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.
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The article was written using results from preclinical studies of the drug based on a combination of LC, glycyrrhizic acid, and methyluracil. The research was conducted in the framework of State Contract for R&D No. 14.N08.11.0068 of Dec. 2, 2015 and was directed by Prof. V. A. Kataev, Chair of the Pharmacy Department, BSMU.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 6, pp. 3 – 7, June, 2021.
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Kataev, V.A., Petrova, S.F., Perfilova, V.N. et al. Pharmacokinetic Parameters of the Lappaconitine, Glycyrrhizic Acid and Methyluracil Combination Exhibiting Antiarrhythmic Properties upon Single Intragastric Administration in Various Doses. Pharm Chem J 55, 531–535 (2021). https://doi.org/10.1007/s11094-021-02454-5
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DOI: https://doi.org/10.1007/s11094-021-02454-5