Dashman T, Witt C, Kuhn D, Gallo-Torres H E
Prostaglandins. 1987 Mar;33(3):419-29. doi: 10.1016/0090-6980(87)90023-2.
The profiles of biliary, fecal and urinary excretion of tritium labeled prostaglandins (PG's) of differing biological activity were investigated in the rat. The PG's (10 micrograms/kg: 2 to 50 microCi/rat, in 1 ml polyethylene glycol-400) were administered intragastrically. Excretion data were expressed as a percentage of the total administered radioactivity. For the orally administered PG's 11R-methyl-16R-fluoro-15R-hydroxy-9-oxoprosta-ci s-5-trans-13-dienoic acid and its methyl ester, excretion was equally divided between urine and feces. The fecal and urinary profile of excretion of 3H after prostacyclin (PGI2) was similar to that following administration of 11R, 16, 16-trimethyl-15R-hydroxy-9-oxoprosta-cis-5-trans-13-dienoic acid (trimoprostil), a PG with antisecretory-antiulcer potential. However, PGI2 was very poorly absorbed from the intestine, while the absorption of trimoprostil was very efficient. Biliary excretion, with little entero-porto-hepatic biliary circulation, was the main route of elimination of trimoprostil, thereby resulting in rapid elimination of drug-related products and diminishing the potential for systemic liability in the rat.
在大鼠中研究了具有不同生物活性的氚标记前列腺素（PG）的胆汁、粪便和尿液排泄情况。PG（10微克/千克：2至50微居里/大鼠，溶于1毫升聚乙二醇-400）经胃内给药。排泄数据以给药总放射性的百分比表示。对于口服给药的PG 11R-甲基-16R-氟-15R-羟基-9-氧代前列腺素-5-反式-13-二烯酸及其甲酯，尿液和粪便中的排泄量相等。前列环素（PGI2）给药后3H的粪便和尿液排泄情况与具有抗分泌-抗溃疡潜力的PG 11R、16、16-三甲基-15R-羟基-9-氧代前列腺素-5-反式-13-二烯酸（曲莫前列素）给药后的情况相似。然而，PGI2从肠道的吸收很差，而曲莫前列素的吸收非常有效。胆汁排泄是曲莫前列素的主要消除途径，肠-肝-胆循环很少，从而导致与药物相关的产物迅速消除，并降低了大鼠全身不良反应的可能性。
