Chanal J L, Cousse H, Sicart M T, Bonnaud B, Marignan R
Eur J Drug Metab Pharmacokinet. 1981;6(3):171-7. doi: 10.1007/BF03189486.
Hesperidin methylchalcone resorption and excretion were studied in rats, using 14C-labelling. The level of radioactivity in the blood showed a peak 1-2 hours after oral administration of the labelled compound, at a dose of 10 mg/kg body weight. The blood kinetics pattern suggested an entero-hepatic cycle, which was demonstrated by i.v. administration of the compound at the same dose. The blood profiles for both administration routes, demonstrated that the bioavailability of the active principle was good. Urinary excretion was lower than faecal excretion after oral ingestion, and both were comparable after administration via the i.v. route. Moreover, excretion mainly occurred within the first 24 hours following administration. When hesperidin methylchalcone was given in a therapeutic, pharmaceutical formulation, its bioavailability was greatly improved. (This was not due to the alcoholic ingredient in the formula).
使用14C标记法在大鼠中研究了橙皮苷甲基查耳酮的吸收和排泄情况。以10mg/kg体重的剂量口服给予标记化合物后,血液中的放射性水平在1-2小时达到峰值。血液动力学模式表明存在肠肝循环,静脉注射相同剂量的化合物也证实了这一点。两种给药途径的血液曲线表明活性成分的生物利用度良好。口服摄入后尿排泄低于粪便排泄,静脉给药后两者相当。此外,排泄主要发生在给药后的头24小时内。当以治疗性药物制剂形式给予橙皮苷甲基查耳酮时,其生物利用度大大提高。(这并非由于制剂中的酒精成分)