Статья

Pharmacokinetic Parameters of the Lappaconitine, Glycyrrhizic Acid and Methyluracil Combination Exhibiting Antiarrhythmic Properties upon Single Intragastric Administration in Various Dose

Kataev, V.A., Petrova, S.F., Perfilova, V.N., Murinov, Y.I., Bashkatov, S.A., Ivanov, S.P., Kataev, V.V., Agletdinov, E.F.
2021

The pharmacokinetic properties of a finished dosage form (FDF) of a combination of lappaconitine, glycyrrhizic acid, and methyluracil (LGM) possessing antiarrhythmic activity were studied. The FDF of LGM upon a single intragastric administration in various doses [1680, 3360, and 6720 mg/kg in terms of lappaconitine (LC)] was rapidly absorbed from the gastrointestinal tract with the maximum blood-plasma concentration of LC being reached 15 min after drug intake. LC had a short elimination half-life and retention time in the body. The drug was extensively distributed throughout organs and tissues and exhibited tropism for the kidneys, liver, and myocardium. LC was metabolized to form N-deacetyllappaconitine (N-DLC). Its metabolite was detected in urine for at least 72 h, which indicated predominant excretion of the drug through the kidneys. The pharmacokinetic profile of N-DLC was similar to that of LC. © 2021, Springer Science+Business Media, LLC, part of Springer Nature.

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