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

ABSTRACT

The 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 (C_max). Total CoQ₁₀ (T_max) 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 (t_1/2) 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 t_1/2, and it may be suggested that fewer doses are required to maintain healthy circulatory CoQ₁₀ levels.

KEYWORDS. :

• CoQ₁₀
• pyridoxal 5′-phosphate
• phosphatidyl choline
• half-life
• pharmacokinetics