{"product_id":"oral-drug-delivery-for-modified-release-formulations-isbn-9781119772699","title":"Oral Drug Delivery for Modified Release Formulations","description":"\u003cb\u003eORAL DRUG DELIVERY FOR MODIFIED RELEASE FORMULATIONS\u003c\/b\u003e  \u003cp\u003e\u003cb\u003eProvides pharmaceutical development scientists with a detailed reference guide for the development of MR formulations\u003c\/b\u003e \u003c\/p\u003e\u003cp\u003e\u003ci\u003eOral Drug Delivery for Modified Release Formulations \u003c\/i\u003eis 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. \u003c\/p\u003e\u003cp\u003eDivided 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: \u003c\/p\u003e\u003cul\u003e\n\u003cli\u003eProvides authoritative coverage of physiology, physicochemical determinants, and in-vitro in-vivo correlation (IVIVC)\u003c\/li\u003e \u003cli\u003eExplains the different types of MR formulations and defines the key terms used in the field\u003c\/li\u003e \u003cli\u003eDiscusses the present status of MR technologies and identifies current gaps in research\u003c\/li\u003e \u003cli\u003eIncludes a summary of regulatory guidelines from both the US and the EU\u003c\/li\u003e \u003cli\u003eShares industrial experiences and perspectives on the evaluation of MR dosage formulations\u003c\/li\u003e\n\u003c\/ul\u003e  \u003cp\u003e\u003ci\u003eOral Drug Delivery for Modified Release Formulations\u003c\/i\u003e 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. \u003c\/p\u003e\u003cp\u003ePreface xvii\u003c\/p\u003e \u003cp\u003eList of Contributors xix\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart I Understanding of Physiology and Anatomy – Factors Influencing Drug Release and Absorption from MR Formulations 1\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003e1a Composition of Gastric Fluids Under Fasting and Fed Conditions 3\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eJens Van Den Abeele and Patrick Augustijns\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1a.1 Gastric Volume 3\u003c\/p\u003e \u003cp\u003e1a.2 Gastric Acid 3\u003c\/p\u003e \u003cp\u003e1a.3 Buffer Capacity 4\u003c\/p\u003e \u003cp\u003e1a.4 Mucus\/Viscosity 5\u003c\/p\u003e \u003cp\u003e1a.5 Enzymes 5\u003c\/p\u003e \u003cp\u003e1a.6 Surface Tension 6\u003c\/p\u003e \u003cp\u003e1a.7 Osmolality 6\u003c\/p\u003e \u003cp\u003e1a.8 Duodenogastric Reflux 7\u003c\/p\u003e \u003cp\u003e\u003cb\u003e1b Composition of the Small Intestinal Contents Under Fasting and Fed Conditions 11\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eEdmund S. Kostewicz\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1b.1 Small Intestinal Volume 11\u003c\/p\u003e \u003cp\u003e1b.2 pH Profile Along the Small Intestine 12\u003c\/p\u003e \u003cp\u003e1b.3 Composition of the Luminal Contents 12\u003c\/p\u003e \u003cp\u003e1b.4 Other Characteristics of Small Intestinal Fluids 14\u003c\/p\u003e \u003cp\u003e1b.5 Influence of Age, Gender, and Disease on the Small Intestinal Composition 15\u003c\/p\u003e \u003cp\u003e\u003cb\u003e1c The Luminal Environment in the Proximal Colon 19\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eMaria Vertzoni and Christos Reppas\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1c.1 Volume of Luminal Contents 19\u003c\/p\u003e \u003cp\u003e1c.2 Luminal pH Values 20\u003c\/p\u003e \u003cp\u003e1c.3 Buffer Capacity 22\u003c\/p\u003e \u003cp\u003e1c.4 Characteristics of Liquid Fraction of Contents 22\u003c\/p\u003e \u003cp\u003e1c.5 Concluding Remarks 22\u003c\/p\u003e \u003cp\u003e\u003cb\u003e2 Gastrointestinal Transit and Hydrodynamics Under Fasting and Fed Conditions 25\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eMirko Koziolek\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e2.1 Introduction 25\u003c\/p\u003e \u003cp\u003e2.2 