Safety and Pharmacokinetics of an Extract of Naringenin (Citrus)

Pennington Biomedical Research Center

Status and phase: Completed; Early Phase 1

Conditions: Safety Issues; Pharmacokinetics

Treatments: Dietary Supplement: Naringenin; Other: Placebo

Study type: Interventional

Funder types: Other

Identifiers

NCT03582553

2018-011

Details and patient eligibility

About

This study evaluates the safety of administering single ascending doses (150, 300, 600, and 900 mg) of a citrus extract of the flavonoid narigenin, and assesses the blood concentrations of naringenin following oral administration of the extract.

Full description

Naringenin is a component of food with therapeutic potential to improve glucose metabolism. In order to explore the mechanisms by which naringenin may increase energy expenditure and improve glucose metabolism in humans, it is of vital importance that the safety, tolerability, and bioavailability of naringenin are evaluated, when administered to humans. This study tests the safety of four doses of a citrus extract of naringenin and measures serum concentrations of naringenin at the 150 mg and 600 mg doses over a period of 24 hours, and at the 300 and 900 mg doses at four hours after subjects have been given the respective doses of naringenin.

Enrollment: 18 patients

Sex: All

Ages: 18+ years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Adult (≥18 years)
• Body mass index between 20 and 35 kg/m2
• Must have fasting blood sugar <126 mg/dL)
• Must be willing to refrain from consuming citrus fruits and tomato in any form, for 36 hours prior to each test day.

Exclusion criteria

• Report citrus allergies.
• Report a history of cardiovascular disease, diabetes, or cancer
• Have evidence of hepatic disease or dysfunction
• Are currently pregnant or breastfeeding
• Are women of childbearing potential who will not use an effective method of birth control
• Chronically use of medications except over the counter medications that have been stopped 72 hours prior to the study visit
• Report clinically significant GI malabsorption syndromes
• Have clinically significant abnormal laboratory markers
• Anticipate surgery during the study period.
• Report history of substance abuse or alcoholism or significant psychiatric disorder that would interfere with the ability to complete the study.
• Have donated blood during the month prior to study entry or plan to do so during the study.
• Have participated in other studies using an investigational drug during the preceding three months.
• Are current smokers or have smoked within the previous three months.

Trial design

Primary purpose: Other

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: Quadruple Blind

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18 participants in 5 patient groups, including a placebo group

150 mg dose

Experimental group

Description:

Blood will be drawn at at 0, 2, 3, 3.5, 4, 4.5, 6, 8,12, and 24 hours to measure serum naringenin concentrations in response to a single 150 mg oral dose of an extract of Citrus sinensis (sweet orange) containing naringenin and its precursor naringin.

Treatment:

Dietary Supplement: Naringenin

300 mg dose

Experimental group

Description:

Blood will be drawn at at 0, and 4 hours to measure serum naringenin concentrations in response to a single 300 mg oral dose of an extract of Citrus sinensis (sweet orange) containing naringenin and its precursor naringin.

Treatment:

Dietary Supplement: Naringenin

600 mg dose

Experimental group

Description:

Blood will be drawn at at 0, 2, 3, 3.5, 4, 4.5, 6, 8,12, and 24 hours to measure serum naringenin concentrations in response to a single 600 mg oral dose of an extract of Citrus sinensis (sweet orange) containing naringenin and its precursor naringin.

Treatment:

Dietary Supplement: Naringenin

900 mg dose

Experimental group

Description:

Blood will be drawn at at 0, and 4 hours to measure serum naringenin concentrations in response to a single 900 mg oral dose of an extract of Citrus sinensis (sweet orange) containing naringenin and its precursor naringin.

Treatment:

Dietary Supplement: Naringenin

Placebo

Placebo Comparator group

Description:

Subjects in the first cohort will receive 150 mg and 300 mg ascending doses of naringenin and subjects in the second cohort will receive 600 mg and 900 mg ascending doses of naringenin. Each cohort will also have a placebo group.

Treatment:

Other: Placebo