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Juszczyk E, Kisło K, Żero P, et al. Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial. Pharmaceutics. 2021;13(6)doi: 10.3390/pharmaceutics13060804.
Juszczyk, E., Kisło, K., Żero, P., Tratkiewicz, E., Wieczorek, M., Paszkowska, J., Banach, G., Wiater, M., Hoc, D., Garbacz, G., Sczodrok, J., & Danielak, D. (2021). Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial. Pharmaceutics, 13(6), . https://doi.org/10.3390/pharmaceutics13060804
Juszczyk, Ewelina, et al. "Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial." Pharmaceutics vol. 13,6 (2021). doi: https://doi.org/10.3390/pharmaceutics13060804
Juszczyk E, Kisło K, Żero P, Tratkiewicz E, Wieczorek M, Paszkowska J, Banach G, Wiater M, Hoc D, Garbacz G, Sczodrok J, Danielak D. Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial. Pharmaceutics. 2021 May 28;13(6). doi: 10.3390/pharmaceutics13060804. PMID: 34071286; PMCID: PMC8227174.
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Pharmaceutics. 2021 May 28;13(6). doi: 10.3390/pharmaceutics13060804.

Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial.

Pharmaceutics

Ewelina Juszczyk, Kamil Kisło, Paweł Żero, Ewa Tratkiewicz, Maciej Wieczorek, Jadwiga Paszkowska, Grzegorz Banach, Marcela Wiater, Dagmara Hoc, Grzegorz Garbacz, Jaroslaw Sczodrok, Dorota Danielak

Affiliations

  1. Research and Development Center, Celon Pharma S.A., Marymoncka 15, 05-052 Kazu? Nowy, Poland.
  2. Physiolution Polska sp. z o.o., 74 Pi?sudskiego St., 50-020 Wroc?aw, Poland.
  3. Physiolution GmbH, Walther Rathenau Strasse 49a, 17489 Greifswald, Germany.
  4. Department of Physical Pharmacy and Pharmacokinetics, Poznan University of Medical Sciences, 6 ?wi?cickiego St., 60-781 Pozna?, Poland.

PMID: 34071286 PMCID: PMC8227174 DOI: 10.3390/pharmaceutics13060804

Abstract

Sustained-release (SR) formulations may appear advantageous in first-in-human (FIH) study of innovative medicines. The newly developed SR matrix tablets require prolonged maintenance of API concentration in plasma and should be reliably assessed for the risk of uncontrolled release of the drug. In the present study, we describe the development of a robust SR matrix tablet with a novel G-protein-coupled receptor 40 (GPR40) agonist for first-in-human studies and introduce a general workflow for the successful development of SR formulations for innovative APIs. The hydrophilic matrix tablets containing the labeled API dose of 5, 30, or 120 mg were evaluated with several methods: standard USP II dissolution, bio-predictive dissolution tests, and the texture and matrix formation analysis. The standard dissolution tests allowed preselection of the prototypes with the targeted dissolution rate, while the subsequent studies in physiologically relevant conditions revealed unwanted and potentially harmful effects, such as dose dumping under an increased mechanical agitation. The developed formulations were exceptionally robust toward the mechanical and physicochemical conditions of the bio-predictive tests and assured a comparable drug delivery rate regardless of the prandial state and dose labeled. In conclusion, the introduced development strategy, when implemented into the development cycle of SR formulations with innovative APIs, may allow not only to reduce the risk of formulation-related failure of phase I clinical trial but also effectively and timely provide safe and reliable medicines for patients in the trial and their further therapy.

Keywords: GPR40 agonist; biorelevant dissolution testing; first in human clinical trials; simulation of gastrointestinal passage; stress test device; sustained-release tablets

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