Absorption Kinetics of Berberine and Dihydroberberine and Their Impact on Glycemia: A Randomized, Controlled, Crossover Pilot Trial.
Level 2 - randomized trial
Randomized double-blind crossover pilot trial
PubMed 35010998 · doi:10.3390/nu14010124
What was done
A randomized, double-blind, crossover pilot trial in 5 healthy males (mean age 26 ± 2.6 years) compared four 4-dose protocols: placebo, 500 mg berberine (B500), 100 mg dihydroberberine (D100), and 200 mg dihydroberberine (D200). Participants ingested three doses the day prior with meals, fasted overnight (8–10 hours), and consumed the fourth dose with a standardized test meal (30 g glucose solution plus 3 slices of white bread). Venous blood samples were collected at 0, 20, 40, 60, 90, and 120 minutes post-ingestion to measure plasma berberine, glucose, and insulin peak concentration (Cmax) and area under the curve (AUC).
What was found
Baseline plasma berberine differed across conditions (p = 0.006), with D100 differing from placebo and B500. Berberine Cmax for D100 was 3.76 ± 1.4 ng/mL versus 0.22 ± 0.18 ng/mL for placebo (p = 0.005) and 0.4 ± 0.17 ng/mL for B500 (p = 0.005). Cmax for D200 reached 12.0 ± 10.1 ng/mL (trend vs B500, p = 0.06; D100 vs D200, p = 0.11). Berberine AUC over 120 minutes for D100 was 284.4 ± 115.9 ng/mL × min, significantly higher than placebo (20.2 ± 16.2 ng/mL × min, p = 0.007) and B500 (42.3 ± 17.6 ng/mL × min, p = 0.04). No significant differences were observed across conditions for glucose (p = 0.97) or insulin (p = 0.24).
Why it matters
Oral dihydroberberine markedly improves plasma berberine bioavailability compared to standard berberine at lower oral doses, potentially overcoming the poor absorption profile of standard berberine.
Limits
The sample size is extremely small (n = 5) and restricted to healthy, young, insulin-sensitive males. Baseline berberine concentrations differed between conditions, suggesting possible carryover effects. The study measured only acute 2-hour postprandial responses and demonstrated no functional glycemic or insulinemic effects in this population.
Cited by
- contradicts Dihydroberberine is approximately 40 times more bioavailable/absorbable than standard berberine.