Erttmann R R, Damm K H
Arch Int Pharmacodyn Ther. 1976 Sep;223(1):96-106.
Probenecid-induced effects on bile flow and biliary excretion of exogenous compounds, e.g. 3H-ouabain were investigated on bile-fistula rats. Clearance measurements of 14C-mannitol under incresed doses of probenecid gave evidence that the drug acts at the canalicular site only. Biliary excretion of radioactivity after 14C-probenecid administration was found to be saturated at a dosage of 100 mg X kg-1. Probenecid exerts its choleretic effect by osmotic activity in a "bile acid-like" manner. This is confirmed by a close positive correlation between the excretion of radioactivity after treatment with 14C-probenecid and bile flow. The effects of probenecid on the biliary excretion of exogenous compounds, e.g. ouabain, imply beside choleresis also inhibitory effects on transport systems. As a result of both effects the biliary excretion of ouabain remains unchanged within a within a wide range of probenecid doses.
在胆瘘大鼠身上研究了丙磺舒对胆汁流量和外源性化合物（如3H-哇巴因）胆汁排泄的影响。在增加丙磺舒剂量的情况下对14C-甘露醇进行清除率测量，结果表明该药物仅作用于胆小管部位。给予14C-丙磺舒后，放射性物质的胆汁排泄在剂量为100mg·kg-1时达到饱和。丙磺舒通过渗透活性以“胆汁酸样”方式发挥其利胆作用。用14C-丙磺舒处理后放射性物质的排泄与胆汁流量之间密切的正相关证实了这一点。丙磺舒对外源性化合物（如哇巴因）胆汁排泄的影响，除了利胆作用外，还意味着对转运系统有抑制作用。由于这两种作用，在丙磺舒剂量的很大范围内，哇巴因的胆汁排泄保持不变。
