Andreasen F, Christensen C K, Jakobsen F K, Mogensen C E
Acta Pharmacol Toxicol (Copenh). 1981 Sep;49(3):223-9. doi: 10.1111/j.1600-0773.1981.tb00897.x.
Three principles for the use of HPLC with spectrophotometric detection to determine the concentration of furosemide and of 4-chloro-5-sulfamoyl anthranilic acid (CSA) were studied. A reversed phase microbondapack C18 column was used for the separation of either unchanged furosemide (I), CSA (II) or the diazo product of CSA (III). The sensitivity of the methods for the determination of furosemide added to serum in vitro were for I 0.05, for II 0.020 and for III 0.01 microgram/ml. The methods I and II were used to study the excretion pattern in the urine of furosemide and CSA after intravenous injection of 80 mg to 10 normal subjects. An average of 48.1 +/- 9.8% (S.D.) of the furosemide was excreted during the first hour as unchanged furosemide. Simultaneously 1.9 +/- 0.8% of the dose was excreted as CSA. Only very low concentrations of CSA were found in serum and that metabolite apparently was excreted with a higher renal clearance than furosemide during the period 30-60 min. after the administration (30.3 +/- 145 ml/min. for CSA and 88 +/- 23 ml/min. for furosemide). During the 24 hour period following the administration 52.6 +/- 8.1 mg was excreted as unchanged furosemide and 11.4 +/- 5.2 mg as a glucuronidated product.
研究了使用高效液相色谱-分光光度检测法测定呋塞米和4-氯-5-氨磺酰基邻氨基苯甲酸(CSA)浓度的三项原则。使用反相微径键合硅胶C18柱分离未变化的呋塞米(I)、CSA(II)或CSA的重氮产物(III)。体外测定血清中添加的呋塞米的方法灵敏度,对于I为0.05,对于II为0.020,对于III为0.01微克/毫升。方法I和II用于研究10名正常受试者静脉注射80毫克后呋塞米和CSA在尿液中的排泄模式。平均48.1±9.8%(标准差)的呋塞米在第一小时以未变化的呋塞米形式排泄。同时,1.9±0.8%的剂量以CSA形式排泄。在血清中仅发现极低浓度的CSA,并且在给药后30 - 60分钟期间,该代谢物的肾清除率明显高于呋塞米(CSA为30.3±145毫升/分钟,呋塞米为88±23毫升/分钟)。在给药后的24小时内,52.6±8.1毫克以未变化的呋塞米形式排泄,11.4±5.2毫克以葡萄糖醛酸化产物形式排泄。