Impact of Food Intake on Berberine Kinetics

NCT06273241 | Completed

• 1 other identifier: IPHA-2024-009
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

The influence of genetic variants of the CYP2D6 enzyme and the Organic Cation Transporter 1 (OCT-1) on the kinetics of berberine (BERKI-1) has recently been studied. A significant sex difference was observed. These results lead to the BERKI-2 study, investigating the influence of the female hormonal cycle on berberine kinetics. In this study, women took a single berberine dose once in the first and once in the second half of their menstrual cycle, men served as a control group ingesting a single berberine dose. Contrary to expectations, the previously observed sex difference could not be confirmed. In both BERKI-1 and 2 studies, the plasma concentration curve exhibited two peaks. The first after about 2-3 h, and the second after approximately 5 h of berberine intake. All participants took a single dose of Berberine under fasting conditions in the morning and 4 h after berberine intake, the participants ate a meal. Shortly after meal intake, the plasma concentration curve peaked again. BERKI-3 will investigate the impact of food intake on berberine bioavailability and the kinetic properties. Given the suspected influence of berberine on glycemic control, the investigators will also measure insulin and glucose after the meal at noon. As in BERKI-1 and 2, time dependent blood and urine samples will be collected after a single berberine dose. One by measuring berberine metabolites by Liquid Chromatography and Mass-spec One dose will be taken in the fasted condition and the other two after a light or high caloric meal, respectively. 24 healthy volunteers with an equal ratio of man and women will be enrolled.

Conditions

Pharmacokinetic Study in Healthy Volunteers

Keywords

berberine; food effect; pharmacokinetic

Outcome Measures

Primary Outcomes (1)

• Berberine plasma concentration fasted vs fed

  Difference of berberine plasma concentrations between the fasted and fed condition, expressed as area under the curve (AUC0-24h).

  24 hours

Secondary Outcomes (1)

• Berberine plasma concentrations light vs heavy meal

  24 hours

Other Outcomes (2)

• Blood glucose concentrations

  2 hours

• Blood insulin concentrations

  2 hours

Study Arms (3)

Berberine intake in fasted condition

PLACEBO COMPARATOR

Intake of 1000 mg berberine in the fasted condition (intake of last meal: before 20:00 on the day before the study visit)

Other: food intake

Berberine intake after a low caloric meal

ACTIVE COMPARATOR

Intake of 1000 mg berberine after a light caloric meal (2 toasts, butter, cheese, marmalade)

Other: food intake

Berberine intake after a high caloric meal

ACTIVE COMPARATOR

Intake of 1000 mg berberine after a high caloric meal (2 toasts with butter, 2 fried eggs, 2 slices of bacon, 3 hash brown and 240ml of whole milk)

Other: food intake

Interventions

food intake OTHER

A single dose of 1000 mg berberine in two capsules will be administered with 250 ml of still water in the overnight fasting condition as the control condition. The two intervention arms will test the effect of different meals on berberine kinetics. A total amount of 12 blood samples at defined time points (baseline; 1; 2; 3; 4; 5; 6; 7; 8; 24 h) will be taken. For glucose and insulin measurements, blood samples will be obtained at 4 h, 5 h and 6 h .

Berberine intake after a high caloric meal; Berberine intake after a low caloric meal; Berberine intake in fasted condition

Eligibility Criteria

• Age: 18 Years - 40 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• wildtype genotypes for CYP2D6 and organic cation transporter 1 (OCT-1)
• understands the study purpose and design
• contractually capable and provides signed informed consent form
• healthy condition or mild and/or well treated forms of allergies, asthma, hypertension and orthopedic diseases

You may not qualify if:

• BMI ≤18,5kg/m2 and ≥29,9 kg/m2
• only in women: known pregnancy or lactation period
• only in women: positive pregnancy test at screening or any other study visit
• anemia: Hb \< 13 g/dl (8,07 mmol/l) in men or \< 12 g/dl (7,45 mmol/l) in women
• elevated liver function tests (ALAT, ASAT, yGT, Bilirubin \> 2xULN)
• reduced renal function (eGFRMDRD \< 60ml/min/1,7m2)
• currently mentally unstable
• use of recreational drugs more than twice a week
• poor venous conditions that make it impossible to place a peripheral venous catheter and regularly draw blood through it

Sponsors & Collaborators

• University Medicine Greifswald: lead

Study Sites (1)

University Medicine Greifswald, Institute of Pharmacology

Greifswald, Mecklenburg-Vorpommern, 17487, Germany

Location

MeSH Terms

Interventions

Eating

Intervention Hierarchy (Ancestors)

Nutritional Physiological Phenomena; Diet, Food, and Nutrition; Physiological Phenomena; Digestive System Physiological Phenomena; Digestive System and Oral Physiological Phenomena

Study Officials

• Stefan Engeli, Prof.

  Universitätsmedizin Greifswald, Institut für Pharmakologie

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: NONE
• Masking Details: This study will be an open label study. Participants will be selected from an existing database of the Institute of Pharmacology Greifswald.
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Professor

Model Details: This is an unblinded, randomized, prospective study comparing berberine intake in fasted condition and after a high or low caloric meal in a cross-over design.

Study Record Dates

• First Submitted: February 15, 2024
• First Posted: February 22, 2024
• Study Start: March 4, 2024
• Primary Completion: May 11, 2024
• Study Completion: May 11, 2024
• Last Updated: January 24, 2025

Record last verified: 2025-01

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)