title: Pomelo enhances cyclosporine bioavailability in healthy male Thai volunteers.
abstract: The aim of this study was to investigate the effect of pomelo pulp on the pharmacokinetics of cyclosporine in healthy male Thai volunteers. The study design was an open-label, randomized, single dose, crossover study with a 2-week washout period. A single oral dose of 2 × 100 mg cyclosporine was administered with 200 mL of water. Each subject received 250 g of pomelo pulp or 250 mL of water 1 hour before drug administration and once again 10 minutes following drug administration. Blood samples were collected over a 24 hour period. The point estimates (90% confidence intervals) of the test/control ratio using logarithmic transformed data for the area under the curve (AUC) for blood concentration from time 0 to infinity (AUC(0- ∞)) and the observed maximum concentration (C(max)) were 128.8% (120.6-137.6) and 136.1% (126.0-146.8), respectively. These 90% confidence intervals were higher than the accepted bioequivalence range defined by the European Medicines Agency guidelines for narrow therapeutic index drugs (90%-111% for AUC and 80%-125% for C(max)). However, the apparent terminal half-life (t(1/2)) was not significantly different. In conclusion, co-administration of cyclosporine and pomelo pulp increased the relative bioavailability of cyclosporine.
authors.affiliation: Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand.
authors.forename: Wirin
authors.initials: W
authors.lastname: Anlamlert
authors.forename: Pakawadee
authors.initials: P
authors.lastname: Sermsappasuk
authors.forename: Dhirayudh
authors.initials: D
authors.lastname: Yokubol
authors.forename: Sirada
authors.initials: S
authors.lastname: Jones
mesh_terms: D000293:Adolescent; D000328:Adult; D044466:Asian People; D001682:Biological Availability; D002957:Citrus; D018592:Cross-Over Studies; D016572:Cyclosporine / Q000097:blood / Q000493:pharmacokinetics*; D005638:Fruit; D064368:Healthy Volunteers; D041743:Herb-Drug Interactions; D006801:Humans; D008297:Male; D055815:Young Adult
chemical_list: D016572:Cyclosporine
keywords: Citrus grandis; bioavailability; cyclosporine; drug interaction; pomelo