Oral Drug Delivery for Modified Release Formulations E-Book

• Herausgeber: John Wiley & Sons
• Kategorie: Wissenschaft und neue Technologien
• Sprache: Englisch

Seitenzahl: 1452

Veröffentlichungsjahr: 2022

Beschreibung

ORAL DRUG DELIVERY FOR MODIFIED RELEASE FORMULATIONS

Provides pharmaceutical development scientists with a detailed reference guide for the development of MR formulations

Oral Drug Delivery for Modified Release Formulations is an up-to-date review of the key aspects of oral absorption from modified-release (MR) dosage forms. This edited volume provides in-depth coverage of the physiological factors that influence drug release and of the design and evaluation of MR formulations.

Divided into three sections, the book begins by describing the gastrointestinal tract (GIT) and detailing the conditions and absorption processes occurring in the GIT that determine a formulation’s oral bioavailability. The second section explores the design of modified release formulations, covering early drug substance testing, the biopharmaceutics classification system, an array of formulation technologies that can be used for MR dosage forms, and more. The final section focuses on in vitro, in silico, and in vivo evaluation and regulatory considerations for MR formulations. Topics include biorelevant dissolution testing, preclinical evaluation, and physiologically-based pharmacokinetic modelling (PBPK) of in vivo behaviour. Featuring contributions from leading researchers with expertise in the different aspects of MR formulations, this volume:

• Provides authoritative coverage of physiology, physicochemical determinants, and in-vitro in-vivo correlation (IVIVC)
• Explains the different types of MR formulations and defines the key terms used in the field
• Discusses the present status of MR technologies and identifies current gaps in research
• Includes a summary of regulatory guidelines from both the US and the EU
• Shares industrial experiences and perspectives on the evaluation of MR dosage formulations

Oral Drug Delivery for Modified Release Formulations is an invaluable reference and guide for researchers, industrial scientists, and graduate students in general areas of drug delivery including pharmaceutics, pharmaceutical sciences, biomedical engineering, polymer and materials science, and chemical and biochemical engineering.

Leseprobe

Oral Drug Delivery for Modified Release Formulations

Edited by

Edmund S. Kostewicz

Fraunhofer Institute for Translational

Medicine and Pharmacology ITMP

Frankfurt, Germany

Maria Vertzoni

National and Kapodistrian University of Athens

Athens, Greece

Heather A. E. Benson

Curtin University of Technology

Perth, WA, Australia

Michael S. Roberts

University of South Australia/University of Queensland

Brisbane, QLD, Australia

This edition first published 2022© 2022 John Wiley & Sons, Inc.

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The right of Edmund S. Kostewicz, Maria Vertzoni, Heather A. E. Benson and Michael S. Roberts to be identified as the authors of the editorial material in this work has been asserted in accordance with law.

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Library of Congress Cataloging‐in‐Publication Data

Names: Kostewicz, Edmund S., editor. | Vertzoni, Maria, editor. | Benson, Heather A. E., editor. | Roberts, Michael S., 1949‐ editor.Title: Oral drug delivery for modified release formulations / edited by Edmund S Kostewicz, Maria Vertzoni, Heather A E Benson, Michael S Roberts.Description: Hoboken, NJ : Wiley, 2022. | Includes bibliographical references and index.Identifiers: LCCN 2021025872 (print) | LCCN 2021025873 (ebook) | ISBN 9781119772699 (cloth) | ISBN 9781119772705 (Adobe PDF) | ISBN 9781119772712 (epub)Subjects: MESH: Delayed‐Action Preparations | Administration, Oral | Drug Delivery SystemsClassification: LCC RS199.5 (print) | LCC RS199.5 (ebook) | NLM QV 786 | DDC 615/.6–dc23LC record available at https://lccn.loc.gov/2021025872LC ebook record available at https://lccn.loc.gov/2021025873

Cover image: © yodiyim/iStock/Getty Images; yulia_lavrova/ShutterstockCover design by Wiley

Preface

Given the ease of application, the oral route for drug delivery is the most common administration route for patients. To provide the desired efficacy and safety profile, there are situations where the ability to control the rate and site of drug release is required over conventional dosage formulations. Modified release (MR) formulations are presently an important element of pharma portfolios and offer pharmaceutical development teams the opportunity to use diverse and at times complex technologies for the oral delivery of drugs.

