Manz G, Glynn J P
Z Rheumatol. 1975 Nov-Dec;34(11-12):400-7.
The authors report on the drug benorylate which is available in the Federal Republic under the name of Benortan (4-acetamidophenyl-2-acetoxybenzoat). Numerous examinations have shown that it is well tolerated by mouth and that it has beneficial clinical effects with few side effects. Benorylate is a neutral, fat-soluble, water-insoluble substance which upon absorption is almost completely hydrolyzed into salicylate and paracetamol. 6 patients with classical seropositive rheumatoid arthritis and with a highly active synovialitis of one or both knee joints not previously treated received 4 g of a 40% benorylate suspension orally twice daily over a period of 9-14 days. On different days at exactly determined times of drug administration blood, and on the day of synovectomy synovial fluid and synovial tissue, were taken and frozen to - 70 degrees C and subsequently examined as to the content of salicylate, paracetamol, and unchanged benorylate. The plasma levels of salicylate and paracetamol were generally distinctly higher than the concentrations of these metabolites in the synovial fluid. Benorylate which is practically not detectable in blood is found in the synovial tissue and is detectable in greatest quantities in the most inflamed synovial villi. Benorylate can probably penetrate into the synovial membrane like its metabolites salicylate and paracetamol; it remains, however, to be examined whether the metabolites are distributed differently in different synovial areas (active inflamed and unattacked synovial tissue, respectively) in the same way as benorylate per se.
作者报道了一种名为贝诺酯的药物,在联邦共和国它以贝诺坦(4 - 乙酰氨基苯基 - 2 - 乙酰氧基苯甲酸酯)的名称上市。大量研究表明,口服该药物耐受性良好,临床效果良好且副作用少。贝诺酯是一种中性、脂溶性、水不溶性物质,吸收后几乎完全水解为水杨酸酯和对乙酰氨基酚。6例经典血清阳性类风湿关节炎患者,其一个或两个膝关节存在高度活跃的滑膜炎且此前未接受过治疗,在9 - 14天的时间里,每天口服两次40%的贝诺酯混悬液,每次4克。在给药的不同日子,在精确确定的给药时间采集血液,在滑膜切除术当天采集滑液和滑膜组织,冷冻至 - 70摄氏度,随后检测其中水杨酸酯、对乙酰氨基酚和未变化的贝诺酯的含量。血浆中的水杨酸酯和对乙酰氨基酚水平通常明显高于滑液中这些代谢物的浓度。在血液中几乎检测不到的贝诺酯在滑膜组织中被发现,且在炎症最严重的滑膜绒毛中含量最高。贝诺酯可能像其代谢物水杨酸酯和对乙酰氨基酚一样能够渗透到滑膜中;然而,这些代谢物在不同滑膜区域(分别为活跃炎症滑膜组织和未受侵袭的滑膜组织)的分布是否与贝诺酯本身的分布方式不同,仍有待研究。