McDowall R D, Lee R M
J Chromatogr. 1983 Jul 8;275(2):377-85. doi: 10.1016/s0378-4347(00)84383-2.
A selective assay of a new histamine H2-receptor antagonist, SK&F 93479, in human plasma has been developed. The method uses liquid-liquid extraction from the biological sample and analysis of the resulting extract by normal-phase high-performance liquid chromatography with UV detection for quantitation of the drug and an added standard. The assay is sufficiently accurate and precise to determine the compound at concentrations as low as 0.025 mg 1(-1). The coefficient of variation of the assay averages 5.7% at concentrations between 0.1 and 2.0 mg 1(-1), but increases to 21.8% at 0.02 mg 1(-1). SK&F 93479 can be determined in spiked plasma samples, at concentrations between 0.05 and 0.80 mg 1(-1) with a bias of between -7.5 and +3.6%, but at 0.02 mg 1(-1) concentrations were underestimated by 15% on average. The assay has been used for pharmacokinetic and bioavailability studies: after a single 0.5 mg kg-1 oral dose in man, plasma concentrations can be monitored for up to 70 h after dosing.
已开发出一种用于检测人血浆中新型组胺H2受体拮抗剂SK&F 93479的选择性分析方法。该方法采用从生物样品中进行液液萃取，并通过正相高效液相色谱法对所得萃取物进行分析，利用紫外检测对药物和添加的标准品进行定量。该分析方法足够准确和精密，能够测定低至0.025 mg l⁻¹浓度的化合物。在浓度为0.1至2.0 mg l⁻¹之间时，该分析方法的变异系数平均为5.7%，但在0.02 mg l⁻¹时增加到21.8%。在加标血浆样品中，浓度在0.05至0.80 mg l⁻¹之间时，可以测定SK&F 93479，偏差在-7.5%至+3.6%之间，但在0.02 mg l⁻¹浓度时，平均低估了15%。该分析方法已用于药代动力学和生物利用度研究：在人体单次口服0.5 mg kg⁻¹剂量后，给药后长达70小时内可监测血浆浓度。
