Kripalani K J, Cohen A I, Weliky I, Schreiber E C
J Pharm Sci. 1975 Aug;64(8):1351-9. doi: 10.1002/jps.2600640820.
The absorption, distribution and metabolic fate of triamcinolone acetonide-14C-21-phosphate were studied in the dog, monkey, and rat. A comparison of levels of radioactivity in blood or plasma, reached after intramuscular or intravenous administration, indicated that the drug was completely absorbed from the site of intramuscular injection within 10-15 min in all three species. Within 1-5 min after intramuscular or intravenous administration, the 21-phosphate ester was completely hydrolyzed to triamcinolone acetonide, which was present in the blood. The radioactivity was eliminated rapidly (t1/2 = 1-2 hr) from plasma (dogs, monkeys, and rats) and tissues (rats) after intramuscular or intravenous administration. In the three species, the major route of excretion was via the bile; however, the ratio of biliary to urinary excretion among the species varied considerably (from 1.5 to 15). In rats, excretion of radioactivity as expired carbon dioxide accounted for only 2-3 percent of the dose. 6beta-Hydroxytriamcinolone acetonide was the major metabolite in urine of the three species. Hydrolytic cleavage of the acetonide group did not appear to be significant.
研究了磷酸曲安奈德 -14C -21 在犬、猴和大鼠体内的吸收、分布及代谢情况。比较肌肉注射或静脉注射后血液或血浆中的放射性水平表明，在所有这三个物种中，该药物在 10 - 15 分钟内从肌肉注射部位完全吸收。在肌肉注射或静脉注射后 1 - 5 分钟内，21 - 磷酸酯完全水解为曲安奈德，其存在于血液中。肌肉注射或静脉注射后，放射性物质从血浆（犬、猴和大鼠）和组织（大鼠）中迅速消除（t1/2 = 1 - 2 小时）。在这三个物种中，主要排泄途径是通过胆汁；然而，不同物种之间胆汁排泄与尿液排泄的比例差异很大（从 1.5 到 15）。在大鼠中，作为呼出二氧化碳的放射性排泄仅占剂量的 2 - 3%。6β - 羟基曲安奈德是这三个物种尿液中的主要代谢产物。丙酮基团的水解裂解似乎并不显著。
