The effects of pummelo juice on pharmacokinetics of sildenafil in healthy adult male Jordanian volunteers.
OBJECTIVE
The main purpose of this work was to investigate the effect of pummelo juice on the pharmacokinetics of sildenafil after oral administration.


METHODS
This was a comparative, randomized, two-period, two-treatment, two-sequence, single dose, crossover study investigating the effect of pummelo juice on the pharmacokinetics of sildenafil citrate tablets (equivalent to 50 mg sildenafil) in healthy male participants under fasting conditions compared with water as a control. Six healthy normal adult males were administered 50 mg sildenafil with pummelo juice or water at two different periods in a crossover study.


RESULTS
Study results showed that pummelo juice reduced the rate and extent of sildenafil bioavailability to around 60% [maximum plasma concentration (C(max)); from 212.44 ng/ml to 134.07 ng/ml, 90% confidence interval (90% CI) 44.70-89.11, and area under the plasma concentration time curve from zero to infinity (AUC(infinity)); from 564.51 ng.hr/ml to 336.87 ng.hr/ml, 90% CI 39.17-90.92]. This interaction was opposite to that expected and is speculated to be due to either an effect on transporters or a physicochemical interaction between sildenafil and some components of the juice.


CONCLUSIONS
Patients should be advised not to drink pummelo juice before or immediately after taking sildenafil.
Al-Ghazawi
Mutasim A
MA
Department of Biopharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, University of Jordan, Amman, Jordan. alghazam@ju.edu.jo
Tutunji
Maha S
MS
AbuRuz
Salah M
SM
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D001628:Beverages; D001682:Biological Availability; D015992:Body Mass Index; D002957:Citrus; D018592:Cross-Over Studies; D018565:Food-Drug Interactions; D005638:Fruit; D006207:Half-Life; D006801:Humans; D007597:Jordan; D008297:Male; D058986:Phosphodiesterase 5 Inhibitors; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011687:Purines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D000068677:Sildenafil Citrate; D013223:Statistics as Topic; D013450:Sulfones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
D058986:Phosphodiesterase 5 Inhibitors; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011687:Purines; D013450:Sulfones; D000068677:Sildenafil Citrate