HPLC-荧光法测定盐酸文拉法辛胶囊的生物等效性

Determination of bioequiavailability of Venlafaxine hydrochloride capsule by HPLC with fluorescence detector

目的采用HPLC-荧光检测法测定盐酸文拉法辛胶囊的生物等效性。方法采用液-液萃取法处理血清样品,用Hypersil C18色谱柱,流动相为乙腈-pH6.8磷酸盐缓冲液-三乙胺(30:70:1,用磷酸调pH2.8);荧光检测器检测,激发和发射波长分别为276、598 nm,流速1.0 m.lmin-1。结果18名健康志愿者分别空腹po150 mg盐酸文拉法辛胶囊后,两种制剂在受试者体内的药动学参数Cmax分别为348.38±98.99、344.20±96.22μg.L-1;t1/2分别为5.079±1.322、5.046±1.503 h;AUC0-∞分别为2425.2±874.5、2431.1±819.1μg.h.L-1,受试制剂与参比制剂的相对生物利用度为99.94%±14.22%。结论所建方法灵敏、简便、快速、准确。两种制剂具有生物等效性。

OBJECTIVE An HPLC method with fluorescence detector for study of bioequiavailability of Venlafaxine hydrochloride capsule was established. METHODS The drug was extracted by liquid - 1 iquid extraction. The concentrations of Venlafaxine hydrochloride in the serum were determined by HPLC with C18 column and the mobile phase of acetonitrile - pH6.8 phosphate buffer solutiontriethylamine （30 ： 70 ： 1, regulating pH2.8 with H3 PO4 ） at the flow rate of 1.0 ml· min^ - 1. The excitation and emission wave lengths were set at 276 and 598 nm, respectively. RESULTS A dose of 150 mg Venlafaxine hydrochloride capsule was given to eighteen healthy volunteers. The main pharmacokinetic parameters of the test and reference capsules were as follows ： Cmax were 348.38 ± 98. 99.344.20 ± 96.22 μg· L^-1 ; t 1/2 were 5. 079 ± 1. 322,5. 046 ±1. 503 h; AUC0-∞ were 2425.2 ± 874.5,2431.1± 819.1 μg· h· L^-1 , respectively. And the relative bioavailability of the test capsule to the reference was 99.94% ± 14.22%. CONCLUSION The method is sensitive, simple, accurate and reproducible. The two capsules are bioequivalent.