A Randomized, Double-Blind, Crossover Study on the Pharmacokinetics of a Novel Formulation of CoQ10 With Pyridoxal 5′-Phosphate and Phosphatidyl Choline

Abstract

ABSTRACTThe pharmacokinetics of a single 30-mg dose of a novel enteric-coated coenzyme Q10 (CoQ10) formulation with pyridoxal 5′-phosphate and phosphatidyl choline (CoQ10-P5P-PC) was investigated against two comparators CoQ10 (NPN 02176955) and CoQ10 (DIN 02231736) in 21 healthy volunteers, with screening CoQ10 levels of 0.8 ± 0.2 mg/L. A randomized, double-blind, crossover study was designed with a washout period of 2 weeks between each formulation and blood sampled at 2, 4, 5, 6, 8, 12, 24, 48 and 72 hr postdose. Significantly, higher plasma concentrations were demonstrated for the CoQ10 (NPN 02176955) formulation at 6 and 8 hr postdose (p = .010 and p = .042, respectively). There were no significant differences between formulations with respect to the area under the curve, AUC(0–72 hr), or the maximum plasma concentration (Cmax). Total CoQ10 (Tmax) reached maximum plasma concentrations at 6.4 ± 2.5 hr after supplementation with CoQ10 (NPN 02176955), 8.0 ± 9.8 hr with CoQ10-P5P-PC, and 9.5 ± 9.3 hr with CoQ10 (DIN 02231736). The estimated elimination half-life (t1/2) was 92.3 hr after a single oral dose of CoQ10-P5P-PC, 38.2 hr with CoQ10 (NPN 02176955), and 80.7 hr with CoQ10 (DIN 02231736). The results suggest that CoQ10 is available for a longer time in subjects’ administered with CoQ10-P5P-PC in comparison with the other two formulations studied. There were no significant differences in adverse events, by severity, causality, or organ system. The CoQ10-P5P-PC formulation was found to be superior in the t1/2, and it may be suggested that fewer doses are required to maintain healthy circulatory CoQ10 levels.