HPLC法测定人血浆中阿伐斯汀的浓度及其药动学研究

Determination of Acrivastine in Human Plasma by HPLC and Its Pharmacokinetic Study

目的:建立以高效液相色谱法测定人血浆中阿伐斯汀浓度的方法,研究其在健康男性体内的药动学。方法:血浆样品经乙腈提取并浓缩后进样测定,外标法定量,色谱柱为Symmetry ShieldTM PR18,流动相为乙腈-2%三乙胺水溶液(用稀磷酸调节pH值至6.8±0.2)=25∶75,流速为1.0mL.min-1,柱温为35℃,紫外检测波长为250nm。结果:阿伐斯汀血药浓度在4.6875～600ng·mL-1范围内线性关系良好(r=0.9994);方法回收率为96.14%～98.89%,日内RSD=1.60%～3.00%,日间RSD=2.03%～6.98%;口服阿伐斯汀胶囊后的药-时数据符合一室药动学模型。结论:本方法简便、灵敏、准确、回收率高,适用于阿伐斯汀的血药浓度测定及临床药动学研究。

OBJECTIVE： To establish an HPLC method for the determination of acrivastine in human plasma and study its pharmaeokinetics in healthy male volunteers. METHODS： The plasma sample was extracted with acetonitriles and concentrated and quantified with external reference method on a Symmetry ShieldTMpR18 column. The mobile phase was a mixture of acetonitrile- 0.2% triethylamine （adjusted pH to 6.8± 0.2 by dilute phosphoric acid solution, 25 ： 75） at a flow rate of 1.0 mL · min^ -1. The column temperature was 35 ℃ . The detection wavelength was set at 250 nm. RESULTS： The linear range of acrivastine was 4. 687 5--600 ng · mL^-1（ r = 0.999 4） . The methodological recovery was 96.14%-98.89%; the intra- day RSD was 1.60%- 3.00% and interday RSD was 2.03%- 6.98%. The concentrationtime pharmacokinetic parameters after oral administration of acrivastine capsules were in line with the one - compartment mode. CONCLUSION ： The method is simple, sensitive, accurate with high recovery, and it is applicable for the concentration determination and clinical pharmacokinetic study of acrivastine.