Nicholls Andrew, Harris-Collazo Raúl, Huang Michael, Hardiman Yun, Jones Richard, Moro Luigi
Pharmaceutical Consulting, Encinitas, CA 92024, USA.
J Int Med Res. 2013 Apr;41(2):386-94. doi: 10.1177/0300060513476588. Epub 2013 Mar 7.
To compare the pharmacokinetics of the extended-release MMX® formulation of budesonide (Uceris®) with that of Entocort® EC, an extended (controlled ileal) release formulation of budesonide.
Using an open-label, randomized, three-period crossover, Latin square design, healthy male or female volunteers received single doses of 6 mg Uceris®, 9 mg Uceris® or 9 mg Entocort® EC. Standard pharmacokinetic parameters were assessed.
The study included 12 subjects. The 9 mg Uceris® and 9 mg Entocort® EC formulations had comparable area under the concentration-time curve (AUC) data, but 9 mg Uceris® had a notably longer time to first appearance in plasma (median Tlag, 6 h versus 1 h, respectively), and a delayed time to maximum concentration (median Tmax, 15 h versus 5 h, respectively) compared with 9 mg Entocort® EC. The ratio of log-transformed AUC0-last (Uceris®/Entocort® EC) was 91% (90% confidence interval [CI] 77%, 108%) and the corresponding maximum concentration ratio was 79% (90% CI 63%, 100%).
Uceris was associated with a similar extent (AUC) of systemic exposure to budesonide compared with that following Entocort. However, for Uceris, the pharmacokinetic profile was delayed, a pattern consistent with greater colonic delivery of the active substance.
比较布地奈德的缓释型MMX®制剂（Uceris®）与布地奈德的缓释（回肠控释）制剂Entocort® EC的药代动力学。
采用开放标签、随机、三周期交叉拉丁方设计，健康男性或女性志愿者接受6 mg Uceris®、9 mg Uceris®或9 mg Entocort® EC的单剂量给药。评估标准药代动力学参数。
该研究纳入了12名受试者。9 mg Uceris®和9 mg Entocort® EC制剂的浓度-时间曲线下面积（AUC）数据具有可比性，但与9 mg Entocort® EC相比，9 mg Uceris®在血浆中首次出现的时间明显更长（中位Tlag分别为6小时和1小时），达到最大浓度的时间延迟（中位Tmax分别为15小时和5小时）。对数转换后的AUC0-last（Uceris®/Entocort® EC）比值为91%（90%置信区间[CI] 77%，108%），相应的最大浓度比值为79%（90% CI 63%，100%）。
与Entocort相比，Uceris与布地奈德全身暴露的程度（AUC）相似。然而，对于Uceris，药代动力学特征延迟，这一模式与活性物质在结肠的递送增加一致。
