Labopharm, Inc, 480 boul Armand-Frappier, Laval, Québec, H7V 4B4, Canada.
J Clin Pharmacol. 2010 May;50(5):544-53. doi: 10.1177/0091270009347673. Epub 2010 Jan 5.
The pharmacokinetics of a once-daily formulation of tramadol (Tramadol Contramid OAD 200-mg tablets) following single-dose and multiple-dose administration was compared with that of an immediate-release product (tramadol IR 50-mg tablets) in 2 separate studies. In both studies, AUC parameters met bioequivalence criteria, whereas C(max) of Tramadol Contramid OAD was lower than that of tramadol IR following a 200-mg daily dosage. After single-dose administration, the mean tramadol concentration at 1 hour postdose was within the range associated with analgesic efficacy (>100 ng/mL), and the mean concentration remained above this level for the remainder of the dosing interval. Steady state was attained within 48 hours following multiple-dose administration. Tramadol Contramid OAD provides a rapid rise in plasma concentrations and an equivalent daily systemic exposure as tramadol IR, with a reduction in peak plasma concentrations.
在两项研究中，对比了每日一次给予曲马多（曲马多控释片 OAD200mg 片剂）单剂量和多剂量给药后的药代动力学，与即释产品（曲马多 IR50mg 片剂）进行了比较。在这两项研究中，AUC 参数符合生物等效性标准，而在每日 200mg 剂量后，曲马多控释片 OAD 的 C(max)低于曲马多 IR。单剂量给药后，1 小时后药物浓度达峰，在与镇痛疗效相关的范围内（>100ng/mL），并且在整个给药间隔的其余时间内，平均浓度保持在此水平之上。多剂量给药后 48 小时内达到稳态。曲马多控释片 OAD 可快速提高血浆浓度，与曲马多 IR 具有相同的每日全身暴露量，同时降低了血浆峰浓度。
