Open    Access



Effect of food on the Oral Bioavailability of Berberine and Monacolin Administered in Combination in Healthy Male Volunteers



Author(s)

Stefano Persiani, Federica Sala, Monique Zangarini, Carla Manzotti, Milena Colovic, Yves Donazzolo, Beatrice Barbetta, Cristina Vitalini, Giampaolo Giacovelli, Claudio Benvenuti and Lucio C. Rovati

Full-Text PDF XML     3979 Views

DOI:10.17265/2328-2150/2014.12.003

Objectives: To investigate the effect of food on the bioavailability of a combination of monacolin and berberine in healthy volunteers. Methods: Eighteen male volunteers received a single recommended oral dose of the combination under fasted conditions (reference) and fed conditions (high fat meal; test), in a randomized, open label, crossover fashion. Plasma concentrations of berberine, monacolin and its metabolite were measured by LC-MS/MS. Pharmacokinetic parameters were determined by non-compartmental analysis. No effect of food was assumed if the 90% CIs (confidence intervals) for estimated ratio test/reference was included in the acceptance limits 0.80-1.25 for phenotyping metrics AUC_t and C_max. Key findings: For berberine, the C_max and AUC_t test/reference ratios were 2.97 and 2.69, respectively, and relevant 90% CIs (2.25-3.91 and 2.15-3.36, respectively) were above the acceptance limit. For lovastatin hydroxy acid, the active metabolite of monacolin, the test/reference ratios were 1.18 (C_max) and 0.98 (AUC_t). The 90% CIs fell entirely within the acceptance limit for AUC_t, (0.85-1.13), whereas the upper bound of the 90% CIs for C_max (1.01-1.37) was just above the predefined interval. Conclusions: Food intake significantly increases berberine bioavailability and does not significantly affect monacolin bioavailability when these two extracts are administered in combination.

Berberine, monacolin, food effects, bioavailability, ArmoLIPID PLUS, healthy volunteers.

Persiani, S., et al. 2014. “Effect of food on the Oral Bioavailability of Berberine and Monacolin Administered in Combination in Healthy Male Volunteers.” Journal of Pharmacy and Pharmacology 2 (12): 703-712.