Imaging Techniques Used for Assessment of Transit Times and Hydrodynamics 25\u003c\/p\u003e \u003cp\u003e2.3 Oral Cavity and Esophagus 25\u003c\/p\u003e \u003cp\u003e2.4 Stomach 26\u003c\/p\u003e \u003cp\u003e2.5 Small Intestine 29\u003c\/p\u003e \u003cp\u003e2.6 Large Intestine 31\u003c\/p\u003e \u003cp\u003e2.7 Whole Gut Transit Time 32\u003c\/p\u003e \u003cp\u003e2.8 Therapy- Related Effects on GI Transit 33\u003c\/p\u003e \u003cp\u003e2.9 Motility Disorders Affecting the GI Transit of Oral Dosage Forms 33\u003c\/p\u003e \u003cp\u003e2.10 Patient- Related Effects on GI Transit 34\u003c\/p\u003e \u003cp\u003e2.11 Conclusion 36\u003c\/p\u003e \u003cp\u003e\u003cb\u003e3 Intestinal Epithelium and Drug Transporters 39\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eKarelle Ménochet, Hugues Chanteux, Jamie Henshall, Jean- Marie Nicolas, Sara Wright, Judith van Asperen, and Anna-Lena Ungell\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e3.1 Introduction: Oral Drug Absorption General Mechanisms and Influencing Factors 39\u003c\/p\u003e \u003cp\u003e3.2 Expression of Drug Transporters in the Intestinal Epithelium 40\u003c\/p\u003e \u003cp\u003e3.3 Uptake Transporters Present at the Intestinal Level 40\u003c\/p\u003e \u003cp\u003e3.4 Regional Distribution of Uptake Transporters 42\u003c\/p\u003e \u003cp\u003e3.5 Efflux Transporters at the Intestinal Level 42\u003c\/p\u003e \u003cp\u003e3.6 Regional Distribution of Efflux Transporters 43\u003c\/p\u003e \u003cp\u003e3.7 Impact of the Regional Distribution of Enzymes and Transporters in the Intestine on the Enzyme\/Transporter Interplay 43\u003c\/p\u003e \u003cp\u003e3.8 Species Differences in Regional Expression of Uptake and Efflux Transporters 44\u003c\/p\u003e \u003cp\u003e3.9 Models for Regional Assessment of Intestinal Permeability 45\u003c\/p\u003e \u003cp\u003e3.10 Use of PBPK to Integrate Formulation and Permeation Knowledge 46\u003c\/p\u003e \u003cp\u003e3.11 Impact of Regional Solubility and Permeability Along the Intestine 47\u003c\/p\u003e \u003cp\u003e3.12 Formulation Excipients and Their Potential Modulatory Effects on Transporters 48\u003c\/p\u003e \u003cp\u003e3.13 Other Confounding Factors Affecting Drug Intestinal Absorption 51\u003c\/p\u003e \u003cp\u003e3.14 Drug–Drug Interactions 52\u003c\/p\u003e \u003cp\u003e3.15 Conclusion and Future Challenges 53\u003c\/p\u003e \u003cp\u003e\u003cb\u003e4 The Interplay Between Drug Release and Intestinal Gut- Wall Metabolism 65\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eAdam S. Darwich, Oliver J. Hatley, Andrés Olivares- Morales, Farzaneh Salem, Alison Margolskee, and Amin Rostami- Hodjegan\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e4.1 The Role of Gut Wall Metabolism in Determining Oral Bioavailability 65\u003c\/p\u003e \u003cp\u003e4.2 Factors Affecting Gut Wall Metabolism 69\u003c\/p\u003e \u003cp\u003e4.3 Preclinical and Clinical In Vivo and In Situ Models for Studying Intestinal Metabolism 71\u003c\/p\u003e \u003cp\u003e4.4 In Vitro Assays for Studying Intestinal Metabolism 72\u003c\/p\u003e \u003cp\u003e4.5 Models for Studying Bacterial Degradation 74\u003c\/p\u003e \u003cp\u003e4.6 In Vitro–In Vivo Extrapolation of Metabolic Clearance and In Silico Models for Predicting In Vivo Gut Wall Metabolism 75\u003c\/p\u003e \u003cp\u003e4.7 Oral Extended- Release Formulations and Gut Wall Metabolism 76\u003c\/p\u003e \u003cp\u003e4.8 Excipient Effects on Gut Wall Metabolism 77\u003c\/p\u003e \u003cp\u003e4.9 Considerations for Intestinal Metabolism in Special Populations 77\u003c\/p\u003e \u003cp\u003e4.10 Summary 79\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart II Design of MR Formulations – Considerations, Mechanisms and Technologies 87\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003e5 