Oral Drug Delivery for Modified Release Formulations

Preface and Introduction and overview of MR formulations Part I Understanding of physiology and anatomy - factors influencing drug release and absorption from MR formulations 1. Composition of the GI lumen under fasting and fed conditions a. Composition of gastric fluids under fasting and fed conditions - Jens Van Den Abeele and Patrick Augustijns Drug Delivery and Disposition, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, O&N II, Herestraat 49 - box 921, 3000 Leuven, Belgium b. Composition of small intestinal fluids under fasting and fed conditions Edmund Kostewicz Institute for Pharmaceutical Technology, Goethe University, Max-von-Laure Str. 9, 60439 Frankfurt am Main, Germany c. Composition of large intestinal fluids under fasting and fed conditions Christos Reppas and Maria Vertzoni Department of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece. 2. Gastrointestinal transit and hydrodynamics under fasting and fed conditions Mirko Koziolek Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport, Ernst Moritz Arndt University of Greifswald, Greifswald, Germany 3. Intestinal Epithelium and Drug Transporters Karelle Ménochet*1, Hugues Chanteux*2, Jamie Henshall1, Jean-Marie Nicolas2, Sara Wright1, Judith van Asperen2 and Anna-Lena Ungell2 1UCB Celltech, Slough, United Kingdom 2UCB Biopharma SPRL, Braine-l'Alleud, Belgium 4. The interplay between drug release and intestinal gut-wall metabolism Adam S. Darwich1, Oliver J.D. Hatley2, Andrés Olivares-Morales1,3, Farzaneh Salem2, Alison Margolskee1, Amin Rostami-Hodjegan1,2 1Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, University of Manchester, Manchester M13 9PT, United Kingdom 2Certara, Blades Enterprise Centre, Sheffield, S2 4SU, United Kingdom 3Roche Pharma Research and Early Development (pRED), Roche Innovation Center Basel, Basel, Switzerland Part II Design of MR formulations - considerations, mechanisms and technologies 5. Preformulation considerations for design of oral modified-release products Christel A. S. Bergström1 and René Holm2 1 Department of Pharmacy, Uppsala University, Uppsala Biomedical Centre P.O. Box 580, SE-751 23 Uppsala, Sweden. 2 Drug Product Development, Janssen Research & Development, Johnson & Johnson, Turnhoutseweg 30, 2430 Beerse, Belgium. 6. The Application of Biopharmaceutics Classification Systems to Modified Release Formulations James M Butler Biopharmaceutics, Drug Product Design & Dev GlaxoSmithKline R&D Ware UK 7. Technologies and mechanisms for oral modified release by monolithic and multiparticulate delivery systems Gaia Colombo*, Stavros Politis, Alessandra Rossi University of Ferrara 44121 FERRARA (Italy) 8. Lipid based Formulations Joseph P. O'Shea, Caitriona M. O'Driscoll, Brendan T. Griffin Pharmacodelivery Group, School of Pharmacy, University College Cork, Ireland 9. Strategies for MR formulation development: Mesoporous Silica Georgios K. Eleftheriadis, Eleni Kontogiannidou, Christina Karavasili, Dimitrios G. Fatouros Department of Pharmacy, Laboratory of Pharmaceutical Technology, Aristotle University of Thessaloniki, 54124 GR 10. Hot melt extrusion technology for modified release (MR) formulation development Harpreet Sandhu, Siva Ram Kiran Vaka, Dipen Desai, Paras Jariwala, Aruna Railkar, Wantanee Phuapradit and Navnit Shah Paras Jariwala, Aruna Railkar, Wantanee Phuapradit Kashiv Pharma LLC, 995 Route 202/206 Bridgewater, NJ 08807 11. Gattefosse: Strategies for MR formulation development - Lipids Yvonne Rosiaux, Vincent Jannin and Cécile Morin Gattefossé SAS - 36 chemin de Genas 69804 Saint Priest France 12. Evonik: Polymethacrylates for Modified Release Formulations Miriam Robota, Felix Hofmann and Meike Pistner Meike Pistner Evonik Nutrition & Care GmbH, Darmstadt, Germany 13. Capsugel - Strategies for Modified Release oral formulation development Aurélien Sivert1, Randy Wald2, Chris Craig2, Hassan Benameur1 Randy Wald 1Capsugel/Lonza R&D, Strasbourg, France 2Capsugel/Lonza R&D, Bend, Oregon USA Part III Evaluation of MR formulations 14. Dissolution equipment and hydrodynamic considerations for evaluating MR formulations Sandra Klein Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport, Ernst Moritz Arndt University of Greifswald, Greifswald, Germany 15. The role and application of dissolution media for the investigation of modified release formulations Institute for Pharmaceutical Technology, Goethe University, Max-von-Laue Str. 9, 60439 Frankfurt am Main, Germany 16. Biorelevant dissolution testing to forecast the in vivo performance of modified release formulations Mirko Koziolek Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport, Ernst Moritz Arndt University of Greifswald, Greifswald, Germany 17. In vitro dissolution tests for considering dissolution in the lower intestine Constantinos Markopoulos, Maria Vertzoni 1Faculty of Pharmacy, School of Health Sciences, National & Kapodistrian University of Athens, Greece 18. Preclinical evaluation - animal models to evaluate MR formulations René Holm Drug Product Development, Janssen Research and Development, Johnson & Johnson, Turnhoutseweg 30, 2340 Beerse, Belgium. E-mail: rholm@its.jnj.com 19. In vitro - In vivo correlations for modified release formulations Ivana Tomic1 and Jean-Michel Cardot2 1Novartis Pharma AG, Technical R&D, Physic Garden 3 - 3.14.49, CH-4002 Base, Switzerland 2Université Clermont Auvergne MEDIS, CHU Clermont-Ferrand, CIC1405, INSERM, F-63000 Clermont-Ferrand, France 20. Application of the Simcyp Population-Based PBPK Simulator to the Modelling of MR Formulations Nikunjkumar Patel, Shriram M. Pathak and David B. Turner Simcyp Ltd (A Certara Company); UK 21. PK-Sim(r) for modeling oral drug delivery of modified release formulations Donato Teutonico, Michael Block, Lars Kuepfer, Juri Solodenko, Thomas Eissing*, Katrin Coboeken Michael Block, Lars Kuepfer, Katrin Coboeken Bayer AG, Clinical Pharmacometrics, Germany 22. Clinical Evaluation - In vivo bioequivalence assessment of MR formulations Konstantina Soulele, Panos Macheras Laboratory of Biopharmaceutics and Pharmacokinetics, Faculty of Pharmacy, University of Athens, Athens 15771, Greece 23. U.S. Regulatory Considerations for Modified Release Products Hao Zhu, Ramana S. Uppoor, Mehul Mehta Office of Clinical Pharmacology, U.S. Food and Drug Administration, 10903 New Hampshire Avenue, Silver Spring, MD 20993, USA 24. Regulatory Assessment, European Perspective Malin Filler and Anders Lindahl 25. Industry perspectives for the evaluation of MR formulations Irena Tomaszewska and Mark McAllister Pfizer, Medicinal Sciences, Sandwich, U