Kinetics of absorption and elimination of ofloxacin in humans after oral and rectal administrations.
Ofloxacin pharmacokinetics have been studied in four healthy subjects after a single oral or rectal dose, each of 200 mg. For the oral dose tmax was about 2 h, Cmax 1.96 +/- 0.56 micrograms/ml and AUC1-15 15.22 micrograms/ml.h. Two-phase elimination pharmacol kinetics were observed for the oral dose, t1/2 for the rapid elimination phase was 3.3 h and for the slow phase 10 h. With the rectal dose tmax was 6 h, Cmax 0.71 +/- 0.44 microgram/ml and AUC0-15 7.58 micrograms/ml.h. The relative rectal bioavailability (AUC rectal/AUC oral) was 49.8%. Elimination rate of the rectal dose was generally slow (t1/2 = 9 h), an observation attributable to the sustained-release effect of the rectal suppository base, PEG 6000. The indication is that the rectal formulation cannot be substituted totally for the oral without first increasing the rectal dose; the 200 mg suppository can however be employed as a follow-up therapy to the oral dose in certain situations.
Eboka
C J
CJ
Faculty of Pharmacy, University of Benin, Nigeria.
Okor
R S
RS
Akerele
J O
JO
Aigbavboa
S O
SO
D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D006801:Humans; D008297:Male; D015242:Ofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols; D012007:Rectum; D012463:Saliva / Q000378:metabolism*; D013488:Suppositories
D000890:Anti-Infective Agents; D013488:Suppositories; D011092:Polyethylene Glycols; D015242:Ofloxacin