As defined by the European Medicines Agency, MR formulations can include prolonged release, delayed release, and multiphasic release (biphasic and pulsatile), which can either be multiple‐ or single‐unit dosage forms.

Oral Drug Delivery for MR Formulations focuses on the key aspects that need to be considered when developing MR formulations to ensure a successful clinical outcome.

The book is divided into three sections. In the first section, a greater understanding of the physiological and anatomical factors influencing drug release and absorption, particularly for MR formulations, is given. The book begins with a description of the gastrointestinal tract (GIT), from the stomach through to the colon (Chapter 1), followed by a description of transit and hydrodynamic conditions that the formulation is exposed to as it passes through the GI tract (Chapter 2). Once the drug is released from the formulation, a detailed description of the intestinal epithelium and the absorption processes occurring along the GIT is provided (Chapter 3). Another factor determining the oral bioavailability is the role of gut wall metabolism, which is described in detail in Chapter 4.

The second section of the book deals with the design of MR formulations in terms of the considerations, mechanisms, and examples of different technologies that are available. It begins with the physicochemical characterization of drug substances that is needed for the design of MR dosage forms (Chapter 5) and includes essential early drug substance testing and early performance testing of formulations. Further, the biopharmaceutics classification system is presented as a system to enable pharmaceutical development teams to consider biopharmaceutics‐related challenges to assess the feasibility of developing MR formulations (Chapter 6). The following chapters provide a detailed description of the vast array of different formulation technologies that can be considered for MR formulations. These include diverse strategies from monolithic and multiparticulate delivery systems (Chapter 7), lipid‐based formulations (Chapter 8), mesoporous silica (Chapter 9), and hot melt extrusion technology (Chapter 10). Additionally, a number of organizations specializing in the development of functional excipients and innovative drug delivery solutions for MR formulations have provided guidance on how their technologies can be applied to MR development programs, which include Gattefossé SAS (Chapter 11), Evonik Operations GmbH (Chapter 12), and Capsugel/Lonza R&D (Chapter 13).

The final section of the book deals with the in vitro, in silico, and in vivo evaluation and regulatory considerations for MR formulations. Chapters 14–17 deal with the in vitro investigation of MR formulations in terms of the dissolution equipment, hydrodynamic conditions, dissolution media, and summary of biorelevant dissolution testing conditions to forecast the in vivo performance of these formulations. The use of animal models for the preclinical evaluation is considered in Chapter 18, while in Chapter 19, the use of an in vitro–in vivo correlation, and how it can be employed to estimate the in vivo performance of MR formulations, is explored. Given the ever‐expanding role of physiologically based pharmacokinetic modeling (PBPK) to simulate in vivo behavior, Chapters 20 and 21 illustrate the application of two important PBPK models including Simcyp Simulator and PK‐SIM for predicting the in vivo performance of MR formulations. In terms of the subsequent clinical evaluation of the MR product, this is further explained in Chapter 22. Of importance, the following two chapters provide a summary of the regulatory guidelines that need to be considered from both a US (Chapter 23) and EU (Chapter 24) perspective. To reflect on the challenges currently facing the pharmaceutical industry, the final chapter shares some industrial experiences and perspectives on the evaluation of MR dosage formulations.

Both Maria and myself would like to warmly thank all of the authors for their valuable contributions to this book. We trust that Oral Drug Delivery for MR Formulations will provide pharmaceutical development scientist with a thorough reference guide for the development of MR formulations.

