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建立维拉帕米的反相高效液相色谱分析方法,并对其大鼠体内过程特性进行分析研完。方法:生物样品在碱性条件下经过正已烷一乙醚(30:70)提取,用Kromasil C_(18)反相柱(150mm×4.6mm,5μm),甲醇-水-三乙胺(70:30:0.1)为流动相,流速1.0mL.min~(-1),荧光检测波长为λ_(ex)275nm和λ_(ex)315nm。结果:方法回收率为92.3％～104.8％,测定血药浓度线性范围为8.5～85ng.mL~(-1)(r=0.9992),最低检测限0.6ng.ml~-。SD大鼠一次性灌胃盐酸维拉帕米片后血浆C-t曲线呈二室开放模型,达峰时间为(0.28±0.1)h。给药1.25h时,在主要的效应器官的浓度分布特点是:C_心>C_(大脑)>C_(小脑),在主要消除器官的浓度分布特点是:C_肝>C_肾>C_脾。结论:本法准确,灵敏度较高,可用于维拉帕米的体内过程研究。维拉帕米的肝首过效应应引起重视,主要由肾脏排泄。
The established RP-HPLC method of verapamil was used to analyze the process characteristics of rat in vivo. Methods: The biological samples were extracted with n-hexane (30:70) under alkaline conditions and eluted with Kromasil C 18 reverse phase column (150 mm × 4.6 mm, 5 μm), methanol-water- 30: 0.1) was used as the mobile phase at a flow rate of 1.0 mL · min ~ (-1). The detection wavelength was λ_ (ex) 275 nm and λ_ (ex) 315 nm. Results: The recoveries were 92.3% -104.8%. The linear range was 8.5 ~ 85 ng.mL ~ (-1) (r = 0.9992). The lowest detection limit was 0.6ng.ml ~ -. After a single oral dose of verapamil hydrochloride in SD rats, the plasma C-t curve showed a two-compartment open model with a peak time of (0.28 ± 0.1) h. At 1.25h, the concentration profiles in the main effector organs were characterized by: C_center> C_ (brain)> C_ (cerebellum), the concentration distribution in the main elimination organs characterized by: C_ liver> C_renal> C _spleen. Conclusion: This method is accurate and sensitive and can be used for in vivo process study of verapamil. Verapamil liver first pass effect should be taken seriously, mainly by the kidneys excretion.