously received BIA 2-093. * Subjects who had donated and/or received any blood or blood products within the previous two months prior to screening. * Subjects who were vegetarians, vegans and/or had 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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) | pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose | Maximum observed plasma concentration of BIA 2-093 |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Time of Occurrence of Cmax (Tmax) | pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose | Time of occurrence of Cmax of BIA 2-093 |
| Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Sampling Time at Which Concentrations Were at or Above the Limit of Quantification (AUC0-t) | pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose | Area under the plasma concentration versus time curve from time zero to the last sampling time at which concentrations were at or above the limit of quantification (AUC0-t) of BIA 2-093 |
| Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC0-oo) | pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose | Area under the plasma concentration versus time curve from time zero to infinity (AUC0-oo) of BIA 2-093 |
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Fasting Period single 800 mg oral dose of BIA 2-093 following 10 hours of fasting or following either a standard high fat content breakfast. | 12 |
| Total | 12 |
Baseline characteristics
| Characteristic | Fasting Period |
|---|---|
| Age, Categorical <=18 years | 0 Participants |
| Age, Categorical >=65 years | 0 Participants |
| Age, Categorical Between 18 and 65 years | 12 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 12 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 10 / 12 |
| serious Total, serious adverse events | 0 / 12 |
Outcome results
Primary
Maximum Observed Plasma Concentration (Cmax)
Maximum observed plasma concentration of BIA 2-093
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Single Group | Maximum Observed Plasma Concentration (Cmax) | Fed | 12799 ng/mL | Standard Deviation 1769 |
| Single Group | Maximum Observed Plasma Concentration (Cmax) | Fasting | 11302 ng/mL | Standard Deviation 1866 |
Secondary
Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC0-oo)
Area under the plasma concentration versus time curve from time zero to infinity (AUC0-oo) of BIA 2-093
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Single Group | Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC0-oo) | Fasting | 243589 ng.h/mL | Standard Deviation 31052 |
| Single Group | Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC0-oo) | Fed | 242459 ng.h/mL | Standard Deviation 32085 |
Secondary
Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Sampling Time at Which Concentrations Were at or Above the Limit of Quantification (AUC0-t)
Area under the plasma concentration versus time curve from time zero to the last sampling time at which concentrations were at or above the limit of quantification (AUC0-t) of BIA 2-093
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Single Group | Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Sampling Time at Which Concentrations Were at or Above the Limit of Quantification (AUC0-t) | Fasting | 243155 ng.h/mL | Standard Deviation 31213 |
| Single Group | Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Sampling Time at Which Concentrations Were at or Above the Limit of Quantification (AUC0-t) | Fed | 229350 ng.h/mL | Standard Deviation 41366 |
Secondary
Time of Occurrence of Cmax (Tmax)
Time of occurrence of Cmax of BIA 2-093
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18, 24, 36, 48, 72 and 96 hours post-dose
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Single Group | Time of Occurrence of Cmax (Tmax) | Fasting | 3.5 hours |
| Single Group | Time of Occurrence of Cmax (Tmax) | Fed | 4.0 hours |