Bioavailability and Sustained Plasma Concentrations of CoQ10 in Healthy Volunteers by a Novel Oral Timed-Release Preparation

Abstract

Coenzyme Q10 (CoQ10) is a natural compound with potent antioxidant properties. Its provision through diet does not always allow adequate levels in the human body, and supplementation is often necessary. This bioavailability study intended to explore the plasma concentration levels of a novel CoQ10 oral preparation (COQUN®, Coenzyme Q10 Miniactives Retard 100 mg capsules) mimicking assumption on a regular basis. Twenty-four healthy adults tested a single dose of CoQ10 100 mg in one day to assess bioavailability. After a one week wash-out period, they were randomly assigned (1:1) to continuous administration for four weeks: Group A (n = 12) 100 mg once a day (OD); and Group B (n = 12) 100 mg twice a day (BID). During the single dose phase, Cmax was observed at 4 h, and the mean values of AUCt and Tmax were 8754 μg/mL·h and 4.29 h, respectively. The multiple dose phase showed increasing plasma levels up to 7 days after the start of administration, and sustained high concentrations during the all administration period. No relevant adverse events were reported. These results show that Miniactives® technology can release CoQ10 to allow high constant blood concentrations without a sharp decrease. This may be the first step of evidence for a potential new antioxidative treatment in human chronic diseases deserving high CoQ10 levels.

Comparative Bioavailability of Different Coenzyme Q10 Formulations in Healthy Elderly Individuals

“…These efforts have been focused on reductions in its particle size and the modulation of its water solubility/dispersibility, e.g., using complexation, solubilization, or reduction [3]. In a recent study, very promising results using modified-release preparations were also reported [14].…”

Miso Soup Consumption Enhances the Bioavailability of the Reduced Form of Supplemental Coenzyme Q10

“…Another limitation of our study was that there is no negative control, i.e., meals alone. In the previous reports, there was no placebo control for the determination of the absorption/bioavailability of CoQ 10 supplements [25][26][27][52][53][54][55]. Also, the effect of CoQ 10 contents in the provided meals seemed to be extremely low as the estimated CoQ 10 amount was less than one two-hundredth of the CoQ 10 supplements ingested.…”

Effect of antioxidants coenzyme Q10 and β‑carotene on the cytotoxicity of vemurafenib against human malignant melanoma

“…Due to the low concentration of coenzyme Q10 in melanoma cell lines, and in sera of patients with melanoma, CoQ10 was used in combination with an optimized dose of recombinant interferon α-2b in a 3-year trial, which demonstrated that this combination significantly reduced the recurrence rate ( 79 ). A recent study reported that the mean of maximum plasma concentration in a group of healthy volunteers who received 100 mg (Bid) of CoQ10 was 1501 µg/l (1.8 µM) ( 80 ). It is also known that 300 mg per day is a common dosage of commercial products of coenzyme Q10 ( 81 ).…”