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

Autor:	Yu. I. Murinov, S. F. Petrova, V. A. Kataev, V. V. Kataev, S. A. Bashkatov, V. N. Perfilova, E. F. Agletdinov, Sergey P. Ivanov
Rok vydání:	2021
Předmět:	Pharmacology Drug Gastrointestinal tract Chemistry media_common.quotation_subject Metabolite Urine Dosage form Excretion chemistry.chemical_compound Pharmacokinetics Intragastric administration Drug Discovery media_common
Zdroj:	Pharmaceutical Chemistry Journal. 55:531-535
ISSN:	1573-9031 0091-150X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::d49912423cff77f86b6ea52e620d497c https://doi.org/10.1007/s11094-021-02454-5 Zobrazit plný text záznamu Plný text ve formátu PDF