Active metabolite from Tamiflu ® solution is bioequivalent to that from capsule delivery in healthy volunteers: A cross-over, randomised, open-label study

• Published in: Vaccine 2006-11, Vol.24 (44), p.6660-6663
• Main Authors: Brewster, M., Smith, J.R., Dutkowski, R., Robson, R.
• Format: Article
• Language: English
• Subjects: Active pharmaceutical ingredient (API); Administration, Oral; Adult; Antiviral Agents - administration & dosage; Antiviral Agents - pharmacokinetics; Antiviral Agents - therapeutic use; Applied microbiology; Area Under Curve; Bioavailability; Biological and medical sciences; Capsules; Chemistry, Pharmaceutical; Confidence intervals; Cross-Over Studies; Female; Fundamental and applied biological sciences. Psychology; Humans; Influenza; Influenza, Human - prevention & control; Male; Metabolites; Microbiology; Oseltamivir; Oseltamivir - administration & dosage; Oseltamivir - pharmacokinetics; Pandemics; Pharmacokinetic; Regulatory approval; Therapeutic Equivalency; Vaccines; Vaccines, antisera, therapeutical immunoglobulins and monoclonal antibodies (general aspects); Viruses
• ISSN: 0264-410X; 1873-2518
• DOI: 10.1016/j.vaccine.2006.05.080

The bioavailability of oseltamivir phosphate and oseltamivir carboxylate were assessed in healthy volunteers when delivered as a solution of the active pharmaceutical ingredient (API) compared with the commercial capsule formulation. The 90% confidence intervals (CIs) for the ratios of the two treatments (capsule versus solution) were within the reference region [0.80–1.25] for area under the curve (AUC 0–infinity: [0.94–0.99]) and maximum observed plasma concentrations ( C max: [0.93–1.08]). Thus, the two formulations were bioequivalent for oseltamivir carboxylate. For pandemic stockpiling of Tamiflu ®, governments can therefore choose between the capsule formulation alone, the API alone, or quantities of both.