Guo W Y, Zhu J R, Li Z S, Jiang W D, Yang J M
Laboratory of Clinical Pharmacology, Zhong Shan Hospital, Shanghai Medical University, China.
Zhongguo Yao Li Xue Bao. 1993 Sep;14(5):433-6.
The pharmacokinetics of moracizine (Mor) and moracizine sulfoxide (Mor-SO) determined by reversed phase HPLC was reported. The data in 6 volunteers after a single oral dose (600 mg) showed an one-compartment open model. The peak concentration in plasma (2.1 +/- 0.4 micrograms.ml-1) of Mor reached within 1-2 h. The Mor-SO concentration in plasma was much lower (0.19 +/- 0.06 micrograms.ml-1) than that of Mor, but its elimination T1/2 (2.3 +/- 1.0 h) was similar to that of Mor (1.5 +/- 1.0 h). The recoveries of Mor, Mor-SO, moracizine sulfone (Mor-SO2) in urine within 48 h were 0.07%, 0.25%, and 0.06% of the total dose, respectively. The Mor and Mor-SO concentration ranges in plasma for 9 arrhythmic patients after 2-wk therapeutic trial were 0.09 +/- 0.07 to 0.9 +/- 0.5 microgram.ml-1 and 0.040 +/- 0.023 to 0.15 +/- 0.06 micrograms.ml-1, respectively. These results suggested that cumulative doses would not result in accumulation of the drug and the anti-arrhythmic effect of Mor-SO might not be realized.
报道了采用反相高效液相色谱法测定的莫雷西嗪（Mor）和莫雷西嗪亚砜（Mor-SO）的药代动力学。6名志愿者单次口服剂量（600mg）后的数据显示为一室开放模型。Mor的血浆峰浓度（2.1±0.4μg.ml-1）在1-2小时内达到。血浆中Mor-SO的浓度（0.19±0.06μg.ml-1）远低于Mor，但其消除半衰期（2.3±1.0小时）与Mor（1.5±1.0小时）相似。48小时内尿液中Mor、Mor-SO、莫雷西嗪砜（Mor-SO2）的回收率分别为总剂量的0.07%、0.25%和0.06%。9名心律失常患者经过2周治疗试验后血浆中Mor和Mor-SO的浓度范围分别为0.09±0.07至0.9±0.5μg.ml-1和0.040±0.023至0.15±0.06μg.ml-1。这些结果表明，累积剂量不会导致药物蓄积，且Mor-SO的抗心律失常作用可能无法实现。
