The goal of this interventional study is to to evaluate the oral bioavailability of the crystallized form of pterostilbene (ccPT) compared to its commercial free base form (pterostilbene (PT) in healthy volunteers. The main question it aims to answer are: • Do the crystallized forms of pterostilbene (ccPT) using two different encapsulation methods exhibit greater bioavailability than its commercial free base form (PT)? Participants will attend to four visits: a preselection visit (V0), a visit for the first postprandial study (V1), a visit for the second postprandial study (V2) after one-week washing period and a visit for the third postprandial study (V3) after another one week washing period. Researchers will analyze the three postprandial assays to determine which type of ccPT encapsulation provides the highest bioavailability compared to the commercial free base form (PT).
The oxidative stress (OS) is a condition where pro-oxidative processes overwhelm cellular antioxidant defenses due to disruption in redox signaling. This results in the body's inability to eliminate reactive oxygen species (ROS) or repair damages, potentially leading to severe impacts on cells, tissues, and organs. Pterostilbene (PT) is a stilbenoid found in various natural sources, emerging as an antioxidant with potential preventive and therapeutic properties in numerous diseases. Despite its promising properties, PT's low water solubility and bioavailability pose challenges. Nutraceutical co-crystallization is a recent strategy to enhance solubility and oral bioavailability. It has been identified that a new pterostilbene:picolinic acid (1:1) co-crystal, significantly increasing solubility and oral bioavailability compared to commercial free base PT. The study aims to evaluate oral bioavailability (AUC0-24h) of PT (free and total) from ccPT compared to commercial PT, using two different encapsulation methods. Secondary objectives include determining pharmacokinetic parameters such as AUCinf, relative oral bioavailability (Frel), Cmax, Tmax, and T1/2 for both free and total PT. This randomized, crossover, single-blind clinical trial aims to provide insights into the effectiveness of the new ccPT formulation in enhancing PT's oral bioavailability compared to the commercial PT formulation.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
SINGLE
Enrollment
6
Participants will intake one gelatin capsule with 75 mg of Pterostilbene cocrystal (ccPT).
Participants will intake one capsule with 50 mg of Pterostilbene free form (PT)
Participants will intake one gastro-resistant capsule with 75 mg of Pterostilbene cocrystal (ccPT).
Fundació Eurecat
Reus, Spain
Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels, both free and total.
Fasting pterostilbene levels in plasma will be determined by liquid chromatography coupled to mass spectrophotometry before consume the capsule with pterostilbene until 24 hours postprandially at 8 points after consuming the capsule (0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours and 24 hours). Total PT will be quantified indirectly after hydrolysis of the conjugated glucuronide and sulfate metabolites to free PT in the presence of β-glucuronidase and arylsulfatase in the plasma samples.
Time frame: At week 1, week 2 and week 3
Area under the curve (AUC 0-inf) of plasma pterostilbene levels, both free and total.
Fasting pterostilbene levels in plasma will be determined by liquid chromatography coupled to mass spectrophotometry before consume the capsule with pterostilbene until 24 hours postprandially at 8 points after consuming the capsule (0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours and 24 hours). Total PT will be quantified indirectly after hydrolysis of the conjugated glucuronide and sulfate metabolites to free PT in the presence of β-glucuronidase and arylsulfatase in the plasma samples.
Time frame: At week 1, week 2 and week 3
Relative bioavailability of plasma pterostilbene levels (Frel).
Relative bioavailability of plasma pterostilbene levels, both free and total
Time frame: At week 1, week 2 and week 3
Maximum plasma concentration (Cmax)
Maximum plasma concentration of pterostilbene, total and free.
Time frame: At week 1, week 2 and week 3
Time for maximum plasma concentration (Tmax)
Time period for the maximum plasma concentration of pterostilbene, both total and free.
Time frame: At week 1, week 2 and week 3
Half-life (T1/2).
Time taken for half the initial dose of pterostilbene, both total and free, administered to be eliminated from the body.
Time frame: At week 1, week 2 and week 3
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.