Gordon S, Morrison J
Steroids. 1978 Jul-Aug;32(1):25-35. doi: 10.1016/0039-128x(78)90096-x.
The metabolic fate of 9-fluoro-11beta,16alpha,17,21-tetrahydroxy-1,4-pregnadiene-3,20-dione cyclic 16,17-acetal with 2(-14)C-acetone, triamcinolone acetonide (TA) was studied in rabbits, dogs, monkeys and rats and found to be qualitatively similar in all species. In the dog, rat and monkey the major excretory route was the feces irrespective of the mode of administration. In the rabbit the excreted radioactivity was equally distributed between urine and feces. The metabolites were isolated by preparative thin layer chromatography, located by autoradiography, eluted and analyzed by MS, IR, UV and NMR. The major metabolites of triamcinolone acetonide (TA) were identified as the C-21 carboxylic acids of TA and of the 6beta hydroxy-TA, (6BETA-OH-TA) and the previously identified (1,2) 6beta-OH-TA. In addition MS and UV data indicate the presence of 9-fluoro-11beta,16alpha, 17-trihydroxy-3,20-dioxo-1,4,6-pregnatrien-21-oic acid cyclic 16,17 acetal with 2(-14)C-acetone.
研究了9-氟-11β,16α,17,21-四羟基-1,4-孕二烯-3,20-二酮与2(-14)C-丙酮的环状16,17-缩醛（曲安奈德，TA）在兔、犬、猴和大鼠体内的代谢命运，发现其在所有物种中的代谢性质相似。在犬、大鼠和猴中，无论给药方式如何，主要排泄途径都是粪便。在兔中，排泄的放射性在尿液和粪便中均匀分布。通过制备型薄层色谱法分离代谢产物，通过放射自显影定位，洗脱后用质谱（MS）、红外光谱（IR）、紫外光谱（UV）和核磁共振（NMR）进行分析。曲安奈德（TA）的主要代谢产物被鉴定为TA和6β-羟基-TA（6BETA-OH-TA）的C-21羧酸以及先前鉴定的（1,2）6β-羟基-TA。此外，质谱和紫外光谱数据表明存在9-氟-11β,16α,17-三羟基-3,20-二氧代-1,4,6-孕三烯-21-酸与2(-14)C-丙酮的环状16,17-缩醛。
