[Pharmacokinetics of moracizine and moracizine sulfoxide in healthy volunteers].
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.
Guo
W Y
WY
Laboratory of Clinical Pharmacology, Zhong Shan Hospital, Shanghai Medical University, China.
Zhu
J R
JR
Li
Z S
ZS
Jiang
W D
WD
Yang
J M
JM
D000328:Adult; D000368:Aged; D001145:Arrhythmias, Cardiac / Q000188:drug therapy / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D016293:Moricizine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000627:therapeutic use
D016293:Moricizine; C076194:moricizine sulfoxide