Effect of food on the pharmacokinetics of the oral phosphodiesterase 5 inhibitor udenafil for the treatment of erectile dysfunction.
OBJECTIVE
Udenafil is a cyclic guanosine 3',5'-monophosphate-specific phosphodiesterase type 5 (PDE5) inhibitor developed for the treatment of erectile dysfunction. The aim was to evaluate the effect of food on the pharmacokinetics of udenafil.


METHODS
An open, randomized, three-way crossover study was conducted. Fifteen healthy male volunteers received a single 200-mg oral dose of udenafil while fasting, after a low-fat meal, and after a high-fat meal separated by 7-day washout periods. Serial blood samples were taken up to 48 h after oral administration.


RESULTS
Under fasting conditions, udenafil was rapidly absorbed and t(max) was observed typically 1.5 h after administration. The mean t(max) values after a low-fat meal and a high-fat meal were 2.6 and 2.1 h, respectively. The ratios (90% confidence intervals) of the geometric means compared with the fasting condition for C(max) and AUC(last) were 0.79 (0.70, 0.90) and 0.96 (0.89, 1.03) in the low fat-fed condition, respectively, and 1.01 (0.89, 1.15) and 1.03 (0.96, 1.11), respectively, in the high fat-fed condition.


CONCLUSIONS
The t(max) of udenafil was delayed under the fed conditions. However, although the C(max) was reduced by approximately 21% in the low fat-fed state, overall bioavailability was not affected when taken with food.
Kim
Tae-Eun
TE
Department of Pharmacology and Clinical Pharmacology, Seoul National University College of Medicine and Hospital, Daejeon, Korea.
Kim
Bo-Hyung
BH
Kim
Jung-Ryul
JR
Lim
Kyoung Soo
KS
Hong
Jang Hee
JH
Kim
Kyu-pyo
KP
Kim
Hwa-Sook
HS
Shin
Sang-Goo
SG
Jang
In-Jin
IJ
Yu
Kyung-Sang
KS
D000328:Adult; D000368:Aged; D019540:Area Under Curve; D018592:Cross-Over Studies; D007172:Erectile Dysfunction / Q000188:drug therapy*; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D008875:Middle Aged; D010726:Phosphodiesterase Inhibitors / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011743:Pyrimidines / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013449:Sulfonamides; D055815:Young Adult; D000096926:Benzenesulfonamides
D010726:Phosphodiesterase Inhibitors; D011743:Pyrimidines; D013449:Sulfonamides; C419664:udenafil; D000096926:Benzenesulfonamides