Pharmacokinetic evaluation of two different formulations of megestrol acetate in patients with advanced malignancies.
The bioequivalence of two megestrol acetate formulations, 160-mg "tablets" and 160-mg "sachets," was investigated in a single-dose, open-label, balanced-for-sequence cross-over study involving 12 advanced-cancer patients. The observed plasma megestrol-acetate time course obtained with both formulations was consistent with the literature data. The main source of variability in the pharmacokinetic parameters was intersubject variability; drug formulation played only a minor (and nonsignificant) role. The width of the 90% confidence interval of the area-under-the-curve (AUC) ratio (sachets: tablets) computed according to Schuirmann (0.9-1.4) was mainly due to the presence of a single outlier, showing an AUC ratio of 2.7. The trend to higher bioavailability of the new formulation was not significant, especially as compared with the dose-response data reported in the literature.
Camaggi
C M
CM
Dipartimento di Chimica Organica, Università di Bologna, Italy.
Strocchi
E
E
Martoni
A
A
Zamagni
C
C
Cacciari
N
N
Robustelli della Cuna
G
G
Pavesi
L
L
Tedeschi
M
M
Silva
A
A
Pannuti
F
F
D000284:Administration, Oral; D000368:Aged; D001682:Biological Availability; D018592:Cross-Over Studies; D006801:Humans; D008297:Male; D008535:Megestrol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D019290:Megestrol Acetate; D008875:Middle Aged; D009369:Neoplasms / Q000378:metabolism*; D011208:Powders; D013607:Tablets
D011208:Powders; D013607:Tablets; D008535:Megestrol; D019290:Megestrol Acetate