Tacrolimus, rectal, sublingual, pharmacokinetics. Tacrolimus, rectaal, sublinguaal, farmacokinetiek.
Conditions
Interventions
Three single doses of tacrolimus will be administered in randomized order with an interval of at least 1 week:
1. A sublingual dose of 3 mg
2. A rectal dose of 15 mg
3. An oral dose of 7 mg.
Venous blood samples are drawn at prespecified time points.
Sponsors
Dr. MHL Christiaans
Maastricht University Medical Centre
P. Debyelaan 25
6229 HX Maastricht
Eligibility
Inclusion criteria
Inclusion criteria: 1. Legally capacitated; 2. 18-65 years old; 3. Using adequate contraception (female volunteers of childbearing potential); 4. Able to comply with the study protocol and willing to give written informed consent.
Exclusion criteria
Exclusion criteria: 1. Concomitant use of medication, grapefruit juice or St John’s worth; 2. Smoking 10 or more cigarettes per day; 3. Simultaneous participation in another clinical trial; 4. Pregnancy or lactation (female volunteers); 5. Abnormal liver biochemistry (>2x upper normal limit); 6. Renal insufficiency (estimated creatinin clearance according to Cockroft-Gault 160/100 mmHg, measured after at least 10 min rest in semi-recumbent position; 8. Prolonged QT interval, corrected for heart rate using the Bazett’s formula (women>470 ms, men>450 ms); 9. Active infection, as determined by clinical examination.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the blood concentration of tacrolimus – time curve (AUC). | — |
Secondary
| Measure | Time frame |
|---|---|
| Relative bioavailability (F) for rectal and sublingual administration compared to oral administration of tacrolimus, time point after administration at which maximal blood concentration of tacrolimus is reached (tmax) and elimination rate constant (kel) for tacrolimus. | — |
Contacts
Public ContactM.H.L. Christiaans
Outcome results
None listed