Pharmacological Profile of Different Quercetin Formulations

Factors Group of Nutritional Companies

Status: Completed

Conditions: Pharmacokinetics

Treatments: Dietary Supplement: Quercetin LipoMicel (1000 mg); Dietary Supplement: Regular/standard Quercetin (500 mg); Dietary Supplement: Quercetin LipoMicel (500 mg); Dietary Supplement: Quercetin LipoMicel (250 mg)

Study type: Interventional

Funder types: Industry

Identifiers

NCT05611827

2021-03-002

Details and patient eligibility

About

This study aims to evaluate the pharmacokinetics of quercetin in healthy participants after the administration of different formulations in a single- and multiple-dose phase. In the single-dose study, plasma uptake (AUC0-24 and Cmax) of standard quercetin is compared with that of LipoMicel®-a novel food-grade delivery form of quercetin. In the multiple dose study, accumulating plasma concentrations of formulated quercetin are observed over 72hrs, after repeated doses of LipoMicel treatments (AUC0-72).

At least ten healthy adults participate in an open-label, diet-controlled, crossover, plasma uptake study. Participants receive three different doses (250 mg, 500 mg or 1000 mg) of quercetin aglycone orally.

Full description

Objective of this study is to investigate the pharmacokinetic profile of formulated quercetin (LipoMicel®), administered at three different doses, in healthy participants and compare it with that of a standard formulation. The pharmacokinetics of the different quercetin treatments are observed over 24hrs after a single orally administered dose of quercetin (e.g., using AUC0-24 and Cmax). Furthermore, the accumulating plasma concentrations of formulated quercetin are monitored over a 72hr period (e.g., using AUC0-72), following multiple orally administered doses of LipoMicel treatments (250 mg-1000 mg) plus the circulating metabolites of quercetin are determined in the human plasma.

Enrollment: 10 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• age 18-65
• healthy, good physical condition

Exclusion criteria

• pregnancy or breast-feeding
• gastrointestinal conditions (acute or chronic)
• liver disease (acute or chronic)
• kidney disease (acute or chronic)
• cardiovascular disease (acute or chronic)
• hematological disease
• diabetes
• allergy or intolerance to gluten
• allergy or intolerance to quercetin
• use of any form of nicotine or tobacco, CBD/THC
• alcohol and substance abuse history
• use of medications (e.g., anti-inflammatory)
• use of quercetin supplements
• participation in another investigational study

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

---

10 participants in 4 patient groups

Quercetin LipoMicel (250 mg)

Experimental group

Description:

Each participant receives their treatment of Quercetin LipoMicel at a total dose of 250 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 250 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.

Treatment:

Dietary Supplement: Quercetin LipoMicel (250 mg)

Quercetin LipoMicel (500 mg)

Experimental group

Description:

Each participant receives their treatment of Quercetin LipoMicel at a total dose of 500 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 500 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.

Treatment:

Dietary Supplement: Quercetin LipoMicel (500 mg)

Quercetin LipoMicel (1000 mg)

Experimental group

Description:

Each participant receives their treatment of Quercetin LipoMicel at a total dose of 1000 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 1000 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.

Treatment:

Dietary Supplement: Quercetin LipoMicel (1000 mg)

Regular/standard Quercetin (500 mg)

Experimental group

Description:

Each participant receives their treatment of standard/raw Quercetin at a total dose of 500 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). A standardized lunch and dinner are served after 4h and 8h of product administration. Capillary whole blood samples are collected (after a 10hr overnight fast) at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin. A washout period of at least 7 days between each treatment will be used.

Treatment:

Dietary Supplement: Regular/standard Quercetin (500 mg)