文爱东 吴寅 杨春娥 杨志福 王莉 王志睿 周伦 (第四军医大学西京医院药剂科 西安 710032)
摘 要 目的：建立测定人血浆中地奥司明苷元浓度的液相色谱-串连质谱检测法，并研究地奥司明片在健康人体内的药物动力学特征。方法：用LC/MS/MS法测定，色谱柱为CAPCELL PAK UG120柱，流动相为乙腈-0.1％甲酸溶液（80∶20，v/v），流速0.6 ml•min-1，柱温为24 ℃，对12名健康志愿者口服地奥司明片后不同时间点的血药浓度进行测定，并用统计矩法计算药动学参数。结果：地奥司明片中地奥司明苷元在健康受试者体内的主要药动学参数tmax为（12.1±0.9）h，Cmax为（8.88±2.69）ng•ml-1，t1/2为（11.9±2.5）h，AUC0-48 h为（183±55 ）ng•h•ml-1，AUC0-∞为（200±61）ng•h•ml-1。结论：本方法具有良好的准确性、精密度和较高的灵敏度、简便快速，能满足地奥司明的血药浓度测定和药动学研究。
关键词 地奥司明；地奥司明苷元；药物动力学；液相色谱-串连质谱法
中图分类号：R969.1
文献标识码：A
文章编号：1008-049X(2007)07-0632-03
Pharmacokinetics of Diosmin Tablets in Healthy Human Volunteers
Wen Aidong，Wu Yin，Yang Chune，Yang Zhifu，Wang Li，Wang Zhirui，Zhou Lun (Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, Xi'an 710032, China)
ABSTRACT Objective: To establish a LC-MS/MS assay for determining diosmin aglycone in human plasma and to study the pharmacokinetic characteristics of diosmin tablets in healthy volunteers.Method: The plasma concentrations of diosmin tablets in 12 healthy volunteers were determined by LCMSMS. A CAPCELL PAK UG120 column was used, with the mobile phase consisted of acetonitrile0.1% methanoic acid (80:20, v/v) and flow rate was 0.6 ml•min-1. The temperature of column was set at 24 ℃. The concentratins of diosmin aglycone in plasma at different time points after oral administration in 12 healthy volunteers were monitored and then the pharmacokinetics parameters were calculated by statistical moment.Result: The main pharmacokinetics parameters of diosmin tablets are as follows:tmax(12.1±0.9) h, Cmax(8.88±2.69) ng•ml-1,t1/2 (11.9±2.5) h, AUC0-48 h(183±55)ng•h•ml-1,AUC0-∞(200±61) ng•h•ml-1.Conclusion: The method reported here is accurate, sensitive, simple and rapid, and may be used for blood concentration monitoring and pharmacokinetic study.
KEY WORDS Diosmin; Diosmin aglycone; Pharmacokinetics; LC-MS/MS
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