Journal of Antimicrobial Chemotherapy, Vol 39, 87-92, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
R Teng, LC Dogolo, SA Willavize, HL Friedman and J Vincent
Two studies determined the oral bioavailability of trovafloxacin (CP-
99,219) in healthy volunteers under fasted and fed conditions. In a
randomized, two-way crossover study, 12 fasting subjects received two 100
mg tablets of trovafloxacin and an equivalent dose of alatrofloxacin
(CP-116,517), administered by i.v. infusion over 1 h. Alatrofloxacin, the
L-Ala-L-Ala prodrug of trovafloxacin, is rapidly converted in the body to
trovafloxacin. After the oral dose of trovafloxacin, the mean Cmax and AUC
were 2.2 mg/L and 30.4 mg x h/L, respectively. After the infusion of
alatrofloxacin, the Cmax and AUC of trovafloxacin were 3.2 mg/L and 34.7 mg
x h/L, respectively. The mean T(1/2) after both treatments was about 11 h.
The mean Cl and Vd(ss) of trovafloxacin after the infusion of
alatrofloxacin were 1.32 mL/min/kg and 1.13 L/kg, respectively. The mean
oral bioavailability of trovafloxacin was estimated to be 87.6% (range
64.8-122.1%). Another randomized, open, three-way crossover study was
conducted in 12 healthy male volunteers to investigate the effect of food
in the gastrointestinal tract on the bioavailability of trovafloxacin. Each
subject received three 100 mg tablets after fasting overnight (treatment A)
or after a standard breakfast (treatment B), or 300 mg as oral aqueous
suspension after fasting overnight (treatment C). Mean Tmax after treatment
B occurred 2.2 h later (3.6 h vs 1.4 h) than after treatment A. Mean Cmax
and AUC were 2.3 and 2.6 mg/L and 38.2 and 39.5 mg x h/L after B and A,
respectively. About 5% of the administered dose was recovered unchanged in
the 24 h urine sample after all three treatments. Thus, the food reduced
mean Cmax by 12% but had no appreciable effect on mean AUC. The mean
bioavailability of trovafloxacin administered as treatment regimen B was
96.6% relative to that of treatment A. The respective mean
bioavailabilities of trovafloxacin as treatments B and A were 91.3% and
94.5% respectively of that of treatment C. The results of these studies
indicate that trovafloxacin has good oral bioavailability and that the
ingestion of food is unlikely to have a clinically significant effect on
the bioavailability of trovafloxacin.
ORIGINAL ARTICLES
Oral bioavailability of trovafloxacin with and without food in healthy volunteers
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
CiteULike 
Connotea 
Del.icio.us What's this?
This article has been cited by other articles:
|
|
 |
|
  A. M. Noreddin, V. L. Haynes, and G. G. Zhanel Pharmacokinetics and Pharmacodynamics of the New Quinolones Journal of Pharmacy Practice, December 1, 2005; 18(6): 432 - 443. [Abstract] [PDF]
|
|