Bolten W, Waldorf-Bolten E, Sarfert D, Lehmann W, Miehlke W
Rheumaklinik, Bad Rappenau.
Z Rheumatol. 1990 Nov-Dec;49(6):374-7.
Twelve patients with osteoarthrosis were locally treated with Felbinac Gel (biphenyl acetic acid (BPAA) 3%) three times daily for 14 days (five patients), 28 days (six patients) or 42 days (one patient) before elective knee joint surgery. BPAA plasma concentrations as of the seventh day of treatment were steady at between 423 and 1040 ng/ml. In surgery, synovial and tissue samples were taken to determine BPAA concentrations. Moderate and sometimes higher synovial BPAA levels in the treated knee joint compared to the contralateral knee seem to indicate a combined direct and systemic absorption. The highest BPAA concentrations (1497-13939 ng/g) were measured in the skin. Drug levels in the synovial membrane (36-994 ng/g), the synovia (104-768 ng/ml), tendon (less than 10-197 ng/g), cartilage (less than 10-109 ng/g), muscle (12-101 ng/g), and subcutis (16-97 ng/g) were lower. BPAA neither accumulates in the skin, nor in any other peri-articular tissue. A steady state was reached as of the 14th day of treatment at the latest. None of the patients reported any local or systemic side effects.
12例骨关节炎患者在择期膝关节手术前,局部使用联苯乙酸凝胶(3%联苯乙酸(BPAA)),每日3次,持续14天(5例患者)、28天(6例患者)或42天(1例患者)。治疗第7天时,BPAA血浆浓度稳定在423至1040 ng/ml之间。手术中,采集滑膜和组织样本以测定BPAA浓度。与对侧膝关节相比,治疗的膝关节滑膜中BPAA水平中等,有时更高,这似乎表明存在直接吸收和全身吸收。皮肤中测得的BPAA浓度最高(1497 - 13939 ng/g)。滑膜(36 - 994 ng/g)、滑液(104 - 768 ng/ml)、肌腱(低于10 - 197 ng/g)、软骨(低于10 - 109 ng/g)、肌肉(12 - 101 ng/g)和皮下组织(16 - 97 ng/g)中的药物水平较低。BPAA既不在皮肤中蓄积,也不在任何其他关节周围组织中蓄积。最迟在治疗第14天时达到稳态。所有患者均未报告任何局部或全身副作用。