Müller F O, Schall R, Groenewoud G, Hundt H K, van der Merwe J C, van Dyk M
Department of Pharmacology, University of the Orange Free State, Bloemfontein, South Africa.
Eur J Clin Pharmacol. 1993;44(1):69-72. doi: 10.1007/BF00315283.
The objectives of this study were to establish if, and to what extent, benzbromarone affects allopurinol/oxypurinol kinetics, and to compare the uric acid lowering capabilities of Allomaron (allopurinol 100 mg plus benzbromarone 20 mg) with the effects of allopurinol alone in patients with confirmed gout. We studied 14 adult men in an open randomized cross-over study. After a 14 day run-in period with Zyloprim (2 x 100 mg allopurinol tablets in the morning), the patients were randomly allocated to morning doses of either Allomaron (2 tablets) or Zyloprim (2 tablets). Seven days later cross-over was effected and the alternative treatment was taken for a further 7 days. On days 7 and 14 the patients came into hospital and venous blood samples were taken over 24 h for allopurinol and oxypurinol assays by HPLC. Serum uric acid was determined on days -14, 1, 7, and 14. Benzbromarone lowered plasma oxypurinol concentrations (Allomaron/Zyloprim mean ratio of AUC0-->24 was 59%; 95% confidence interval 54-64%), but did not affect plasma allopurinol concentrations. Despite this pharmacokinetic interaction of benzbromarone with allopurinol, resulting in lower plasma concentrations of oxypurinol, Allomaron was superior to allopurinol alone in lowering serum uric acid, probably because of the added uricosuric effect of benzbromarone.
本研究的目的是确定苯溴马隆是否以及在何种程度上影响别嘌醇/氧嘌呤醇的动力学，并比较Allomaron（100毫克别嘌醇加20毫克苯溴马隆）与单独使用别嘌醇对确诊痛风患者降低尿酸的能力。我们在一项开放随机交叉研究中对14名成年男性进行了研究。在使用丙磺舒（早上服用2片100毫克别嘌醇片）进行14天的导入期后，患者被随机分配为早上服用Allomaron（2片）或丙磺舒（2片）。7天后进行交叉，再服用另一种药物7天。在第7天和第14天，患者入院，在24小时内采集静脉血样，通过高效液相色谱法进行别嘌醇和氧嘌呤醇检测。在第-14、1、7和14天测定血清尿酸。苯溴马隆降低了血浆氧嘌呤醇浓度（Allomaron/丙磺舒的AUC0→24平均比值为59%；95%置信区间为54-64%），但不影响血浆别嘌醇浓度。尽管苯溴马隆与别嘌醇存在这种药代动力学相互作用，导致血浆氧嘌呤醇浓度降低，但Allomaron在降低血清尿酸方面优于单独使用别嘌醇，这可能是因为苯溴马隆增加了促尿酸排泄的作用。
