Oral Bioavailability of Pterostilbene Cocrystal Compared to Its Free Form (BIOPTERO)

Biological Availability Clinical Trial

— BIOPTERO  

Official title:

Evaluation of the Oral Bioavailability of Pterostilbene Cocrystal Compared to Its Free Form in Healthy Volunteers. Crossover, Randomized, Double-Blind Study (BIOPTERO)

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT05561075
• Other study ID #: BIOPTERO
• Status: Completed
• Phase: N/A
• Start date: October 20, 2022
• Est. completion date: November 17, 2022

Study information

• Verified date: March 2023
• Source: Fundació Eurecat
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial Summary

Oxidative stress and reactive oxygen species (ROS) can seriously affect cells, tissues and organs. The human body is capable of counteracting ROS production by stimulating antioxidant defense systems and consequently adapting to the oxidative challenge.

Several transcription factors are involved in the induction of antioxidant genes. Activators of nuclear factor derived from erythroid 2 (NRF2), a protein that controls the expression of certain genes, are considered agents capable of inducing antioxidant capacity and to alleviate ROS. There are some food bioactive compounds, including polyphenols, capable of activating NRF2.

Pterostilbene (PT) is a stilbenoid found in many natural sources, and is emerging as an antioxidant due to its potential preventive and therapeutic properties in a long list of diseases. Despite its apparent properties, the water solubility and bioavailability of PT are low.

The co-crystallization of nutraceuticals is a recent strategy based on crystal engineering to overcome their low solubility and, therefore, their low oral bioavailability. It has been identified and characterized a cocrystal of pterostilbene that can increase oral bioavailability in animals by up to 10 times compared to the commercial free base PT.

The main objective of the study is to evaluate the oral bioavailability of the crystallized form of pterostilbene (ccPT) compared to its commercial free base form (pterostilbene (PT).

The secondary objectives of the study are to determine the pharmacokinetic parameters:

• Relative oral bioavailability (Frel)

• Maximum concentration (Cmax).

• Maximum time (Tmax).

• Half life time (T1/2).

During the study there will be 3 visits: a preselection visit (V0), a visit for the first postprandial study (V1) and after one week washing period, a visit for the second postprandial study (V2).

Recruitment information / eligibility

• Status: Completed
• Enrollment: 6
• Est. completion date: November 17, 2022
• Est. primary completion date: November 17, 2022
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: All
• Age group: 18 Years to 65 Years

Eligibility

Inclusion Criteria:

• Men and women between 18 and 65 years of age.

• Sign the informed consent form.

• Know how to read, write and speak Spanish

Exclusion Criteria:

• Take supplements or multivitamin supplements or phytotherapeutic products (especially infusions) that interfere with the treatment under study up to 30 days before the start of the study.

• Be lacto-vegetarian, lacto-ovo-vegetarian, or vegan.

• Present intolerances and/or food allergies related to pterostilbene.

• Be a smoker.

• Having received antibiotic treatment up to 30 days before the start of the study.

• Present values of body mass index = 18kg/m^2 or = 35 kg/m^2.

• Present some chronic disease with clinical manifestations: coronary heart disease, cardiovascular disease, diabetes, celiac disease, Crohn's disease, chronic kidney disease, cancer, autoimmune diseases (such as fibromyalgia), respiratory and/or gastrointestinal diseases that may compromise the absorption of the compound.

• Clinical history of anemia.

• Being pregnant or intending to became pregnant.

• Be in breastfeeding period.

• Being unable to follow the study guidelines.

• Participate in or have participated in a clinical trial or nutritional intervention study in the last 30 days before inclusion in the study.

Related Conditions & MeSH terms

• Biological Availability

Intervention

Dietary Supplement:
• Pterostilbene cocrystal
One capsule with Pterostilbene cocrystal
• Pterostilbene free form
One capsule with Pterostilbene free form

Locations

Country	Name	City	State
Spain	Eurecat	Reus

Sponsors (2)

Lead Sponsor	Collaborator
Fundació Eurecat	Circe, S.L.

Country where clinical trial is conducted

Spain, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels.	Fasting pterostilbene levels in plasma will be determined 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).	At week 1 and week 2
Secondary	Maximum plasma concentration (Cmax)	Maximum plasma concentration of pterostilbene	At week 1 and week 2
Secondary	Time for maximum plasma concentration (Tmax)	Time period for the maximum plasma concentration of pterostilbene.	At week 1 and week 2
Secondary	Half-life (T1/2).	Time taken for half the initial dose of pterostilbene administered to be eliminated from the body	At week 1 and week 2
Secondary	Area Under the Curve (AUC 0-inf) of plasma pterostilbene levels.	Fasting pterostilbene levels in plasma will be determined 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).	At week 1 and week 2
Secondary	Relative oral bioavailability (Frel)	Fasting pterostilbene levels in plasma will be determined 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).	At week 1 and week 2

External Links

•   Technological Centre of Nutrition and Health. Eurecat_Reus.