Drummer O H, Worland P J, Jarrott B
Biochem Pharmacol. 1983 May 15;32(10):1563-8. doi: 10.1016/0006-2952(83)90328-3.
The tissue distribution of captopril, an antihypertensive drug possessing a free sulfhydryl group, and its sulfur-conjugated metabolites was studied in rats by gas chromatography-mass spectrometry at 15, 30 and 60 min following a single 10 mg/kg oral dose of captopril. It was found that tissue accumulation of captopril was rapid with both free and oxidized-forms already present at 15 min post-dose. A maximum concentration of captopril was achieved at 30 min in tissues studied, being substantially higher in kidney (14.2 micrograms/g), with lesser amounts occurring in liver, lung, heart, blood cells, spleen and plasma in that order. Oxidized disulfide forms of captopril were usually present in the same or slightly higher proportion than free captopril except for liver which only contained detectable disulfides at 15 min after oral dosing. S-methylcaptopril was also present at 30 min in all tissues examined with highest levels occurring in liver and kidney (1.05 micrograms/g) followed by plasma, lung, heart, spleen and blood cells.
采用气相色谱-质谱联用技术，在大鼠单次口服10mg/kg卡托普利后15、30和60分钟，研究了具有游离巯基的抗高血压药物卡托普利及其硫结合代谢物的组织分布。结果发现，卡托普利在组织中的蓄积迅速，给药后15分钟时游离型和氧化型均已存在。在所研究的组织中，卡托普利在30分钟时达到最高浓度，肾脏中浓度最高（14.2微克/克），其次是肝脏、肺、心脏、血细胞、脾脏和血浆，浓度依次降低。除肝脏外，卡托普利的氧化二硫形式通常以与游离卡托普利相同或略高的比例存在，肝脏在口服给药后15分钟仅含有可检测到的二硫化物。在给药30分钟时，所有检测组织中均存在S-甲基卡托普利，肝脏和肾脏中含量最高（1.05微克/克），其次是血浆、肺、心脏、脾脏和血细胞。
