Please use this identifier to cite or link to this item:
|Title:||Pharmacokinetics of pterostilbene in Sprague-Dawley rats: The impacts of aqueous solubility, fasting, dose escalation, and dosing route on bioavailability|
|Citation:||Yeo, S.C.M., Ho, P.C., Lin, H.-S. (2013-06). Pharmacokinetics of pterostilbene in Sprague-Dawley rats: The impacts of aqueous solubility, fasting, dose escalation, and dosing route on bioavailability. Molecular Nutrition and Food Research 57 (6) : 1015-1025. ScholarBank@NUS Repository. https://doi.org/10.1002/mnfr.201200651|
|Abstract:||Scope: Pterostilbene (trans-3,5-dimethoxy-4'-hydroxystilbene, PTS) possesses various health-promoting effects. This study aimed to investigate the impacts of aqueous solubility, fasting, dose escalation, and dosing route on its bioavailability in Sprague-Dawley rats. Methods and results: Upon intravenous administration (2.5 mg/kg), PTS had rapid clearance (Cl = 68.2 ± 9.8 mL/min/kg) and moderate terminal elimination half-life (t1/2λz = 93.9 ± 22.3 min). Dose-escalation led to about twofold decline in clearance at the dose of 25 mg/kg (Cl = 36.4±7.8 mL/min/kg). When given in oral suspension (15 mg/kg), PTS had relatively low bioavailability (F = 15.9 ± 7.8%) while fasting substantially attenuated its bioavailability (F< 5.5 %). However, when dosed in a solution formulated with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) (15 mg/kg), PTS possessed good bioavailability (F = 59.2 ± 19.6%). Dose escalation resulted in about twofold increase in bioavailability at the dose of 60 mg/kg. Sublingual delivery (2.5 mg/kg) led to rapid absorption and moderate bioavailability (F = 25.8 ± 13.1%). Statistical comparison clearly indicated that the pharmacokinetics of PTS was more favorable than resveratrol. Conclusion: Aqueous solubility was identified as a barrier to its oral bioavailability while solubilizing PTS with HP-β-CD substantially increased its bioavailability; dose manipulation was a practical strategy to enhance its bioavailability and systemic exposure; and its delivery through oral mucosa was feasible. As PTS possessed superior pharmacokinetics, it is a favorable candidate for further development. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.|
|Source Title:||Molecular Nutrition and Food Research|
|Appears in Collections:||Staff Publications|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Nov 19, 2018
WEB OF SCIENCETM
checked on Nov 19, 2018
checked on Nov 16, 2018
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.