Preformulation Considerations for Design of Oral Modified- Release Products 89\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eChristel A. S. Bergström and René Holm\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e5.1 Introduction 89\u003c\/p\u003e \u003cp\u003e5.2 Purpose of MR Formulations 90\u003c\/p\u003e \u003cp\u003e5.3 Means to Obtain MR Drug Products 91\u003c\/p\u003e \u003cp\u003e5.4 Ionization Constant – pK a \u003ci\u003e93\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e5.5 Lipophilicity 93\u003c\/p\u003e \u003cp\u003e5.6 Solubility 93\u003c\/p\u003e \u003cp\u003e5.7 Chemical Stability 93\u003c\/p\u003e \u003cp\u003e5.8 Solid State Characterization 94\u003c\/p\u003e \u003cp\u003e5.9 Compatibility with Excipients 94\u003c\/p\u003e \u003cp\u003e5.10 Permeability and Metabolism 94\u003c\/p\u003e \u003cp\u003e5.11 Regional Absorption 95\u003c\/p\u003e \u003cp\u003e5.12 Microbial Stability 96\u003c\/p\u003e \u003cp\u003e5.13 Quality by Design (QbD) for MR formulations 97\u003c\/p\u003e \u003cp\u003e5.14 Conclusions 98\u003c\/p\u003e \u003cp\u003e\u003cb\u003e6 The Application of Biopharmaceutics Classification Systems to Modified- Release Formulations 103\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eJames M. Butler\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e6.1 Introduction 103\u003c\/p\u003e \u003cp\u003e6.2 The Use of Biopharmaceutics Classification Systems in Oral Drug Development 103\u003c\/p\u003e \u003cp\u003e6.3 The Application of Classification Systems to MR Drug Product Development – An Evidence- Based Approach 104\u003c\/p\u003e \u003cp\u003e6.4 Summary 114\u003c\/p\u003e \u003cp\u003e\u003cb\u003e7 Technologies and Mechanisms for Oral Modified Release by Monolithic and Multiparticulate Delivery Systems 119\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eGaia Colombo, Stavros Politis, and Alessandra Rossi\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e7.1 Introduction 119\u003c\/p\u003e \u003cp\u003e7.2 Mechanism of Drug Release 121\u003c\/p\u003e \u003cp\u003e7.3 Manufacturing Processes 124\u003c\/p\u003e \u003cp\u003e7.4 Formulation Screening and Characterization 128\u003c\/p\u003e \u003cp\u003e7.5 Conclusions and Perspectives 131\u003c\/p\u003e \u003cp\u003e\u003cb\u003e8 Lipid- based Formulations 137\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eJoseph P. O’Shea, Caitriona M. O’Driscoll, and Brendan T. Griffin\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e8.1 Introduction 137\u003c\/p\u003e \u003cp\u003e8.2 Mechanisms of Lipid- mediated Improvements in Bioavailability 138\u003c\/p\u003e \u003cp\u003e8.3 Lipid- based Formulations for Controlled Release 142\u003c\/p\u003e \u003cp\u003e8.4 Design of Lipid- based Formulations 144\u003c\/p\u003e \u003cp\u003e8.5 Formulation Screening and Characterization 146\u003c\/p\u003e \u003cp\u003e8.6 Industrial Considerations on LBF 154\u003c\/p\u003e \u003cp\u003e8.7 Emerging Applications of Lipid- based Formulations 154\u003c\/p\u003e \u003cp\u003e8.8 Conclusions 155\u003c\/p\u003e \u003cp\u003e\u003cb\u003e9 Strategies for MR Formulation Development: Mesoporous Silica 161\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eGeorgios K. Eleftheriadis, Eleni Kontogiannidou, Christina Karavasili, and Dimitrios G. Fatouros\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e9.1 Introduction 161\u003c\/p\u003e \u003cp\u003e9.2 Technologies 161\u003c\/p\u003e \u003cp\u003e9.3 Characterization 163\u003c\/p\u003e \u003cp\u003e9.4 Stability of Drug Carrier 165\u003c\/p\u003e \u003cp\u003e9.5 Silica- based Materials for the Modified Release of Poorly Soluble Drugs – In Vitro\/In Vivo Applications 166\u003c\/p\u003e \u003cp\u003e9.6 Toxicological Assessment 171\u003c\/p\u003e \u003cp\u003e9.7 Conclusions and Future Directions 