Moriyama M, Furuno K, Oishi R, Gomita Y
Department of Hospital Pharmacy, Okayama University Medical School, Japan.
J Pharm Sci. 1994 Dec;83(12):1751-3. doi: 10.1002/jps.2600831220.
Primidone (PRM) and its active metabolites, phenylethylmalonamide (PEMA) and phenobarbital (PB), in rat plasma were simultaneously determined using a solid-phase extraction technique followed by high-performance liquid chromatography (HPLC). Twenty microliters of plasma was applied to a Bond-Elut C-18 cartridge column with 0.1 microgram of acetanilide (internal standard, IS). After the column was washed, PRM, PEMA, PB, and IS were eluted with methanol and injected into the HPLC system. Calibrations for these substances were linear in the range of 0-20 micrograms/mL. The coefficients of variation were 1.5-7.9% and 3.4-9.1% in the within-day and between-day assays, respectively. The recovery rates were 96.8-101.8%. The pharmacokinetics of these substances were examined after oral administration of PRM (50 mg/kg) to rats. The Tmax values for PRM, PEMA, and PB were 1.4, 5.7, and 6.6 h, respectively, and the Cmax values were 18.2, 8.1, and 9.6 micrograms/mL, respectively. This method is useful for pharmacokinetic studies of PRM and its active metabolites.
采用固相萃取技术结合高效液相色谱法（HPLC）同时测定大鼠血浆中的扑米酮（PRM）及其活性代谢物苯乙基丙二酰胺（PEMA）和苯巴比妥（PB）。将20微升血浆加至含有0.1微克乙酰苯胺（内标，IS）的Bond-Elut C-18柱上。柱清洗后，用甲醇洗脱PRM、PEMA、PB和IS，并注入HPLC系统。这些物质的校准曲线在0-20微克/毫升范围内呈线性。日内和日间测定的变异系数分别为1.5-7.9%和3.4-9.1%。回收率为96.8-101.8%。给大鼠口服PRM（50毫克/千克）后，研究了这些物质的药代动力学。PRM、PEMA和PB的Tmax值分别为1.4、5.7和6.6小时，Cmax值分别为18.2、8.1和9.6微克/毫升。该方法可用于PRM及其活性代谢物的药代动力学研究。
