Henrotin Y, Bassleer C, Reginster J Y, Franchimont P
University of Liège, Belgium.
Clin Rheumatol. 1989 Mar;8 Suppl 1:36-42. doi: 10.1007/BF02214108.
Human chondrocytes in three-dimensional culture were incubated for up to 20 days in the presence of etodolac, a nonsteroidal anti-inflammatory drug which penetrates readily into the synovial fluid. Even at an etodolac concentration of 80 micrograms/ml, DNA synthesis, proteoglycan synthesis, and type-II collagen synthesis were unchanged. Collagenase production was also unaffected by etodolac (60 micrograms/ml). In contrast, prostaglandin E2 production was reduced by 84% in the presence of 60 micrograms/ml of etodolac. The 80 micrograms/ml concentration is 5 times that found in the serum of subjects treated with 200 mg of etodolac twice a day for 6 days, and 33 times the concentration in synovial fluid of arthritic patients treated with etodolac 200 mg twice a day for 7 days. These in vitro results indicate that anti-inflammatory levels of etodolac may not damage articular cartilage in vivo.
将三维培养的人软骨细胞在依托度酸(一种能迅速渗透到滑液中的非甾体抗炎药)存在的情况下培养长达20天。即使在依托度酸浓度为80微克/毫升时,DNA合成、蛋白聚糖合成和II型胶原合成也未发生变化。胶原酶的产生也不受依托度酸(60微克/毫升)的影响。相比之下,在60微克/毫升依托度酸存在的情况下,前列腺素E2的产生减少了84%。80微克/毫升的浓度是每天两次服用200毫克依托度酸,持续6天的受试者血清中浓度的5倍,是每天两次服用200毫克依托度酸,持续7天的关节炎患者滑液中浓度的33倍。这些体外实验结果表明,依托度酸的抗炎水平在体内可能不会损害关节软骨。