173\u003c\/p\u003e \u003cp\u003e\u003cb\u003e10 Hot- Melt Extrusion Technology for Modified- Release (MR) Formulation Development 181\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eHarpreet Sandhu, Siva Ram Kiran Vaka, Dipen Desai, Paras Jariwala, Aruna Railkar, Wantanee Phuapradit, and Navnit Shah\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e10.1 Introduction 181\u003c\/p\u003e \u003cp\u003e10.2 HME Technology Overview 182\u003c\/p\u003e \u003cp\u003e10.3 General Considerations in Developing MR Dosage Forms Using HME Processing 185\u003c\/p\u003e \u003cp\u003e10.4 Material Considerations for MR- HME Application 187\u003c\/p\u003e \u003cp\u003e10.5 Dosage Form Design and Case Studies 189\u003c\/p\u003e \u003cp\u003e10.6 Characterization of HME Products 195\u003c\/p\u003e \u003cp\u003e10.7 Summary 200\u003c\/p\u003e \u003cp\u003e\u003cb\u003e11 Gattefosse: Strategies for MR Formulation Development – Lipids 205\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eYvonne Rosiaux, Vincent Jannin, and Cécile Morin\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e11.1 Introduction 205\u003c\/p\u003e \u003cp\u003e11.2 Lipids Used in SR Matrix 205\u003c\/p\u003e \u003cp\u003e11.3 Processing Lipid SR Matrix 206\u003c\/p\u003e \u003cp\u003e11.4 Understanding Drug Release from Lipid Matrix 208\u003c\/p\u003e \u003cp\u003e11.5 Characterizing Lipid SR Matrix 210\u003c\/p\u003e \u003cp\u003e11.6 Conclusions 211\u003c\/p\u003e \u003cp\u003e\u003cb\u003e12 Polymethacrylates for Modified- Release Formulations 215\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eMiriam Robota, Felix Hofmann, and Meike Pistner\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e12.1 Introduction 215\u003c\/p\u003e \u003cp\u003e12.2 Polymethacrylate Polymers and Their Application in Modified- Release Dosage Forms 215\u003c\/p\u003e \u003cp\u003e12.3 Protective Coatings 218\u003c\/p\u003e \u003cp\u003e12.4 Gastro- Resistant Coatings 221\u003c\/p\u003e \u003cp\u003e12.5 EUDRACAP Functional Ready-To-Fill Capsules for Fast Track Development of Sensitive Drugs 224\u003c\/p\u003e \u003cp\u003e12.6 Modified- Release Technology 224\u003c\/p\u003e \u003cp\u003e12.7 Modified- Release Formulations for Gastrointestinal Targeting 228\u003c\/p\u003e \u003cp\u003e12.8 Matrix Tablets as an Alternative to Modified- Release Multiparticulate Dosage Forms 231\u003c\/p\u003e \u003cp\u003e12.9 Alcohol- Resistant Formulation Concepts with EUDRAGIT® Polymers 232\u003c\/p\u003e \u003cp\u003e12.10 Conclusion 232\u003c\/p\u003e \u003cp\u003e\u003cb\u003e13 Strategies for Modified Release Oral Formulation Development 235\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eAurélien Sivert, Randy Wald, Chris Craig, and Hassan Benameur\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e13.1 Introduction 235\u003c\/p\u003e \u003cp\u003e13.2 Controlled- Release Drug Delivery Systems 235\u003c\/p\u003e \u003cp\u003e13.3 Dual- Release Drug Delivery Systems and Fixed- Dose Combination 242\u003c\/p\u003e \u003cp\u003e13.4 Site- Specific Drug Delivery Systems 243\u003c\/p\u003e \u003cp\u003e13.5 Conclusion\/Future Perspectives 249\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart III Evaluation of MR Formulations 253\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003e14 Dissolution Equipment and Hydrodynamic Considerations for Evaluating Modified- Release Behavior 255\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eSandra Klein\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e14.1 Introduction 255\u003c\/p\u003e \u003cp\u003e14.2 Compendial Dissolution Equipment 255\u003c\/p\u003e \u003cp\u003e14.3 USP Apparatus 7 – Reciprocating Holder 263\u003c\/p\u003e \u003cp\u003e14.4 Noncompendial Dissolution Equipment 264\u003c\/p\u003e \u003cp\u003e14.5 Summary and Conclusion 