Relative bioavailability of coenzyme Q10 formulation for paediatric individualized therapy

MARTINEFSKI M.,; SAMASSA P; BUONTEMPO F; LUCANGIOLI S.; TRIPODI V.

JOURNAL OF PHARMACY AND PHARMACOLOGY

PHARMACEUTICAL PRESS-ROYAL PHARMACEUTICAL SOC GREAT BRITIAN

Año: 2017 vol. 69 p. 567 - 573

0022-3573

Objectives Conduct a preliminary comparison of the bioavailability betweentwo formulations: commercial grade coenzyme Q10 (CoQ10) powder (solid formulation)and a new oil-in-water liquid emulsion and their effect on otherantioxidants.Methods Six healthy individuals participated in a randomized, crossover, open,consecutive design, with a 2-week washout period. Pharmacokinetic parameterswere assessed after a single and multiple intakes of 250 mg CoQ10 given daily for1 week.Key Findings The differences in the pharmacokinetic parameters of maximumplasma concentration, area under the curve between 0?360 and 0?4 h, eliminationhalf-life were statistically significant with a relative bioavailability of 489%increase over solid CoQ10 formulation. A multiple dose supplementationincreased plasma CoQ10 levels in both formulations, liquid emulsion performingbetter (2.4- vs 3.9-fold for solid and liquid formulation, respectively) withoutmodifications on other antioxidants. Furthermore, the plasma CoQ10 at 7th daywas statistically different between formulations (P < 0.05).Conclusions The results obtained showed that liquid emulsion improves thebioavailability of CoQ10 respect to solid form which not only facilitates the individualizedadministration for the child but in turn could increase the therapeuticefficacy, which should be confirmed by further studies.IntroductionCoenzyme Q10 (2,3-dimethoxy-5-methyl-6-decaprenyl-1,4-benzoquinone) (CoQ10) (Figure 1), also known as ubiquinone,is a lipophilic molecule classified as a fat solublequinone. CoQ10 is a component of the mitochondrial respiratorychain where it acts controlling the efficiency ofoxidative phosphorylation and being essential for the productionof cellular energy. Due to its hydrophobicity,CoQ10 is inserted into the mitochondrial inner membrane.Moreover, CoQ10 is also considered an antioxidant agenttogether with other lipophilic antioxidants and plays anintrinsic role in protecting circulating lipoproteins againstoxidative damage.[1,2]Human CoQ10 deficiency can be classified as primary orsecondary resulting in different heterogeneous diseases.Primary CoQ10 deficiency seems to be relative rare and has