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

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.