Drake J, Kirkpatrick C T, Aliyar C A, Crawford F E, Gibson P, Horth C E
Boehringer Ingelheim Ltd, Bracknell, Berkshire, UK.
Br J Clin Pharmacol. 1996 May;41(5):417-20. doi: 10.1046/j.1365-2125.1996.32810.x.
The relative bioavailability and pharmacokinetic profiles of Oramorph SR (OSR) and MST Continus (MST), were evaluated by a randomized, four-way cross-over study in 24 healthy, male volunteers given single oral (30 mg) doses whilst fasting or after a high-fat breakfast. Mean Cmax, tmax, AUC (0,24h), AUC and tlag were significantly greater in fed compared with fasting subjects. Overall relative bioavailability of the two formulations (log AUC), was within the acceptable 80-125% limits for bioequivalence both fed and fasting. Mean fasting Cmax for OSR was greater than MST (P < 0.05) but there was no difference between formulations in mean fed Cmax. No statistically significant difference between OSR and MST was found for other parameters nor in the incidence of adverse events. These results suggest that OSR and MST are bioequivalent and that if patients were to transfer between formulations, dosage adjustment would be unnecessary, irrespective of their meal schedules or food intake.
通过一项随机、四交叉研究，在24名健康男性志愿者中评估了奥施康定控释片（OSR）和美施康定（MST）的相对生物利用度和药代动力学特征。这些志愿者在禁食或高脂早餐后单次口服（30毫克）剂量。与禁食受试者相比，进食受试者的平均Cmax、tmax、AUC(0,24h)、AUC和tlag显著更高。两种制剂的总体相对生物利用度（对数AUC）在进食和禁食状态下均在生物等效性可接受的80 - 125%范围内。OSR的平均禁食Cmax大于MST（P < 0.05），但进食状态下两种制剂的平均Cmax无差异。在其他参数以及不良事件发生率方面，OSR和MST之间未发现统计学显著差异。这些结果表明，OSR和MST具有生物等效性，并且如果患者在两种制剂之间转换，无论其用餐时间或食物摄入量如何，都无需调整剂量。
