摘要
建立了盐酸氟桂嗪的ＨＰＬＣ测定法。血浆样品碱化后用正已烷提取，以ＭｉｃｒｏＰａｃＭＣＨ－５为固定相，６５％甲醇，３５％水（含０．０２ｍｏｌ／Ｌ四丁基溴化铵，ｐＨ３．０）为流动相，紫外检测波长２５４ｎｍ。最低检出浓度为５．０ｎｇ／ｍｌ，线性范围１０．０～２００．０ｎｇ／ｍｌ（ｒ＝０．９９９８，ｎ＝６），平均回收率为（９７．５５±２．６８）％（ＲＳＤ２．１３％。用本法测定了８名健康男性志愿者分别服用杨森产盐酸氟桂嗪胶囊和新昌产盐酸氟桂嗪片剂的血药浓度。结果表明，其血药浓度－时间曲线均符合一房室模型。新昌产盐酸氟桂嗪片的主要药代动力学参数Ｔ１／２Ｋａ＝（０．７７±０．１１）ｈ，Ｔ１／２Ｋｅ＝（５．０７±０．５２）ｈ，Ｔｍａｘ＝（２．７９±０．２４）ｈ，Ｃｍａｘ＝（９５．００±４．５２）ｎｇ／ｍｌ，ＡＵＣ＝（９９７．６±６２．５）ｎｇ·ｈ／ｍｌ，相对生物利用度为９６．４％。
An ion-pair reversed phase HPLC method was established for determination of flunarizine in human plasma. The drug was extracted from alkalized plasma into n-hexane.A MicroPaK MCH-5 column(300 mm×4 mm ID,10μm) was used.the mobile phase consisted of 65%methanol and 35% water containing 0.02 mol/L tetrabutylammonium bromide(adjusted to pH 3.0 with phosphoric acid).The eluted peaks were detected by UV-absorption at 225 nm,The average recovery of the drug from plasma was (97.55±2.08)%with RSD D 2.13% and the minimum detection concentration in plasma was 5 ng/ml.The standard curve was linear over the range of 1 0.0～200.0 ng/ml(r=0.9998).The pharmacokinetic behaviors of flunarlzine for two formulations(tablet and capsule) werestudied in 8 healthy male volunteers after an oral dOse of 20 mg.The concentration-time data of flunarizine in the subjects were better fitted to one-compartmental medel.The pharmacokinetic parameters were estimated as follows.Tablet,T1/2(Ke)=(5.07±0.52)h,Tmax=(2.79±0.24)h,Cmax=(95.00±4.52)ng/ml,and AUC=(997.6±62.5) ng·h/ml;capsule,T1/2(Ke)=(4.82±0.36)h,Tmax=(2.78±0.30)h,Cmax=(97.94±5.72)ng/ml,and AUC=(1036.0±50.4)ng·h/ml.Relative bioavailabillty of tablet was 96.4%as compared with capsule.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1995年第5期300-303,共4页
Journal of China Pharmaceutical University
