Derendorf H, Möllmann H, Voortman G, van den Ouweland F A, van de Putte L B, Gevers G, Dequeker J, van Vliet-Daskalopoulou E
Department of Pharmaceutics, University of Florida, Gainesville 32610.
J Clin Pharmacol. 1990 May;30(5):476-9. doi: 10.1002/j.1552-4604.1990.tb03488.x.
The pharmacokinetics of rimexolone were investigated after intra-articular injection into the knee joints of patients with rheumatoid arthritis. After a single dose of 40 mg rimexolone the drug could be detected in plasma over 3 months. The suspension dissolves in the synovia very slowly and provides a sustained release of the steroid in the joint. Pharmacokinetic analysis was performed on the assumption that the disposition of rimexolone after intra-articular administration is absorption limited ("flip-flop-case"). Dose linearity was studied in a range from 40 to 200 mg. Total body clearance averaged 106 L/h and was independent of dose. The mean residence time of rimexolone in the knee joint is very long and averaged 25 days. It could be shown that the mean residence time of different glucocorticoids correlates well with the duration of their clinical effectiveness.
对类风湿性关节炎患者膝关节进行关节腔内注射后，研究了利美索龙的药代动力学。单次注射40mg利美索龙后，血浆中可在3个月内检测到该药物。该混悬液在滑液中溶解非常缓慢，可在关节内实现类固醇的缓释。药代动力学分析基于关节腔内给药后利美索龙的处置受吸收限制（“翻转情况”）这一假设进行。在40至200mg范围内研究了剂量线性。总体清除率平均为106L/h，且与剂量无关。利美索龙在膝关节中的平均驻留时间非常长，平均为25天。结果表明，不同糖皮质激素的平均驻留时间与其临床疗效持续时间密切相关。
