Kamp J, Loew D, Barkow D, Deister J, Schuster O, Knoell H E
Z Rheumatol. 1984 Jul-Aug;43(4):179-81.
The kinetics of mofebutazone in the plasma and in the synovial fluid was investigated in a pharmacokinetic study. To this purpose 7 volunteers and 36 patients were injected with one ampule Mofesal (650 mg mofebutazone sodium) i.m. The determination of mofebutazone in the plasma and in the synovial fluid was carried out by means of high performance liquid chromatography. The kinetics in the plasma and in the synovial fluid showed a dissociated course of development. Maximum concentrations of the active substance were reached after 1.4h in the plasma and after approx. 2 h in the synovial fluid. While mofebutazone in the plasma is eliminated with a half life time of 1.9 h, the half life time in the synovial fluid amounted to 7.7 h. According to pharmacokinetic simulation calculations no accumulation in the plasma occurred even after the administration of 1 ampule Mofesal three times daily, on the other hand a steady state is presumably reached in the synovia after 4-5 injections. On the basis of this study we regard it once again as essential that the kinetics in the synovial fluid should without doubt be preferred to the kinetics in the plasma for the calculation of a dosage schedule for non-steroidal antiphlogistics.
在一项药代动力学研究中，对莫苯丁酮在血浆和滑液中的动力学进行了研究。为此，给7名志愿者和36名患者肌肉注射了1安瓿莫非沙（650毫克莫苯丁酮钠）。采用高效液相色谱法测定血浆和滑液中的莫苯丁酮。血浆和滑液中的动力学呈现出不同的发展过程。活性物质的最高浓度在血浆中于1.4小时后达到，在滑液中约在2小时后达到。血浆中的莫苯丁酮消除半衰期为1.9小时，而滑液中的半衰期为7.7小时。根据药代动力学模拟计算，即使每天三次注射1安瓿莫非沙，血浆中也不会发生蓄积，另一方面，在滑膜中大概在4 - 5次注射后达到稳态。基于这项研究，我们再次认为，在计算非甾体抗炎药的给药方案时，毫无疑问应以滑液中的动力学而非血浆中的动力学为准。
