Comparative bioavailability of three different preparations of rifampicin.
OBJECTIVE
To study the relative bioavailabilities of two generic rifampicin preparations with Rimactane.


METHODS
Each of nineteen healthy volunteers received a single oral dose of 600 mg of rifampicin in an open cross-over randomised three-way single-dose design with a washout period of 7 days between each doses. Plasma concentrations of rifampicin were determined by HPLC. In vitro dissolution profiles of the same drugs were determined and compared with human bioavailability study results.


RESULTS
No statistically significant difference was found in main bioavailability parameters between Rimactane and generic preparations studied. Both generic preparations also fulfilled the bioequivalence criteria based on the 90% confidence intervals. There was a good correlation between in vivo and in vitro results: faster dissolution time corresponded to the lower Tmax value; lower percentage of released compound to the lower AUC value. Significant intersubject variations were found in main bioavailability parameters; significant negative correlation was found between average AUC values and body weight of the volunteer.


CONCLUSIONS
All three products were bioequivalent. Our results also suggest the suitability of one-compartmental model with lag time, first order input and first order output to describe the kinetics of rifampicin.
Pähkla
R
R
Department of Pharmacology, University of Tartu, Estonia. rein@sam.ee
Lambert
J
J
Ansko
P
P
Winstanley
P
P
Davies
P D
PD
Kiivet
R A
RA
D000284:Administration, Oral; D000328:Adult; D000904:Antibiotics, Antitubercular / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D012293:Rifampin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013810:Therapeutic Equivalency
D000904:Antibiotics, Antitubercular; D012293:Rifampin