<p>We compared the pharmacokinetic parameters of liposomal emulsion and aqueous solution of Mexidol after intravenous injection to rats at a dose of 50 mg/kg. The concentrations of Mexidol in blood plasma and homogenates of the lungs, liver, kidneys, testes, and ovaries were measured 30, 60, 120, 240 min, 24 and 48 h after administration by HPLC. The liposomal Mexidol in contrast to its aqueous solution quickly disappeared from systemic circulation (a 5-fold decrease in plasma concentration was noted as soon as 4 h after administration) and was predominantly absorbed and retained for a longer period by the liver and lungs: after 24 h, the concentration of liposomal Mexidol exceeded that of its water-soluble form by 14.2 times in the liver and by 63% in the lungs. In the testes, the concentration of liposomal Mexidol exceeded that of its water-soluble form during the first 4 h postinjection: by 4 times after 1 h and by 2 times after 4 h, whereas in the ovarian tissues, the same concentrations were observed after administration of liposomal and water-soluble forms. In the gonadal tissues, the water-soluble form of Mexidol was retained longer than its liposomal form.</p>

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Comparative Assessment of Pharmacokinetic Parameters of Mexidol after Intravenous Administration of Liposomal Emulsion and Aqueous Solution to Rats

  • V. S. Shindyaikina,
  • A. V. Siprov,
  • V. I. Inchina,
  • I. A. Gololobova,
  • V. I. Shlyapkina,
  • O. A. Kulikov

摘要

We compared the pharmacokinetic parameters of liposomal emulsion and aqueous solution of Mexidol after intravenous injection to rats at a dose of 50 mg/kg. The concentrations of Mexidol in blood plasma and homogenates of the lungs, liver, kidneys, testes, and ovaries were measured 30, 60, 120, 240 min, 24 and 48 h after administration by HPLC. The liposomal Mexidol in contrast to its aqueous solution quickly disappeared from systemic circulation (a 5-fold decrease in plasma concentration was noted as soon as 4 h after administration) and was predominantly absorbed and retained for a longer period by the liver and lungs: after 24 h, the concentration of liposomal Mexidol exceeded that of its water-soluble form by 14.2 times in the liver and by 63% in the lungs. In the testes, the concentration of liposomal Mexidol exceeded that of its water-soluble form during the first 4 h postinjection: by 4 times after 1 h and by 2 times after 4 h, whereas in the ovarian tissues, the same concentrations were observed after administration of liposomal and water-soluble forms. In the gonadal tissues, the water-soluble form of Mexidol was retained longer than its liposomal form.