Pharmacological Profile of Different Berberine Formulations, and Effects on Blood Sugar Levels

Study Overview
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Brief Summary
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The primary objective of this study is to evaluate the gastrointestinal absorption of berberine (hydrochloride) in a novel formulation in healthy adult volunteers by comparing it with free berberine (hydrochloride) formulation. Several pharmacokinetic parameters are compared. As secondary objective, the immediate or short-term effects of Berberine supplementation on blood sugar levels in healthy volunteers are evaluated via a glucose tolerance test (OGTT) using a portable glucometer.

Official Title
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Comparing the Pharmacological Profile of Different Berberine Formulations, and Their Effects on Blood Sugar Levels

Conditions
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Pharmacokinetics

Intervention / Treatment
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* Dietary Supplement: Berberine LipoMicel
* Dietary Supplement: Regular Berberine hard-gels


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Age 21-65 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 Hematological disease Diabetes Allergy or Intolerance to gluten Allergy or Intolerance to Berberine Use of any form of nicotine or tobacco Alcohol and substance abuse history Use of medications (e.g., blood sugar-lowering agents, or statins) Use of Berberine supplements Participation in another investigational study

Ages Eligible for Study
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Minimum Age: 21 Years
Maximum Age: 65 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Non-Randomized
Intervention Model: Crossover Assignment
Masking: Double


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Berberine LipoMicel soft-gel<br>Each participant receives their treatment of Berberine LipoMicel soft-gel capsules at a total dose of 500 mg berberine. Treatments are consumed with a glass of water (approx. 200 mL), and standardized breakfast. A standardized lunch is served after the 4hr fasting; standardized dinner after 8hrs. Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours. Samples that are not processed the same day are kept frozen at -20°C until further processing and analysis. Processed samples are analyzed by LC-MS within 24 hours after processing. Participants are asked to arrive after an overnight fast (at least 9hrs). Each participant acts as their own control; there is no separate control group. A washout period of at least 7 days between each treatment will be used. Adverse events are recorded throughout the study by direct questioning. | Dietary Supplement: Berberine LipoMicel<br>* Berberine LipoMicel® soft-gels. Total dose of 500 mg of berberine<br>|
| Experimental: Regular Berberine hard-gel<br>Each participant receives their treatment of regular Berberine hard-gel capsules at a total dose of 500 mg berberine. Treatments are consumed with a glass of water (approx. 200 mL), and standardized breakfast. A standardized lunch is served after the 4hr fasting; standardized dinner after 8hrs. Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours. Samples that are not processed the same day are kept frozen at -20°C until further processing and analysis. Processed samples are analyzed by LC-MS within 24 hours after processing. Participants are asked to arrive after an overnight fast (at least 9hrs). Each participant acts as their own control; there is no separate control group. A washout period of at least 7 days between each treatment will be used. Adverse events are recorded throughout the study by direct questioning. | Dietary Supplement: Regular Berberine hard-gels<br>* Total dose of 500 mg of berberine<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| AUC: the area under the concentration-time curve | To evaluate the gastrointestinal absorption of orally ingested berberine (hydrochloride) in a novel formulation in healthy adult volunteers by comparing the Area under the plasma concentration versus time curve (AUC) with that of with free/regular berberine (hydrochloride). | 0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours (post-dose) | 
| Cmax: maximum plasma concentration | To evaluate the gastrointestinal absorption of orally ingested berberine (hydrochloride) in a novel formulation in healthy adult volunteers by comparing the Peak Plasma Concentration (Cmax) with that of with free/regular berberine (hydrochloride). | 0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours (post-dose) | 
| Tmax: the time point of maximum plasma concentration | To evaluate the gastrointestinal absorption of orally ingested berberine (hydrochloride) in a novel formulation in healthy adult volunteers by comparing the time point of maximum plasma concentration (Tmax) with that of with free/regular berberine (hydrochloride). | 0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours (post-dose) | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Effects on Blood sugar levels | To evaluate the immediate or short-term effects of orally ingested Berberine on blood sugar levels in healthy volunteers by using a glucose tolerance test (OGTT). | 0 (Baseline; pre-dose), 0.5, 1, 2, 3, and 4 hours (post-dose) | 
| Changes in Blood sugar concentrations | To evaluate changes in blood sugar concentrations of orally ingested Berberine in healthy volunteers by using a portable glucometer. | 0 (Baseline; pre-dose), 0.5, 1, 2, 3, and 4 hours (post-dose) | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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Bioavailability, Berberine, LipoMicel, Pharmacokinetics