Аннотация:Objective: Oral administration of coenzyme Q10 (CoQ10) is widely used for treatment of numerous diseases. Aqueous solution of solubilized CoQ10 (Kudesan solution, “Akvion”, Russia) could be administered intravenously (i.v.) in experiments on rats. The aim of the study was to evaluate absolute bioavailability of solubilized CoQ10 given by intragastric (i.g.) and intramuscular (i.m.) route.
Design and Methods: The experiments were carried out on three groups of male Wistar rats with implanted arterial catheters for blood collection. Kudesan solution (10 mg/kg) was administrated i.v. via venous catheter (1st group), i.m. (2nd group) and i.g. (3rd group). Blood samples were collected before and during 48 h after administration. CoQ10 plasma levels in blood samples were measured by HPLC with electrochemical detection. Bioavailability of CoQ10 was calculated by comparing the areas under CoQ10 plasma concentration-time curves, plotted for three groups of rats. Pharmacokinetics parameters of i.v., i.m. and i.g. administed CoQ10 were compared. Statistical analysis was performed with two-tailed t-test. The data were expressed as mean ± SE.
Results: The plasma CoQ10 concentrations in 2 min after i.v. bolus was 2826 ± 10,5 mkg/ml. The maximum plasma concentrations of CoQ10 given by i.g. and i.m. route was 0,57 ± 0,07 and 15,7 ± 3,5 mkg/ml correspondingly. Cmax in plasma was achieved in 3-4 h after i.g. and 10-12 h after i.m. administration. Calculated value of absolute bioavailability of CoQ10 was 0.3% by i.g. and 17% by i.m. administration.
Conclusion: Very low bioavailability of existing forms of CoQ10 preparations for oral administration suggests the perspectiveness of development of CoQ10 parenteral forms for fast increase its intravascular concentration at acute cardiovascular events.
Fig. 1. Plasma CoQ10 concentration-time curves after intravenous, intramuscular and intragastric administration.