title: Comparative Pharmacokinetics Study of Icariin and Icariside II in Rats.
abstract: To explore the pharmacokinetic properties of icariin (ICA) and icariside II (ICA II) following intragastric and intravenous administration in rats, a rapid and sensitive method by using ultra-performance liquid chromatography-tandem mass spectroscopy (UPLC-MS/MS) was developed and validated for the simultaneous quantification of ICA and ICA II in rat plasma. The quantification was performed by using multiple reaction monitoring of the transitions m/z 677.1/531.1 for ICA, 515.1/369.1 for ICA II and 463.1/301.1 for diosmetin-7-O-β-d-glucopyranoside (IS). The assay showed linearity over the concentration range of 1.03-1032 ng/mL, with correlation coefficients of 0.9983 and 0.9977. Intra- and inter-day precision and accuracy were within 15%. The lower limit of quantification for both ICA and ICA II was 1.03 ng/mL, respectively. The recovery of ICA and ICA II was more than 86.2%. The LC-MS/MS method has been successfully used in the pharmacokinetic studies of ICA and ICA II in rats. The results indicated that 91.2% of ICA was transformed into ICA II after oral administration by rats, whereas only 0.4% of ICA was transformed into ICA II after intravenous administration. A comparison of the pharmacokinetics of ICA and ICA II after oral administration revealed that the Cmax and AUC0-t of ICA II were 3.8 and 13.0 times higher, respectively, than those of ICA. However, after intravenous administration, the Cmax and AUC0-t of ICA II were about only 12.1% and 4.2% of those of ICA. These results suggest that ICA and ICA II have distinct pharmacokinetic properties, and the insights obtained facilitate future pharmacological action studies.
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. chengtaohx@126.com.
authors.forename: Tao
authors.initials: T
authors.lastname: Cheng
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. yongzhang11@163.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. zhangtongshutcm@hotmail.com.
authors.forename: Tong
authors.initials: T
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. yjll66@outlook.com.
authors.forename: Lu
authors.initials: L
authors.lastname: Lu
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. dingyue-2001@hotmail.com.
authors.forename: Yue
authors.initials: Y
authors.lastname: Ding
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. cmx_1@126.com.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002853:Chromatography, Liquid; D004365:Drugs, Chinese Herbal / Q000737:chemistry; D005419:Flavonoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007302:Insect Repellents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D010880:Piperidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry; D014018:Tissue Distribution
chemical_list: D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D007302:Insect Repellents; D010880:Piperidines; C060988:baohuoside I; C483506:picaridin
keywords: UPLC-MS/MS; icariin; icariside II; pharmacokinetic study