Comparative bioavailability of two oral formulations of levofloxacin in healthy Mexican volunteers.
OBJECTIVE
To assess the bioequivalence of two levofloxacin 500 mg tablets marketed in Mexico.


METHODS
The clinical investigation was designed as a randomized, open-labeled, two-part, two-treatment, two-period crossover study, in 27 healthy male volunteers. 1 tablet of each formulation was administered with 200 ml of water after 10 h overnight fast. After dosing, serial blood samples were collected for a period of 24 h. Plasma concentrations were determined by a validated high-performance liquid chromatographic method and pharmacokinetic parameters were obtained by non-compartmental approach. Analysis of variance (ANOVA) was carried out using log-transformed AUClast, AUC yen and Cmax and untransformed tmax, and 90% confidence intervals for AUClast, AUC yen and Cmax were calculated. If the 90% confidence intervals (CI) for AUClast, AUC yen and Cmax fell fully within the interval 80 - 125%, the bioequivalence of the two formulations was established.


RESULTS
The means (test and reference) for AUClast were 58.869 and 56.297 microg x h/ml, for AUC yen were 63.456 and 60.748 microg x h/ml and for Cmax were 8.691 and 8.445 microg/ml. The geometric mean ratios of the test formulation to reference formulation for AUClast, AUC yen and Cmax (CI) were 104.53% (102.73 - 106.36%), 104.37% (102.04 - 106.75%) and 103.45% (95.57 - 111.97%), respectively. All 90% CI for AUClast, AUC yen and Cmax fell within the Mexican Federal Commission for Prevention of Sanitary Risks (COFEPRIS) accepted bioequivalence range of 80 - 125%.


CONCLUSIONS
Based on the results, the formulations tested are bioequivalent.
Pharmacological Research Unit, National Institute for Respiratory Diseases Ismael Cosío Villegas, Mexico.
M
F J
FJ
Flores-Murrieta
D000284:Administration, Oral; D000704:Analysis of Variance; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D006801:Humans; D064704:Levofloxacin; D008297:Male; D008800:Mexico; D015242:Ofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013607:Tablets; D013810:Therapeutic Equivalency; D055815:Young Adult
D000900:Anti-Bacterial Agents; D013607:Tablets; D064704:Levofloxacin; D015242:Ofloxacin