Sinha A J, Shaw S R, Thornburgh B A
Eur J Drug Metab Pharmacokinet. 1985 Apr-Jun;10(2):171-7. doi: 10.1007/BF03189712.
A single dose of arbaprostil-11 beta-3H (4 micrograms/kg) was administered orally to male rats. A maximum plasma radioactivity concentration equivalent to 2.5 to 2.8 nanograms of the prostaglandin per ml was reached at 30 minutes and was maintained until 120 minutes after drug administration. The plasma drug disappearance half-life was 2.6 hours. These results along with data from tissue distribution studies suggested a rapid uptake of radiolabeled arbaprostil by the glandular stomach tissue followed by an apparent zero-order release of drug-related radioactivity from this tissue "reservoir" into the plasma. Drug-related radioactivity was excreted rapidly, with 96 to 99% of the urinary excretion and 82 to 97% of the fecal excretion being completed within 24 hours. A total of 49.6 +/- 3.5% of the orally administered dose was excreted in the urine and 46.7 +/- 3.9% in the feces. No radioactive residues were detected in the animals at the end of the 120 hour specimen collection period. The metabolic stability of the 11 beta-tritium label and the suitability of arbaprostil-3H for use in human studies was demonstrated.
给雄性大鼠口服单剂量的阿巴前列素 - 11β - 3H（4微克/千克）。给药30分钟时达到最大血浆放射性浓度，相当于每毫升2.5至2.8纳克前列腺素，并维持至给药后120分钟。血浆药物消除半衰期为2.6小时。这些结果以及组织分布研究的数据表明，腺胃组织迅速摄取放射性标记的阿巴前列素，随后药物相关放射性从该组织“储存库”以明显的零级释放进入血浆。药物相关放射性迅速排泄，96%至99%的尿排泄和82%至97%的粪便排泄在24小时内完成。口服剂量的49.6±3.5%经尿液排泄，46.7±3.9%经粪便排泄。在120小时标本采集期结束时，未在动物体内检测到放射性残留。证明了11β - 氚标记的代谢稳定性以及阿巴前列素 - 3H用于人体研究的适用性。
