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<p>An analytical technique for determining a new dimethylphenylacetamide derivative containing a glutamic acid residue as a counter-ion with cerebroprotective activity in blood using high-performance liquid chromatography with mass spectrometric detection is presented. The systemic pharmacokinetic parameters of 2-diethylamino-2,6-dimethylphenylacetamide L-glutaminate (laboratory code LHT-300) were determined after a single intravenous administration to rabbits at a dose of 2.5 mg/kg as <i>C</i><sub>max</sub> = 845 ng/mL, <i>AUC</i><sub>0–24</sub> = 1045 ng/mL/h, <i>t</i><sub>1/2α</sub> = 0.224 h, <i>t</i><sub>1/2β</sub> = 4.69 h, and <i>V</i><sub>ss</sub> = 6.24 L/kg. The bioavailability of LHT-300 after intramuscular administration was 69.1%. High values of the apparent distribution volume (5.44 – 6.24 L/kg) confirmed that LHT-300 was distributed in tissues and possibly permeated into cells. The sufficiently high bioavailability of the compound upon intramuscular administration allowed us to conclude that this administration route could be used in clinical application of the LHT-300 dosage form.</p>

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Pharmacokinetics and Bioavailability of 2-Diethylamino-2′6′-Dimethylphenylacetamide L-Glutaminate

  • 期刊论文

  • 发表日期：

    2025年11月1日

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  • R. M. Termulaeva,
  • N. D. Bunyatyan,
  • S. Ya. Skachilova,
  • M. A. R. Farahmand,
  • E. V. Blinova,
  • A. S. Pirozhkov,
  • E. V. Semeleva,
  • K. D. Blinov,
  • D. E. Timoshkin,
  • A. A. Dmitriev,
  • D. S. Blinov

摘要

An analytical technique for determining a new dimethylphenylacetamide derivative containing a glutamic acid residue as a counter-ion with cerebroprotective activity in blood using high-performance liquid chromatography with mass spectrometric detection is presented. The systemic pharmacokinetic parameters of 2-diethylamino-2,6-dimethylphenylacetamide L-glutaminate (laboratory code LHT-300) were determined after a single intravenous administration to rabbits at a dose of 2.5 mg/kg as Cmax = 845 ng/mL, AUC0–24 = 1045 ng/mL/h, t1/2α = 0.224 h, t1/2β = 4.69 h, and Vss = 6.24 L/kg. The bioavailability of LHT-300 after intramuscular administration was 69.1%. High values of the apparent distribution volume (5.44 – 6.24 L/kg) confirmed that LHT-300 was distributed in tissues and possibly permeated into cells. The sufficiently high bioavailability of the compound upon intramuscular administration allowed us to conclude that this administration route could be used in clinical application of the LHT-300 dosage form.