Cova D, De Angelis L, Giavarini F, Palladini G, Perego R
Department of Pharmacology, CNR Center of Cytopharmacology, University of Milano, Italy.
Int J Clin Pharmacol Ther Toxicol. 1992 Jan;30(1):29-33.
Pharmacokinetic studies of diosmin were performed after an oral administration to healthy volunteers. Diosmin and its aglycone, diosmetin, were determined by HPLC and LC-MS techniques. At least, at the level of sensitivity of our method, no parent compound was present in the plasma but only its aglycone, diosmetin. Analysis of the pharmacokinetic parameters showed that the drug was rapidly absorbed. Diosmetin presents a long plasma elimination half-life ranging from 26 to 43 hours. Our data show the total absence of urinary elimination for both diosmin and its aglycone diosmetin, while its minor metabolites are eliminated in the urine, mainly as glucuronic acid conjugates. The presence of degradation products such as alkyl-phenolic acids confirms a metabolic pattern similar to other flavonoids.
在对健康志愿者口服给予地奥司明后进行了药代动力学研究。通过高效液相色谱法（HPLC）和液相色谱 - 质谱联用技术（LC-MS）测定地奥司明及其苷元香叶木素。至少，在我们方法的灵敏度水平上，血浆中不存在母体化合物，仅存在其苷元香叶木素。药代动力学参数分析表明该药物吸收迅速。香叶木素的血浆消除半衰期较长，范围为26至43小时。我们的数据表明地奥司明及其苷元香叶木素均完全没有经尿液排泄，而其少量代谢产物经尿液排泄，主要以葡萄糖醛酸共轭物形式存在。降解产物如烷基酚酸的存在证实了与其他黄酮类化合物相似的代谢模式。
