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NCT Number: NCT05561075

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

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).

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Key information

Conditions

Biological Availability

Age range

18 year–65 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Not applicable

Primary location

Eurecat

Reus, 43204, Spain

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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.

Treatment and study plan

Pterostilbene cocrystal

Dietary Supplement

One capsule with Pterostilbene cocrystal

Pterostilbene free form

Dietary Supplement

One capsule with Pterostilbene free form

Primary outcomes

  1. Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels.

    Time frame: At week 1 and week 2

    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).

Secondary outcomes

  1. Maximum plasma concentration (Cmax)

    Time frame: At week 1 and week 2

    Maximum plasma concentration of pterostilbene

  2. Time for maximum plasma concentration (Tmax)

    Time frame: At week 1 and week 2

    Time period for the maximum plasma concentration of pterostilbene.

  3. Half-life (T1/2).

    Time frame: At week 1 and week 2

    Time taken for half the initial dose of pterostilbene administered to be eliminated from the body

  4. Area Under the Curve (AUC 0-inf) of plasma pterostilbene levels.

    Time frame: At week 1 and week 2

    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).

  5. Relative oral bioavailability (Frel)

    Time frame: At week 1 and week 2

    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).

Sponsors and collaborators

Lead sponsor

Fundació Eurecat

Other

Collaborators

  • Circe, S.L.

Registry information

Official study title

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

Acronym: BIOPTERO

Important dates

Study start
2022
Primary completion
2022
Study completion
2022
First posted
Sep 30, 2022
Registry last updated
Mar 16, 2023

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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