Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects.
The present study was conducted to determine the absolute bioavailability of fimasartan (FMS; Kanarb(®) ) after the single oral administration of a 60-mg tablet or a single 30-mg intravenous (IV) infusion. This investigation was a randomized, single-dose, open-labeled, two-way crossover study of 16 healthy Korean male subjects. The subjects were divided into two groups (n = 8) and each received either the oral or IV formulation followed by one-week washout period. The Cmax (ng/ml) and AUC∞ (h · ng/ml) following oral and IV administration were 62.4 ± 48.6 and 291.1 ± 121.7; and 683.3 ± 104.3 and 782.3 ± 112.7 (mean ± SD), respectively. The Tmax (h) were 3.0 h (range: 0.5-5.0 h) and 1.0 h (range: 0.8-1.0 h) in the test and reference groups, respectively. The terminal elimination half-lives (t1/2 , h) were similar (5.8 and 5.5 h, respectively) indicating that the route of administration did not influence the absorption or elimination of FMS. The systemic clearance (CL, L/h) and the volume of distribution at steady-state (Vdss , L) were 331.3 ± 444.5 L/h and 403.3 ± 710.4 L following oral administration and 39.1 ± 5.3 L/h and 42.4 ± 25.5 L following IV administration. The absolute bioavailability of the FMS tablet was 18.6%.
Department of Clinical Pharmacology, Inje University, Busan Paik Hospital, Busan, Korea.
Jong-Lyul
JL
Ghim
Central Research Institute, Boryung Pharmaceutical Co, Ltd, Seoul, Korea.
Soo Heui
SH
Paik
Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Busan, Korea.
M
M
Hasanuzzaman
Central Research Institute, Boryung Pharmaceutical Co, Ltd, Seoul, Korea.
Yong Ha
YH
Chi
Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Busan, Korea.
Hyang-Ki
HK
Choi
Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Busan, Korea.
Dong-Hyun
DH
Kim
Department of Clinical Pharmacology, Inje University, Busan Paik Hospital, Busan, Korea.|Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Busan, Korea.
Jae-Gook
JG
Shin
D000284:Administration, Oral; D000328:Adult; D057911:Angiotensin Receptor Antagonists / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D064368:Healthy Volunteers; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D011743:Pyrimidines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013777:Tetrazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
D057911:Angiotensin Receptor Antagonists; D001713:Biphenyl Compounds; D011743:Pyrimidines; D013777:Tetrazoles; C558933:fimasartan
absolute bioavailability; fimasartan; intravenous; oral; pharmacokinetic