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1. Stereoselective metabolic disposition of ofloxacin (OFLX) was studied in rats after oral administration of S-(-)-14C-OFLX and R-(+)-14C-OFLX at a dose of 20 mg/kg. 2. Radioactivity of the S-(-)-isomer was eliminated from blood much faster than that of the R-(+)-isomer. Marked differences in pharmacokinetic parameters exist between the enantiomers; the half life and AUC values of R-(+)-OFLX were greater than those of S-(-)-OFLX. Enantiomeric differences were also seen in the excretion of radioactivity, especially in biliary excretion. 3. 31.3 and 7.4% dose were excreted in the 8 h bile as ester glucuronides after oral administration of S-(-)- and R-(+)-OFLX, respectively. The enantiomeric difference in biliary excretion may be caused by stereoselective glucuronidation of S-(-)-OFLX to the ester glucuronide. 4. The metabolite pattern in serum and urine showed that the ester glucuronide of S-(-)-OFLX was more predominant than that of R-(+)-OFLX. 5. The stereoselective ester glucuronidation of the S-(-)-isomer in rats may induce significant differences in the pharmacokinetic parameters of S-(-)- and R-(+)-OFLX.
O Okazaki, and
T Kurata, and
H Tachizawa
January 1999,
Chirality,
O Okazaki, and
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H Tachizawa
January 1992,
Chirality,
O Okazaki, and
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H Tachizawa
May 1985,
British journal of clinical pharmacology,
O Okazaki, and
T Kurata, and
H Tachizawa
October 1994,
British journal of clinical pharmacology,
O Okazaki, and
T Kurata, and
H Tachizawa
August 1991,
Journal of clinical pharmacology,
O Okazaki, and
T Kurata, and
H Tachizawa
December 2004,
British journal of clinical pharmacology,
O Okazaki, and
T Kurata, and
H Tachizawa
September 1978,
Xenobiotica; the fate of foreign compounds in biological systems,
O Okazaki, and
T Kurata, and
H Tachizawa
May 1988,
Clinical pharmacology and therapeutics,
O Okazaki, and
T Kurata, and
H Tachizawa
May 1989,
Circulation,
O Okazaki, and
T Kurata, and
H Tachizawa
September 1991,
Pharmaceutical research,
