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| Name | Class |
|---|---|
| Circe, S.L. | UNKNOWN |
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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:
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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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Pterostilbene cocrystal | Experimental |
| |
| Pterostilbene free form | Active Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Pterostilbene cocrystal | Dietary Supplement | One capsule with Pterostilbene cocrystal |
|
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
| Measure | Description | Time Frame |
|---|---|---|
| Maximum plasma concentration (Cmax) | Maximum plasma concentration of pterostilbene | At week 1 and week 2 |
| Time for maximum plasma concentration (Tmax) | Time period for the maximum plasma concentration of pterostilbene. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Antoni Caimari, PhD | UTNS (Eurecat_Reus) | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Eurecat | Reus | 43204 | Spain |
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| Label | URL |
|---|---|
| Technological Centre of Nutrition and Health. Eurecat\_Reus. | View source |
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In this study IPD will not be shared with other researchers because all the information will be processed by the UTNS of Eurecat.
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| Pterostilbene free form | Dietary Supplement | One capsule with Pterostilbene free form |
|
| At week 1 and week 2 |
| 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 |
| 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 |
| 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 |