Pharmacokinetics
Conditions
Keywords
Biological Availability, Relative Bioavailability Trial
Brief summary
Rivaroxaban is a substance developed for use in the treatment of blood coagulation disorders.Thrombosis (blood clots) can occur as a result of excessive coagulation activity in the blood vessels. Excessive coagulation activity can occur in children as well, and rivaroxaban is therefore being developed for the treatment of thromboembolic events in children and adolescents. As small children are often unable to swallow tablets, an oral suspension (mixture of a liquid containing finely distributed solids) has been developed which allows dosing according to body weight.The objective of this trial is to compare the bioavailability (proportion of a substance that remains available unchanged in the blood circulation) of a new oral suspension of rivaroxaban with a previously used oral suspension and with a rivaroxaban tablet approved for treatment. In order to evaluate the potential influence of food, the new oral suspension containing 20 mg rivaroxaban will be taken after consuming food. In addition, the pharmacokinetics (concentrations of the drug and breakdown products (metabolites) in blood), safety and tolerability will be assessed.
Interventions
DRUGRivaroxaban (Xarelto, BAY59-7939)
Single dose of 10 mg oral suspension (dry powder) in fasted conditions.
Sponsors
Janssen Research & Development, LLC
Bayer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male subjects * Age: 18 to 55 years (inclusive) at the first screening examination * White * Body Mass Index (BMI): ≥18.0 and ≤29.9 kg/m2 at the screening visit.
Exclusion criteria
* Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal * Known coagulation disorders (e.g. von Willebrand's disease, hemophilia) * Known disorders with increased bleeding risk (e.g. periodontosis, hemorrhoids, acute gastritis, peptic ulcer) * Known sensitivity to common causes of bleeding (e.g. nasal) * Regular use of medicines and use of medication that may have an impact on the study objectives * Clinically relevant findings in the ECG such as a second- or third-degree AV block, prolongation of the QRS complex over 120 msec or of the QTc-interval over 450 msec * Clinically relevant findings in the physical examination * Clinically relevant deviations of the screened laboratory parameters from reference ranges * Participation in another clinical study during the preceding 3 months (Last Treatment from previous study to First Treatment of new study)
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Plasma concentration of rivaroxaban characterized by AUC | Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours), at 48 hr after administration), at 72 hr after administration) | AUC:area under the concentration vs. time curve from zero to infinity after single (first) dose |
| Plasma concentration of rivaroxaban characterized by AUC/D | Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration) | AUC/D: AUC divided by dose |
| Plasma concentration of rivaroxaban characterized by Cmax | Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration) | Cmax: maximum drug concentration in plasma after single dose administration |
| Plasma concentration of rivaroxaban characterized by Cmax/D | Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration) | Cmax/D: Cmax divided by dose |
Countries
Germany
Outcome results
None listed