Winter 2021/22

Edmund S. KostewiczMaria Vertzoni

List of Contributors

Jens Van Den AbeeleDrug Delivery and DispositionDepartment of Pharmaceutical and Pharmacological SciencesKU LeuvenLeuvenBelgium

Cord J. AndreasInstitute for Pharmaceutical TechnologyGoethe UniversityGermany

Judith van AsperenUCB Biopharma SPRLBraine‐l’AlleudBelgium

Patrick AugustijnsDrug Delivery and DispositionDepartment of Pharmaceutical and Pharmacological SciencesKU LeuvenLeuvenBelgium

Christel A.S. BergströmDepartment of PharmacyUppsala Biomedical CentreUppsala UniversityUppsalaSweden

Hassan BenameurCapsugel/Lonza R&DStrasbourgFrance

Michael BlockClinical PharmacometricsBayer AGLeverkusenGermany

James M. ButlerBiopharmaceutics Drug Product DevelopmentGlaxoSmithKline R&DWareUK

Jean‐Michel CardotUniversité Clermont Auvergne MEDISClermont–FerrandFrance

Hugues ChanteuxQuantitative Pharmacologyand DMPKUCB Biopharma SPRLBraine‐l’AlleudBelgium

Katrin CoboekenClinical PharmacometricsBayer AGLeverkusenGermany

Gaia ColomboDepartment of Life Sciences and BiotechnologyUniversity of FerraraFerraraItaly

Chris CraigCapsugel/Lonza R&DBendOregonUSA

Adam S. DarwichDivision of Health Informatics and LogisticsDepartment of Biomedical Engineering and Health SystemsKTH Royal Institute of TechnologyStockholmSweden

Dipen DesaiAmneal PharmaceuticalsBridgewater, NJUSA

Thomas EissingClinical PharmacometricsBayer AGLeverkusenGermany

Georgios K. EleftheriadisDepartment of Pharmacy Laboratory of Pharmaceutical TechnologyAristotle University of ThessalonikiThessalonikiGreece

Dimitrios G. FatourosDepartment of PharmacyLaboratory of Pharmaceutical TechnologyAristotle University of ThessalonikiThessalonikiGreece

Malin FillerSwedish Medical Products AgencyUppsalaSweden

SDS LifescienceDanderydSweden

Brendan T. GriffinPharmacodelivery GroupSchool of PharmacyUniversity College CorkCorkIreland

Oliver J. HatleySimcyp DivisionCertara UK LtdSheffieldUK

Jamie HenshallQuantitative Pharmacology and DMPKUCB CelltechSloughUK

Felix HofmannEvonik Operations GmbHDarmstadtGermany

René HolmDepartment of PhysicsChemistry and PharmacyUniversity of Southern DenmarkCampusvej 555230 Odense MDenmark

Paras JariwalaAmneal PharmaceuticalsBridgewater, NJUSA

Vincent JanninGattefossé SASSaint PriestFrance

Christina KaravasiliDepartment of PharmacyLaboratory of Pharmaceutical TechnologyAristotle University of ThessalonikiThessalonikiGreece

Sandra KleinInstitute of PharmacyUniversity of GreifswaldGreifswaldGermany

Edmund S. KostewiczFraunhofer Institute for TranslationalMedicine and Pharmacology ITMPFrankfurt, Germany

Mirko KoziolekDepartment of Biopharmaceutics and Pharmaceutical TechnologyCenter of Drug Absorption and TransportUniversity of GreifswaldGreifswaldGermany

Eleni KontogiannidouDepartment of PharmacyLaboratory of Pharmaceutical TechnologyAristotle University of ThessalonikiThessalonikiGreece

Lars KuepferClinical PharmacometricsBayer AGLeverkusenGermany

Anders LindahlSwedish Medical Products AgencyUppsalaSweden

Panos MacherasDepartment of PharmacyNational and KapodistrianUniversity of AthensAthensGreece

Alison MargolskeeCentre for Applied Pharmacokinetic ResearchSchool of Health SciencesUniversity of ManchesterManchesterUK

