Safety, Tolerability, and Dose Proportionality of a Novel Transdermal Fentanyl Matrix Patch and Bioequivalence With a Matrix Fentanyl Patch: Two Phase 1 Single-Center Open-Label, Randomized Crossover Studies in Healthy Japanese Volunteers

被引:2
作者
Lorch, Ulrike [1 ]
Pierscionek, Tomasz [1 ]
Freier, Anne [2 ]
Spencer, Christopher S. [2 ]
Taubel, Jorg [1 ,3 ]
机构
[1] St Georges Univ London, Richmond Pharmacol Ltd, Cranmer Terrace, London, England
[2] Richmond Res Inst, London, England
[3] St Georges Univ London, London, England
来源
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT | 2021年 / 10卷 / 03期
关键词
bioequivalence; dose proportionality; fentanyl; Japanese; pharmacokinetic; phase; 1; transdermal patch; DELIVERY-SYSTEM; PHARMACOKINETICS; EFFICACY; VARIABILITY; DRUG; METABOLISM; TRIAL;
D O I
10.1002/cpdd.846
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Two open-label, single-dose, randomized crossover studies were conducted in healthy Japanesemen to (1) assess dose proportionality of 5 doses (1.38, 2.75, 5.5, 8.25, and 11.0 mg) of Lafenta, a novel matrix-type transdermal fentanyl patch with a rate-controlling membrane; and (2) compare patch bioequivalence (11.0 mg) with a commercially available reference patch (Durotep MT Patch [16.8 mg]). Pharmacokinetics, adhesion performance, residual fentanyl, and safety parameters were assessed. Increases in mean AUC(0-t)and C(max)after application of the test patch were dose proportional. The test patch (11.0 mg) was bioequivalent to the 16.8-mg reference patch in terms of mean AUC(0-inf), AUC(0-t), and C-max. Residual fentanyl levels 72 hours postapplication were lower in the test than in the reference patch. Differences in adhesion performance between the test and the reference patch did not affect delivery efficacy and reliability of the novel matrix patch. Safety findings were in line with previous experiences with fentanyl. Both studies showed low variation in fentanyl exposure and delivery via the test patch. The test patch provided equivalent fentanyl exposure at a lower dose than the reference patch formulation with lower variability and the potential to lower medicinal waste.
引用
收藏
页码:260 / 271
页数:12
相关论文
共 31 条
[21]   Relating human genetic variation to variation in drug responses [J].
Median, Ashraf G. ;
Wheeler, Heather E. ;
Jones, Richard Baker ;
Dolan, M. Eileen .
TRENDS IN GENETICS, 2012, 28 (10) :487-495
[22]   A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines [J].
Niepel, Mario ;
Hafner, Marc ;
Mills, Caitlin E. ;
Subramanian, Kartik ;
Williams, Elizabeth H. ;
Chung, Mirra ;
Gaudio, Benjamin ;
Barrette, Anne Marie ;
Stern, Alan D. ;
Hu, Bin ;
Korkola, James E. ;
Gray, Joe W. ;
Birtwistle, Marc R. ;
Heiser, Laura M. ;
Sorger, Peter K. ;
Shamu, Caroline E. ;
Jayaraman, Gomathi ;
Azeloglu, Evren U. ;
Iyengar, Ravi ;
Sobie, Eric A. ;
Mills, Gordon B. ;
Liby, Tiera ;
Jaffe, Jacob D. ;
Alimova, Maria ;
Davison, Desiree ;
Lu, Xiaodong ;
Golub, Todd R. ;
Subramanian, Aravind ;
Shelley, Brandon ;
Svendsen, Clive N. ;
Ma'ayan, Avi ;
Medvedovic, Mario .
CELL SYSTEMS, 2019, 9 (01) :35-+
[23]   Body mass index (BMI) but not body weight is associated with changes in the metabolism of risperidone; A pharmacokinetics-based hypothesis [J].
Paulzen, Michael ;
Haen, Ekkehard ;
Stegmann, Benedikt ;
Hiemke, Christoph ;
Gruender, Gerhard ;
Lammertz, Sarah E. ;
Schoretsanitis, Georgios .
PSYCHONEUROENDOCRINOLOGY, 2016, 73 :9-15
[24]   FENTANYL - A REVIEW FOR CLINICAL AND ANALYTICAL TOXICOLOGISTS [J].
POKLIS, A .
JOURNAL OF TOXICOLOGY-CLINICAL TOXICOLOGY, 1995, 33 (05) :439-447
[25]   Transdermal Delivery of Fentanyl from Matrix and Reservoir Systems: Effect of Heat and Compromised Skin [J].
Prodduturi, Suneela ;
Sadrieh, Nakissa ;
Wokovich, Anna M. ;
Doub, William H. ;
Westenberger, Benjamin J. ;
Buhse, Lucinda .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2010, 99 (05) :2357-2366
[26]   The fentanyl family: A distinguished medical history tainted by abuse [J].
Raffa, R. B. ;
Pergolizzi, J. V. ;
LeQuang, J. A. ;
Taylor, R., Jr. ;
Colucci, S. ;
Annabi, M. H. .
JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS, 2018, 43 (01) :154-158
[27]   SOLUBILITY AND RELATED PHYSICOCHEMICAL PROPERTIES OF NARCOTIC ANALGESICS [J].
ROY, SD ;
FLYNN, GL .
PHARMACEUTICAL RESEARCH, 1988, 5 (09) :580-586
[28]   Increases in Drug and Opioid Overdose Deaths - United States, 2000-2014 [J].
Rudd, Rose A. ;
Aleshire, Noah ;
Zibbell, Jon E. ;
Gladden, R. Matthew .
MMWR-MORBIDITY AND MORTALITY WEEKLY REPORT, 2016, 64 (50-51) :1378-1382
[29]  
Solassol I, 2005, ONCOL REP, V14, P1029
[30]   Should ethnicity serve as the basis for clinical trial design? Importance of race/ethnicity in clinical trials - Lessons from the African-American Heart Failure Trial (A-HeFT), the African-American Study of Kidney Disease and Hypertension (AASK), and the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) [J].
Taylor, AL ;
Wright, JT .
CIRCULATION, 2005, 112 (23) :3654-3660