Medical University/AKH, Department of Special Anaesthesia and Pain Therapy, Vienna, Austria.
Eur J Pharm Biopharm. 2010 Jun;75(2):225-31. doi: 10.1016/j.ejpb.2010.02.005. Epub 2010 Feb 10.
The pharmacokinetic profiles of the two commercially available transdermal fentanyl patches Matrifen (100 microg/h) and Durogesic DTrans (100 microg/h), used to manage severe chronic pain, were compared regarding their systemic exposure, rate of absorption, and safety.
Transdermal matrix fentanyl patches [Matrifen or Durogesic DTrans (100 microg/h)] were applied for 72 h to 30 healthy male subjects in a randomized, four-period (two replicated treatment sequences), crossover study; 28 subjects completed the study. The pharmacokinetic parameters of fentanyl were determined for 144 h after application using plasma samples. Safety of the patches (adverse events) and performance (adhesion, skin irritation, residual fentanyl content in the patch) were evaluated.
The plasma concentration-time curves of Matrifen (Test) and Durogesic DTrans (Reference) were similar. The geometric least square means of the Test/Reference ratio (90% confidence intervals [CI]) were within the range of 80-125%, demonstrating bioequivalence of Matrifen and Durogesic DTrans: AUC(0-tlast) 92.5 (CI 88.7-96.4), AUC(0-inf) 91.7 (CI 88.0-95.7), and C(max) 98.3 (CI 92.9-104.1). After 72 h application, Matrifen had a more efficient utilization of fentanyl (mean+/-SD 82.3+/-9.43%) than Durogesic DTrans (52.3+/-12.8%), with substantially lower residual fentanyl in patch after use. The pharmacokinetic parameters showed lower intra- and inter-subject variability for Matrifen than for Durogesic DTrans patch.
Despite different technologies, the transdermal fentanyl patches Matrifen and Durogesic DTrans are bioequivalent. Compared with Durogesic DTrans, the Matrifen patch had lower initial and lower residual fentanyl content, as well as lower intra- and inter-subject variability, allowing reproducible drug delivery and reliable analgesia.
比较两种市售的芬太尼透皮贴剂（Matrifen 100μg/h 和 Durogesic DTrans 100μg/h）的药代动力学特征，这两种贴剂用于治疗严重慢性疼痛，以评估它们的全身暴露量、吸收速率和安全性。
30 名健康男性受试者被随机分为 4 个周期（2 个重复治疗序列）交叉研究，分别应用芬太尼透皮基质贴剂（Matrifen 或 Durogesic DTrans [100μg/h]）72 小时；28 名受试者完成了这项研究。在贴剂应用后 144 小时内使用血浆样本测定芬太尼的药代动力学参数。评估贴剂的安全性（不良反应）和性能（粘贴性、皮肤刺激、贴剂中残留的芬太尼含量）。
Matrifen（试验）和 Durogesic DTrans（参比）的血浆浓度-时间曲线相似。试验/参比比值的几何均数（90%置信区间[CI]）在 80-125%范围内，表明 Matrifen 和 Durogesic DTrans 具有生物等效性：AUC（0-tlast）92.5（CI 88.7-96.4）、AUC（0-inf）91.7（CI 88.0-95.7）和 C（max）98.3（CI 92.9-104.1）。应用 72 小时后，Matrifen 比 Durogesic DTrans 更有效地利用芬太尼（平均+/-SD 82.3+/-9.43%），使用后贴剂中残留的芬太尼明显减少。与 Durogesic DTrans 贴剂相比，Matrifen 的药代动力学参数显示出较低的个体内和个体间变异性。
尽管使用了不同的技术，但芬太尼透皮贴剂 Matrifen 和 Durogesic DTrans 具有生物等效性。与 Durogesic DTrans 相比，Matrifen 贴剂初始和残留的芬太尼含量较低，个体内和个体间变异性较低，能够实现可重复的药物输送和可靠的镇痛效果。
