RP-HPLC法测定盐酸伪麻黄碱的血药浓度及人体药动学研究

目的：建立高效液相色谱法测定盐酸伪麻黄碱（PSE）血药浓度的方法，研究洛芬伪麻片的人体药动学。方法：8名健康男性受试者单剂量口服洛芬伪麻片（含盐酸伪麻黄碱30mg）后，采用高效液相色谱法测定血浆中盐酸伪麻黄碱的浓度，色谱柱：Diamonsil^TM C18柱（250mm×4．6mm，5μm），流动相：甲醇-0．02mol·L^-1磷酸二氢钠（舍0．005mol·L^-1辛烷磺酸钠，磷酸调pH3．8）（45：55）；流速：1mL·min^-1；检测波长210nm。结果：线性范围20-1000ng·mL^-1（r=0．9998），最低检测限为1．2ng，日内精密度（RSD）小于3．26％，日间精密度（RSD）小于4．89％，绝对回收率为75．76％～86．52％，PSE的主要药动学参数为：AUC0-∞为（1．83±0．60）μg·h·mL^-1，Cmax为（279．52±92．46）ng·mL^-1，tmax为（1．32±0．24）h，t1/2为（5．37±0．92）h。结论：本方法简便、快速、准确，可用于盐酸伪麻黄碱的血药浓度测定及药代动力学研究。

Determination of Pseudoephedrine Hydrochloride in Human Plasma by RP-HPLC and Study of Human Pharmacokinetics

Objective： To develop a RP-HPLC method to determine pseudoephedrine hydrochloride （PSE） in human plasma, and to examine the pharmaeokinetic characteristics of the compound ibuprofen tablets in human. Methods： The compound ibuprofen tablets （contains 30 mg PSE） of single doses were orally administrated to 8 healthy Chinese male volunteers. The plasma concentrations of PSE were determined by RP-HPLC with Diamonsil^TM C18 column （250 mm × 4.6 mm, 5μm）. The mobile phase consisted of mathanol-0.02 mol·L^-1 sodium dihydrogen phosphate （contains 0.005 mol·L^-1 octane sulfonic sodium, adjust to pH 3.8 with phosphoric acid, 45 ： 55） at the flow rate of 1 mL ·min^-1, and the detection wavelength was 210 nm. the main pharmacokinetic parameters were analysed by 3P97 program. Results： The calibration curve was linear in the range of 20 - 1 000 ng·mL^-1 （ r = 0.999 8）. The lower detection limit was 1.2 ng. The inter-day and intra-day RSD were less than 3.26% and 4.89%, respectively. The methodology recovery was 75.76% - 86.52%. The main pharmacokinetic parameters of PSE were as follows： AUC0-∞ was （1.83 ± 0.60）μg · h · mL^-1, Cmax was （279.52± 92.46） ng · mL^-1, tmax was （1.32 ± 0.24） h,t1/2 was （5.37 ± 0.92） h. Conclusion： The established HPLC method is simple, specific, accurate, sensitive and applicable for pharmacokinetics study of PES.