Chérié Lignière G, Montagnani G, Alberici M, Acerbi D
Arzneimittelforschung. 1987 May;37(5):560-3.
Piroxicam pivalic ester (CHF 10/21) is a prodrug of piroxicam and is characterized by a reduced gastric irritant activity. Plasma and synovial fluid samples were simultaneously taken from 7 patients with mono- or poly-articular arthritis causing knee effusion, during 4 weeks of treatment with CHF 10/21 at the dose of 30 mg/day. The time courses of plasma levels of both the prodrug and the active principle were studied and a correlation of the latter with synovial fluid levels was made. After 14 days of treatment the steady-state was reached in the systemic (plasma) and peripheral (synovial fluid) compartments with therapeutically active drug levels. Clinical results were good and a complete disappearance of local pain occurred in 2 cases. Good gastric tolerance was also achieved.
吡罗昔康特戊酸酯(CHF 10/21)是吡罗昔康的前体药物,其特点是胃刺激性活性降低。在7例因单关节或多关节关节炎导致膝关节积液的患者中,以30毫克/天的剂量用CHF 10/21治疗4周期间,同时采集血浆和滑液样本。研究了前体药物和活性成分的血浆水平随时间的变化过程,并将后者与滑液水平进行了相关性分析。治疗14天后,全身(血浆)和外周(滑液)腔室达到稳态,药物水平具有治疗活性。临床结果良好,2例局部疼痛完全消失。还实现了良好的胃耐受性。