Nieuwenhuyse H, Lewis A J
Arzneimittelforschung. 1980;30(10):1646-9.
The persistence and effects of 3H-labelled and intra-articularly administered 11 beta-hydroxy-16 alpha,17 alpha,21-trimethylpregna-1,4-diene-3,20-dione (rimexolone, [3H]-Org 6216 have been investigated in a model of fibrin-induced mono-articular arthritis in the rabbit. It appears that joint swelling is suppressed in a dose-dependent way when the drug is administered into the arthritic joint. With a dose of 15 mg the joint circumference was restored to the initial value recorded prior to antigen challenge within 14 days. Administration of rimexolone into the non-arthritic joint also suppressed contralateral arthritic joint swelling, but this effect was less pronounced and shorter lasting. Radioactivity from [3H]-rimexolone at doses of 5 or 15 mg disappears slowly from both non-arthritic and arthritic knee joints.
在兔纤维蛋白诱导的单关节关节炎模型中，研究了3H标记并经关节内给药的11β-羟基-16α,17α,21-三甲基孕甾-1,4-二烯-3,20-二酮（利美索龙，[3H]-Org 6216）的持久性和作用。当将该药物注入关节炎关节时，关节肿胀似乎以剂量依赖性方式受到抑制。给予15mg剂量时，关节周长在14天内恢复到抗原攻击前记录的初始值。将利美索龙注入非关节炎关节也可抑制对侧关节炎关节肿胀，但这种作用不太明显且持续时间较短。5mg或15mg剂量的[3H]-利美索龙的放射性在非关节炎和关节炎膝关节中均缓慢消失。
