title: Dose linearity after oral administration of tacrolimus 1-mg capsules at doses of 3, 7, and 10 mg.
abstract: Tacrolimus is an immunosuppressant drug used for the prophylaxis of organ rejection in patients who receive allogenic liver or kidney transplants. This study investigated the relationship between tacrolimus blood concentration-time profiles after 3-, 7-, and 10-mg single oral doses were given to 18 healthy, drug-free, nonsmoking, institutionalized male volunteers. The protocol used a single-dose, 3-period, 3-treatment, nonmasked, randomized-block, complete crossover design. The 90% CIs of the ratios of dose-adjusted, mean, log-transformed values of maximum blood concentration, area under the tacrolimus blood concentration-time curve (0 to the last measurable concentration; lower limit of quantitation = 0.5 ng/mL), and area under the blood concentration-time curve (0 to 0) fell within the range of 125%, indicating dose proportionality for these parameters under experimental conditions. Power to detect a 20% difference for the 3 doses tested was 82.2%, 66.7%, and 72.8%, respectively.
authors.affiliation: Fujisawa Healthcare, Inc., Deerfield, Illinois 60015-2548, USA.
authors.forename: I
authors.initials: I
authors.lastname: Bekersky
authors.forename: D
authors.initials: D
authors.lastname: Dressler
authors.forename: Q A
authors.initials: QA
authors.lastname: Mekki
mesh_terms: D000328:Adult; D019540:Area Under Curve; D018592:Cross-Over Studies; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics*; D008297:Male; D016559:Tacrolimus / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics*
chemical_list: D007166:Immunosuppressive Agents; D016559:Tacrolimus