268\u003c\/p\u003e \u003cp\u003e\u003cb\u003e15 The Role and Applications of Dissolution Media for the Investigation of Modified-Release Formulations 273\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eCord J. Andreas and Edmund S. Kostewicz\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e15.1 Introduction 273\u003c\/p\u003e \u003cp\u003e15.2 Compendial Media 274\u003c\/p\u003e \u003cp\u003e15.3 Biorelevant Media 275\u003c\/p\u003e \u003cp\u003e15.4 Biphasic Dissolution Media 282\u003c\/p\u003e \u003cp\u003e15.5 Summary and Outlook 283\u003c\/p\u003e \u003cp\u003e\u003cb\u003e16 Biorelevant Dissolution Testing to Forecast the In Vivo Performance of Modified- Release Formulations 289\u003c\/b\u003e\u003cbr\u003e\u003ci\u003eMirko Koziolek\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e16.1 Introduction 289\u003c\/p\u003e \u003cp\u003e16.2 Factors Affecting the In Vivo Performance of MR Products 289\u003c\/p\u003e \u003cp\u003e16.3 Drug- Related Aspects 290\u003c\/p\u003e \u003cp\u003e16.4 Formulation- Related Aspects 290\u003c\/p\u003e \u003cp\u003e16.5 Biorelevant In Vitro Dissolution Test Methods 290\u003c\/p\u003e \u003cp\u003e16.6 General Remarks on Dissolution Media 290\u003c\/p\u003e \u003cp\u003e16.7 General Remarks on Dissolution Test Devices 291\u003c\/p\u003e \u003cp\u003e16.8 Dissolution Test Methods for the Simulation of Regional Transit Conditions 292\u003c\/p\u003e \u003cp\u003e16.9 Criteria for the Selection of a Suitable Biorelevant In Vitro Dissolution Method 299\u003c\/p\u003e \u003cp\u003e16.10 Conclusion 300\u003c\/p\u003e \u003cp\u003e\u003cb\u003e17 In Vitro and Ex Vivo Dissolution Tests for Considering Dissolution in the Lower Intestine 305\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eConstantinos Markopoulos and Maria Vertzoni\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e17.1 Introduction 305\u003c\/p\u003e \u003cp\u003e17.2 Dissolution Tests for pH- responsive Delivery Systems 306\u003c\/p\u003e \u003cp\u003e17.3 Dissolution Tests for Enzyme- triggered Delivery Systems 313\u003c\/p\u003e \u003cp\u003e17.4 Conclusion 319\u003c\/p\u003e \u003cp\u003e\u003cb\u003e18 Preclinical Evaluation – Animal Models to Evaluate MR Formulations 325\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eRené Holm\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e18.1 Introduction 325\u003c\/p\u003e \u003cp\u003e18.2 When to Use Nonclinical Models in the Development of Modified-release Formulations 325\u003c\/p\u003e \u003cp\u003e18.3 Physiological Factors in Animals Used to Investigate Modified- release Formulations 326\u003c\/p\u003e \u003cp\u003e18.4 Intestinal Site- specific Administration in Animals 330\u003c\/p\u003e \u003cp\u003e18.5 Evaluation of Modified- release Formulations in Animal Models 330\u003c\/p\u003e \u003cp\u003e18.6 Conclusions 334\u003c\/p\u003e \u003cp\u003e\u003cb\u003e19 In Vitro–In Vivo Correlations for Modified Release Formulations 341\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eIvana Tomic and Jean- Michel Cardot\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e19.1 Introduction 341\u003c\/p\u003e \u003cp\u003e19.2 Definitions of IVIVC 341\u003c\/p\u003e \u003cp\u003e19.3 Correlation Levels 341\u003c\/p\u003e \u003cp\u003e19.4 Considerations in IVIVC Development 342\u003c\/p\u003e \u003cp\u003e19.5 IVIVC Models 344\u003c\/p\u003e \u003cp\u003e19.6 Predictability of IVIVC 348\u003c\/p\u003e \u003cp\u003e19.7 Use of IVIVC 350\u003c\/p\u003e \u003cp\u003e19.8 Limitations of an IVIVC 352\u003c\/p\u003e \u003cp\u003e19.9 Conclusion 352\u003c\/p\u003e \u003cp\u003eAcknowledgment 353\u003c\/p\u003e \u003cp\u003eReferences 353\u003c\/p\u003e \u003cp\u003e\u003cb\u003e20 Application of the Simcyp Population- based PBPK Simulator to the Modelling of MR Formulations 