NCT06289140

Oral Bioavailability of a New Formulation of Pterostilbene Cocrystal in Comparison With Its Free Form (BIOPTERO2)

Evaluation of the Oral Bioavailability of a New Formulation of Pterostilbene Co-crystal in Comparison With Its Free Form in Healthy Volunteers: Crossover, Randomized and Simple Blind Study (BIOPTERO2)

• Status: Completed
• Phase: N/A
• Study type: Interventional
• Enrollment: 6 (actual)
• Sponsor: Fundació Eurecat · Academic / Other
• Sex: Male
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

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).

Detailed description

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.

Conditions

• Biological Availability

Interventions

Type	Name	Description
DIETARY_SUPPLEMENT	Pterostilbene cocrystal (ccPT) - Gelatin capsule	Participants will intake one gelatin capsule with 75 mg of Pterostilbene cocrystal (ccPT).
DIETARY_SUPPLEMENT	Pterostilbene free form (PT)	Participants will intake one capsule with 50 mg of Pterostilbene free form (PT)
DIETARY_SUPPLEMENT	Pterostilbene cocrystal (ccPT) - Gastro-resistant capsule	Participants will intake one gastro-resistant capsule with 75 mg of Pterostilbene cocrystal (ccPT).

Timeline

• Start date: 2024-03-11
• Primary completion: 2024-05-07
• Completion: 2024-05-07
• First posted: 2024-03-01
• Last updated: 2024-06-06

Locations

1 site across 1 country: Spain