Constantinos MarkopoulosDepartment of PharmacySchool of Health Sciences National & Kapodistrian University of AthensAthensGreece

Mark McAllisterPfizerPharmaceutical Sciences Small MoleculeSandwichUK

Karelle MénochetQuantitative Pharmacology and DMPKUCB CelltechSloughUK

Mehul MehtaOffice of Clinical PharmacologyU.S. Food and Drug AdministrationSilver Spring, MDUSA

Cécile MorinGattefossé SASSaint PriestFrance

Jean‐Marie NicolasQuantitative Pharmacology and DMPKUCB Biopharma SPRLBraine‐l’AlleudBelgium

Caitriona M. O’DriscollPharmacodelivery GroupSchool of PharmacyUniversity College CorkCorkIreland

Andrés Olivares‐MoralesRoche Pharma Research and EarlyDevelopment (pRED)Roche Innovation Center BaselBaselSwitzerland

Joseph P. O’SheaPharmacodelivery GroupSchool of PharmacyUniversity College CorkCorkIreland

Shriram M. PathakSimcyp DivisionCertara UK LimitedSheffield UK

Nikunjkumar PatelSimcyp DivisionCertara UK LimitedSheffield UK

Wantanee PhuapraditIndependent Scientific AdvisorLewesDelawareUSA

Meike PistnerEvonik Operations GmbHDarmstadtGermany

Stavros PolitisDepartment of PharmacyNational and Kapodistrian University of AthensAthensGreece

Aruna RailkarQuotient SciencesRuddingtonNottinghamUK

Christos ReppasDepartment of PharmacyNational and Kapodistrian University of AthensAthensGreece

Miriam RobotaEvonik Operations GmbHDarmstadtGermany

Amin Rostami‐HodjeganSimcyp DivisionCertara UK LtdSheffieldUK

Centre for Applied Pharmacokinetic ResearchSchool of Health SciencesUniversity of ManchesterManchesterUK

Alessandra RossiDepartment of Food and DrugUniversity of ParmaParmaItaly

Yvonne RosiauxGattefossé SASSaint PriestFrance

Farzaneh SalemSimcyp DivisionCertara UK LtdSheffieldUK

Harpreet SandhuBayer HealthCare Pharmaceuticals Inc.Whippany, NJUSA

Navnit ShahAmneal Pharmaceuticals LLCBridgewater, NJUSA

Aurélien SivertCapsugel/Lonza R&DStrasbourgFrance

Juri SolodenkoClinical PharmacometricsBayer AGLeverkusenGermany

Konstantina SouleleDepartment of PharmacyNational and KapodistrianUniversity of AthensAthensGreece

Donato TeutonicoClinical PharmacometricsBayer AG, LeverkusenGermany

Translational Medicine and Early DevelopmentSanofi R&DChilly‐MazarinFrance

Irena TomaszewskaPfizerPharmaceutical Sciences Small MoleculeSandwichUK

Ivana TomicTechnical R&DNovartis Pharma AGBaselSwitzerland

David B. TurnerSimcyp DivisionCertara UK LimitedSheffieldUK

Anna‐Lena UngellQuantitative Pharmacology and DMPKUCB Biopharma SPRLBraine‐l’AlleudBelgium

Ramana S. UppoorOffice of Clinical PharmacologyU.S. Food and Drug AdministrationSilver Spring, MDUSA

Siva Ram Kiran VakaAmneal Pharmaceuticals LLCBridgewater, NJUSA

Maria VertzoniDepartment of Pharmacy School of Health SciencesNational & Kapodistrian University of AthensAthens Greece

Randy WaldCapsugel/Lonza R&D Bend Oregon USA

Sara WrightEarly Patient Value MissionsUCB CelltechSloughUK

Hao ZhuOffice of Clinical PharmacologyU.S. Food and Drug AdministrationSilver Spring, MDUSA

Part IUnderstanding of Physiology and Anatomy – Factors Influencing Drug Release and Absorption from MR Formulations