Róna K, Földes K, Gachályi B
Orvostovábbképzõ Egyetem I. Belgyógyászati Klinika, Budapest.
Acta Pharm Hung. 1990 Jul;60(4):156-61.
Since the biotransformation of paracetamol (Acetaminophen) is practically confined to conjugation, the quantitative determination of paracetamol excretion may provide important information on phase II of the drug metabolism. We elaborated a simple and rapid liquid chromatographic method for the assessment of paracetamol and its conjugated metabolites in the urine to be available for routine use in the clinicopharmacological laboratory. The persons involved in the trial were administrated 500 mg of paracetamol to be taken on an empty stomach in the morning. Subsequently, their urine was collected for 8 hours. The so-called free paracetamol of unchanged form excreted into the urine was measured from this 0 to 8 hours' urine fraction, then, after treating it with beta-glucuronidase/arysulphatase enzyme, the total amount of paracetamol released from the conjugate, as well as that of the existing free paracetamol, the so-called total paracetamol were determined. The urine extracts containing paracetamol obtained by ethylacetate, at pH 10, and dried under nitrogen stream were analysed by HPLC on an ODS column in an eluent of methanol and water mixture (3:7, v/v) in the presence of 3-acetaminophenol internal standard. The flow rate was 1 ml/min, the detection wavelength was 254 nm.
由于对乙酰氨基酚(扑热息痛)的生物转化实际上仅限于结合反应,因此对乙酰氨基酚排泄量的定量测定可为药物代谢的第二阶段提供重要信息。我们精心设计了一种简单快速的液相色谱法,用于评估尿液中的对乙酰氨基酚及其结合代谢物,以便在临床药理实验室常规使用。参与试验的人员在早晨空腹服用500毫克对乙酰氨基酚。随后,收集他们8小时的尿液。从0至8小时的尿液部分中测量排泄到尿液中的未变化形式的所谓游离对乙酰氨基酚,然后在用β-葡萄糖醛酸酶/芳基硫酸酯酶处理后,测定从结合物中释放的对乙酰氨基酚总量以及现有的游离对乙酰氨基酚总量,即所谓的总对乙酰氨基酚。通过乙酸乙酯在pH 10条件下获得的含有对乙酰氨基酚的尿液提取物,在氮气流下干燥后,在3-乙酰氨基酚内标存在的情况下,于甲醇和水混合物(3:7,v/v)的洗脱液中,在ODS柱上通过HPLC进行分析。流速为1毫升/分钟,检测波长为254纳米。