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PI‐63
Author(s) -
Yeo C.,
Shon J.,
Liu K.,
Lee D.,
Yoon Y.,
Shin J.
Publication year - 2006
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2005.12.084
Subject(s) - simvastatin , pharmacokinetics , pharmacology , traditional medicine , medicine , chemistry
BACKGROUND Previous in vitro and animal experiments reported that pomegranate juice increased markedly the bioavailability of carbamazepine due to a potent inhibition of CYP3A4. This study was aimed to evaluate the effect of pomegranate on the disposition of simvastatin and its active metabolite, simvastatin acid, compared with grapefruit juice in 12 healthy volunteers. METHOD At first, simvastatin (40mg) PK study was conducted. And then, after drinking grapefruit juice or pomegranate juice three times per a day (900mL/day) for three days, simvastatin PK study was repeated in two way, cross‐over with 1 week washout. Blood samples were serially taken up to 12hours. Assay of plasma simvastatin and simvastatin acid were conducted using a LC/MS/MS. RESULTS In the grapefruit juice phase, Cmax(mean : 54.3±25.0 ng/ml & 15.5±9.1 ng/ml) and AUC inf (248.4±11.9 ng·h/ml & 99.62±64.0 ng·h/ml) of simvastatin & simvastatin acid were increased significantly compared when taking simvastatin only (Cmax − 4.3±4.7 & 2.1±1.3; AUC inf − 32.5±21.3 & 13.6±8.9, p <0.05). In contrast, in the pomegranate juice phase, pharmacokinetic parameters (Cmax − 4.3±2.0 & 1.5±0.8; AUC inf − 43.5±30.9 & 10.2±9.0) were not different with those in the only simvastatin phase. CONCLUSION These results suggest that drinking of pomegranate seems not to affect on the disposition of simvastatin in human and have an inhibitory potential of CYP3A4. Future study would be needed. Clinical Pharmacology & Therapeutics (2005) 79 , P23–P23; doi: 10.1016/j.clpt.2005.12.084