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Pharmacokinetic profiles of hydroxysafflor yellow A following intravenous administration of its pure preparations in healthy Chinese volunteers

作者 Li, Chang-Yin; Yin, Jun-Gang; Zhang, Jun; Wang, Xiao-Xiao; Xu, Mei-Juan; Liu, Fang; Zou, Jian-Dong; Ju, Wen-Zheng

期刊 JOURNAL OF ETHNOPHARMACOLOGY , MAR 13 2015,:162

DOI 10.1016/j.jep.2014.12.068 PubMed 25576896

摘要 Ethnopharmacological relevance: Hydroxysaffior yellow A (HSYA), the major active marker compound isolated from Carthamus tinctorius L, has been demonstrated to possess various attractive pharmacological activities. However, there is a lack of information about the complete clinical pharmacokinetic profiles of HSYA following the administration of its pure preparations. The purpose of this study was to fully characterize the pharmacokinetic (PK) properties of HSYA in healthy Chinese volunteers following drip intravenous infusion of injectable powder of pure HSYA (IPPH), a new drug recently approved for the phase I clinical study by China Food and Drug Administration.Materials and methods: 36 healthy subjects of either sex were recruited in this single-center, and open-label, single doses (25, 50, and 75 mg) and multiple doses (50 mg, once daily, 7 consecutive days) study. Plasma samples were analyzed with a validated LC-MS/MS method. Various PK parameters were estimated from the plasma concentration versus time data using non-compartmental methods.Results: After single dose administration of IPPH, the values of AUC(0-t), AUC(0-infinity). and C-max for HSYA were statistically proportional over the dose range of 25-75 mg. After 7 repeated doses of 50 mg IPPH, both C-max. and AUC(0-infinity), were significantly decreased, from 3207 to 2959 mu g L-1, and from 12,811 to 12,135 mu g h L-1 respectively, while t(1/2) was significantly prolonged from 3.912 to 4.414 h. The minimum plasma concentrations on day 5, 6 and 7 showed good stability with no significant difference. Both Cmax and AUC of HSYA in male volunteers were generally lower than that in females. IPPH was generally well tolerated in healthy volunteers by either single or multiple dosing.Conclusion: HSYA displayed moderately linear PK properties over the doses ranging from 25 to 75 mg of IPPH. Repeated administration of IPPH once daily could not lead to the in-vivo drug accumulation, but significantly affect PK behavior of HSYA. Gender difference should be considered for dosage recommendation in the clinic. (C) 2015 Elsevier Ireland Ltd. All rights reserved.

涉及物种 红花 Carthamus tinctorius