Cantelli-Forti G, Maffei F, Hrelia P, Bugamelli F, Bernardi M, D'Intino P, Maranesi M, Raggi M A
Department of Pharmacology, University of Bologna, Italy.
Environ Health Perspect. 1994 Nov;102 Suppl 9(Suppl 9):65-8. doi: 10.1289/ehp.94102s965.
The effects of components of aqueous licorice root extract (LE) on the pharmacokinetics of glycyrrhizin (G) and glycyrrhetic acid (GA) were investigated in rats and humans. The aim of this work was to define the role of pharmacokinetics in G toxicity. In the procedure, G and GA were detected in biological fluids by means of recently improved HPLC methods. Significantly lower G and GA plasma levels were found in rats and humans treated with LE compared to the levels obtained with those in which G alone was administered. The pharmacokinetic curves showed significant differences in the areas under the plasma-time curve (AUC), Cmax, and Tmax parameters. The data obtained from urine samples are in agreement with the above results and confirm a reduced bioavailability of G present in LE compared to pure G. This should be attributed to the interaction during intestinal absorption between the G constituent and the several components in LE. The modified bioavailability could explain the various clinical adverse effects resulting from the chronic oral administration of G alone as opposed to LE.
研究了甘草根水提取物(LE)的成分对大鼠和人体中甘草酸(G)和甘草次酸(GA)药代动力学的影响。这项工作的目的是确定药代动力学在G毒性中的作用。在该实验过程中,通过最近改进的高效液相色谱法在生物体液中检测G和GA。与单独给予G的大鼠和人体相比,给予LE的大鼠和人体中G和GA的血浆水平显著降低。药代动力学曲线在血浆-时间曲线下面积(AUC)、Cmax和Tmax参数方面显示出显著差异。从尿液样本获得的数据与上述结果一致,并证实与纯G相比,LE中G的生物利用度降低。这应归因于G成分与LE中几种成分在肠道吸收过程中的相互作用。生物利用度的改变可以解释单独长期口服G与LE相比产生的各种临床不良反应。