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Determination of Rate and Extent of Scopolamine Release from Transderm Scōp® Transdermal Drug Delivery Systems in Healthy Human Adults

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  • Theme: Team Science and Education for Pharmaceuticals: the NIPTE Model
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Abstract

To estimate strength of a scopolamine transdermal delivery system (TDS) in vivo, using residual drug vs. pharmacokinetic analyses with the goal of scientifically supporting a single and robust method for use across the dosage form and ultimately facilitate the development of more consistent and clinically meaningful labeling. A two-arm, open-label, crossover pharmacokinetic study was completed in 26 volunteers. Serum samples were collected and residual scopolamine was extracted from worn TDS. Delivery extent and rate were estimated by (1) numeric deconvolution and (2) steady-state serum concentration determined from graphical and non-compartmental analyses. In residual drug analyses, mean ± SD scopolamine release rate was 0.015 ± 0.002 mg/h (11% RSD), vs. 0.016 ± 0.006 mg/h (35% RSD) from numeric deconvolution, 0.015 ± 0.005 mg/h (34% RSD) from graphical analysis, and 0.015 ± 0.007 mg/h (44% RSD) from non-compartmental analysis. In residual drug analyses, total drug released was 1.09 ± 0.11 mg (10% RSD), vs. 1.12 ± 0.40 mg (35% RSD) from numeric deconvolution, 1.07 ± 0.35 mg (33% RSD) from graphical analysis, and 1.07 ± 0.45 (42% RSD) from non-compartmental analysis. Extent and rate of scopolamine release were comparable by both approaches, but pharmacokinetic analysis demonstrated greater inter-subject variability.

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Abbreviations

TDS:

Transdermal delivery system

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Funding

This project was funded by the following grants: National Institute for Pharmaceutical Technology and Education U01 Critical Patch Manufacturing Sector Research Initiative (5U01FD004275), and NIH/NCATS CTSA U54TR001356.

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA

    Suresh Kumar Swaminathan & Karunya K. Kandimalla

  2. United States Food and Drug Administration, CDER, Office of Pharmaceutical Quality, Silver Spring, MD, USA

    Caroline Strasinger, Wei Ye & Anna Wokovich

  3. Pharmaceutical Sciences and Experimental Therapeutics, University of Iowa College of Pharmacy, 180 South Grand Avenue, 552 CPB, Iowa City, IA, 52242-1112, USA

    Megan Kelchen, Jamie Carr & Nicole K. Brogden

  4. Institute for Clinical and Translational Sciences, University of Iowa Hospitals and Clinics, Iowa City, IA, USA

    Jamie Carr

  5. United States Food and Drug Administration, CDER, Office of Generic Drugs, Office of Research and Standards, Silver Spring, MD, USA

    Priyanka Ghosh

  6. Department of Anesthesia, University of Iowa Carver College of Medicine, Iowa City, IA, USA

    Srinivasan Rajagopal & Kenichi Ueda

  7. Cardiothoracic Anesthesiology, University of Iowa Carver College of Medicine, Iowa City, IA, USA

    Srinivasan Rajagopal & Kenichi Ueda

  8. College of Pharmacy Analytical Services, University of Minnesota, Minneapolis, MN, USA

    James Fisher

  9. Department of Dermatology, University of Iowa Hospitals and Clinics, Iowa City, IA, USA

    Nicole K. Brogden

Authors
  1. Suresh Kumar Swaminathan
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  2. Caroline Strasinger
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  3. Megan Kelchen
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  4. Jamie Carr
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  5. Wei Ye
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  6. Anna Wokovich
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  7. Priyanka Ghosh
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  8. Srinivasan Rajagopal
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  9. Kenichi Ueda
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  10. James Fisher
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  11. Karunya K. Kandimalla
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  12. Nicole K. Brogden
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Corresponding authors

Correspondence to Karunya K. Kandimalla or Nicole K. Brogden.

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The authors declare that they have no conflicts of interest.

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Views expressed in this manuscript do not necessarily reflect official policies of the United States Food and Drug Administration; nor does any mention of trade names, commercial practices, or organization imply endorsement by the United States Government.

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Guest Editors: Ajaz S. Hussain, Kenneth Morris, and Vadim J. Gurvich

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Swaminathan, S.K., Strasinger, C., Kelchen, M. et al. Determination of Rate and Extent of Scopolamine Release from Transderm Scōp® Transdermal Drug Delivery Systems in Healthy Human Adults. AAPS PharmSciTech 21, 117 (2020). https://doi.org/10.1208/s12249-020-01658-4

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  • DOI: https://doi.org/10.1208/s12249-020-01658-4

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