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已报告,在健康志愿者服用单剂量控制释放(CR)处方或速溶(IR)片剂后和静注维拉帕米以后,维拉帕米影响传导作用(PR-间隔延长)的不同浓度/作用曲线。CR处方的绝对生物利用度与IR处方相比约增加30％,大概由于首过代谢的饱和之故。可是应用CR处方后维拉帕米的效价降低,如和IR处方比较,浓度/作用曲线2倍右移和假定高活性异构体(eutomer)在较慢药物输入速率条件下有较大首过提取。在上述研究中,对于外消旋(R、S)维拉帕米的对映体的选择性分析不能应用常规分析,所有计算基于外消旋维拉帕米的血浆浓度。本研究应用对映体选择性HPLC法,手性固定相和荧光测定。维拉帕米血浆样品的对
It has been reported that verapamil affects the effect of different concentrations of conduction (prolonged PR-intervals) on verapamil following healthy volunteers taking single-dose controlled-release (CR) or instant (IR) tablets and intravenous verapamil, Function curve. The absolute bioavailability of CR prescriptions was approximately 30% higher than that of IR prescriptions, probably due to the first-pass metabolism saturation. However, the potency of verapamil was reduced with CR prescribing, with a 2-fold shift in the concentration / response curve as compared to IR prescribing and the assumption that the higher active eutomer had larger heads at slower drug input rates Extract. In the above studies, the conventional analysis was not applied to the selective analysis of racemic (R, S) verapamil enantiomers, all calculations based on the plasma concentration of racemic verapamil. In this study, enantioselective HPLC, chiral stationary phase and fluorescence were used. Verapamil plasma sample pairs