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首页> 外文期刊>Clinical drug investigation >Dose proportionality and pharmacokinetics of fentanyl buccal soluble film in healthy subjects: a phase I, open-label, three-period, crossover study.
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Dose proportionality and pharmacokinetics of fentanyl buccal soluble film in healthy subjects: a phase I, open-label, three-period, crossover study.

机译：芬太尼颊可溶性膜在健康受试者中的剂量比例和药代动力学：I期，开放标签，三期，交叉研究。

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BACKGROUND AND OBJECTIVES: Fentanyl buccal soluble film (FBSF) is a small, bilayered, water-soluble polymer film (BioErodible MucoAdhesive; BEMA) that adheres to the buccal mucosa and rapidly delivers fentanyl into the systemic circulation. It is approved for the treatment of cancer breakthrough pain in adult opioid-tolerant patients. The objective of this study was to evaluate the dose proportionality of the pharmacokinetics of FBSF in healthy subjects across a range of doses. METHODS: This was a phase I, open-label, single-dose, three-period, Latin-square crossover study in which 12 healthy subjects received single FBSF doses of 200, 600 and 1200 mug with 72 hours between doses. Oral naltrexone was administered to each subject prior to and after each study dose. Serial venous blood samples were collected for 48 hours after study drug administration. Adverse events were recorded throughout the study. Dose linearity was examined using a power model (P = a x Doseb), where P represents the dependent variable (maximum plasma drug concentration [C(max)], area under the plasma concentration-time curve [AUC] from time zero to time of the last measurable concentration [AUC(last)], or AUC from time zero to infinity [AUC(infinity)]), and a and b are constants. A value of b approximately 1 indicated linearity. RESULTS: Following administration of FBSF doses of 200-1200 mug, mean C(max) values increased in a linear manner with values ranging from 0.383 ng/mL to 2.19 ng/mL, respectively. Mean AUC(last) values increased from 3.001 ng.h/mL to 19.17 ng.h/mL and mean AUC(infinity) increased in a linear manner from 3.456 ng.h/mL to 20.43 ng.h/mL. All reported adverse events were considered to be mild to moderate in severity. CONCLUSIONS: This study demonstrates that peak fentanyl plasma concentrations and overall exposure increase in a dose-proportional manner following administration of FBSF.
机译：背景与目的：芬太尼颊可溶性膜（FBSF）是一种小的双层水溶性聚合物膜（BioErodible MucoAdhesive; BEMA），它粘附于颊粘膜并将芬太尼迅速递送至全身循环。它被批准用于治疗成人阿片耐受性患者的癌症突破性疼痛。这项研究的目的是评估健康受试者在一系列剂量范围内FBSF药代动力学的剂量比例。方法：这是第一阶段，开放标签，单剂量，三期，拉丁方交叉研究，其中12名健康受试者接受了200、600和1200马克杯的FBSF单次剂量，两次剂量之间间隔72小时。在每个研究剂量之前和之后，向每个受试者施用口服纳曲酮。服用研究药物后48小时收集静脉血样。在整个研究中记录不良事件。使用功效模型（P = ax Doseb）检查剂量线性，其中P代表因变量（最大血浆药物浓度[C（max）]，从零时至血浆时间的血浆浓度-时间曲线[AUC]下的面积）。最后可测量的浓度[AUC（last）]或从时间零到无穷大的AUC [AUC（无穷大）]，并且a和b是常数。 b的值大约为1表示线性。结果：FBSF剂量为200-1200马克杯给药后，平均C（max）值呈线性增加，范围分别为0.383 ng / mL至2.19 ng / mL。平均AUC（last）值从3.001 ng.h / mL增加到19.17 ng.h / mL，平均AUC（infinity）以线性方式从3.456 ng.h / mL增加到20.43 ng.h / mL。所有报告的不良事件均被视为轻度至中度。结论：这项研究表明，在服用FBSF后，芬太尼血浆峰值浓度和总暴露量呈剂量比例增加。

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