The pharmacokinetics and myocardial levels of coenzyme Q10 after intramuscular injection of its solubilized formтезисы доклада

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Дата последнего поиска статьи во внешних источниках: 12 января 2016 г.

Работа с тезисами доклада

[1] The pharmacokinetics and myocardial levels of coenzyme q10 after intramuscular injection of its solubilized form / E. Kalenikova, E. Gorodetskaya, E. Kharitonova, O. Medvedev // Journal of Hypertension. — Vol. 29 of № e-Suppl. A. — Lippincott Williams & Wilkins Ltd United States, 2011. — P. 319–319. Objective: Coenzyme Q10 (CoQ10, hypotensive and cardioprotective agent) has very poor per os bioavailability due to its high lipophylity and limited solubility. Cardioprotective effect of CoQ10 is provided with increased CoQ10 myocardial content as a result of the long-term per os administration. In this study the pharmacokinetics and tissue levels of CoQ10 following intramuscular injection of its solubilised form were examined. Design and Methods: The experiments were carried out on two groups of male Wistar rats with implanted arterial catheters. Solubilized CoQ10 (Kudesan solution, “Akvion”, Russia) was administrated in dose 10 mg/kg intramuscularly (i.m.) in the first group and per os in the second group. The content of CoQ10 were determined in plasma, left ventricle myocardium and liver by HPLC with electrochemical detection. Blood samples were collected before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 24, and 48 h after CoQ10 administration. Tissues samples were collected 48 h after administration. Bioavailability of CoQ10 was calculated by comparing the areas under plasma concentration – time curves (AUC, mkg*h/ml). Pharmacokinetics parameters of i.m. and per os administrated CoQ10 were compared. Statistical analysis was performed with two-tailed t-test. The data were expressed as mean ± SE. Results: Pharmacokinetics parameters of i.m. administrated CoQ10 differed significantly from those of per os administrated CoQ10. The plasma concentrations of CoQ10 during 48h after i.m. administration were significantly higher than those after per os administration. Tmax after i.m. administration was about 8 h, after per os administration – about 3 h. The maximum plasma concentrations after i.m. bolus was 8-fold (p<0,01) higher than that after per os administration. AUC for i.m. administrated CoQ10 was 134.6±10.5, for per os administrated CoQ10 – 6.7±2.3. Hence, bioavailability of CoQ10 after i.m. versus per os administration was 1900% (p<0,01). It was accompanied with increase of CoQ10 level in myocardium by 17% and in liver by 175%. Conclusion: Intramuscular administration of solubilized CoQ10 ensures growth of myocardial CoQ10 content and gives occasion to investigation efficiency of this rout of administration at acute cardiovascular events. [ DOI ]

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