355\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eNikunjkumar Patel, Shriram M. Pathak, and David B. Turner\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e20.1 Introduction 355\u003c\/p\u003e \u003cp\u003e20.2 The ADAM Oral Absorption Model 357\u003c\/p\u003e \u003cp\u003e20.3 Handling of Modified Release Formulations 358\u003c\/p\u003e \u003cp\u003e20.4 System Information 361\u003c\/p\u003e \u003cp\u003e20.5 MR Case Studies\/Examples 363\u003c\/p\u003e \u003cp\u003e20.6 Conclusion 370\u003c\/p\u003e \u003cp\u003e\u003cb\u003e21 PK- Sim for Modeling Oral Drug Delivery of Modified- Release Formulations 375\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eDonato Teutonico, Michael Block, Lars Kuepfer, Juri Solodenko, Thomas Eissing, and Katrin Coboeken\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e21.1 General Introduction on PK- Sim® and MoBi® 375\u003c\/p\u003e \u003cp\u003e21.2 Gastrointestinal Transit and Absorption Model 376\u003c\/p\u003e \u003cp\u003e21.3 Formulations Available in PK- Sim® 380\u003c\/p\u003e \u003cp\u003e21.4 Dissolved Form 380\u003c\/p\u003e \u003cp\u003e21.5 Zero and First- order Release and Lint80 Release 381\u003c\/p\u003e \u003cp\u003e21.6 Weibull 381\u003c\/p\u003e \u003cp\u003e21.7 Particle Dissolution 382\u003c\/p\u003e \u003cp\u003e21.8 Dissolution Media and Transit Times 383\u003c\/p\u003e \u003cp\u003e21.9 Case Studies 384\u003c\/p\u003e \u003cp\u003e21.10 Outlook 386\u003c\/p\u003e \u003cp\u003e\u003cb\u003e22 Clinical Evaluation – In Vivo Bioequivalence Assessment of MR Formulations 391\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eKonstantina Soulele and Panos Macheras\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e22.1 Introduction\/Historical Background 391\u003c\/p\u003e \u003cp\u003e22.2 Clinical Evaluation of New and Generic Modified- Release Formulations 392\u003c\/p\u003e \u003cp\u003e22.3 Summary 403\u003c\/p\u003e \u003cp\u003e\u003cb\u003e23 US Regulatory Considerations for Modified Release Products 409\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eHao Zhu, Ramana S. Uppoor, and Mehul Mehta\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e23.1 Introduction 409\u003c\/p\u003e \u003cp\u003e23.2 Clinical Development Programs for Nongeneric MR Dosage Forms 410\u003c\/p\u003e \u003cp\u003e23.3 Considerations for Clinical Development Programs for Generic MR Products 417\u003c\/p\u003e \u003cp\u003e23.4 Studies to Support Postapproval Changes for MR Products 418\u003c\/p\u003e \u003cp\u003e23.5 Summary 421\u003c\/p\u003e \u003cp\u003eDisclaimer 421\u003c\/p\u003e \u003cp\u003eReferences 422\u003c\/p\u003e \u003cp\u003e\u003cb\u003e24 Regulatory Assessment, European Perspective 425\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eMalin Filler and Anders Lindahl\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e24.1 Introduction 425\u003c\/p\u003e \u003cp\u003e24.2 Quality of Oral Extended- Release Products 425\u003c\/p\u003e \u003cp\u003e24.3 Quality by Design in Pharmaceutical Development 429\u003c\/p\u003e \u003cp\u003e24.4 Pharmacokinetic and Clinical Evaluation of Modified Release Dosage Forms 431\u003c\/p\u003e \u003cp\u003e24.5 Concluding Remarks 436\u003c\/p\u003e \u003cp\u003e\u003cb\u003e25 Industry Perspectives for the Evaluation of MR Formulations 439\u003cbr\u003e\u003c\/b\u003e\u003ci\u003eIrena Tomaszewska and Mark McAllister\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e25.1 Introduction 439\u003c\/p\u003e \u003cp\u003e25.2 Commercially Marketed MR Products – Historical Trends and Emerging Themes 439\u003c\/p\u003e \u003cp\u003e25.3 Early- stage MR Product Development 440\u003c\/p\u003e \u003cp\u003e25.4 Current Themes for Industrial MR Product Evaluation: (1) Dissolution Acceleration 444\u003c\/p\u003e \u003cp\u003e25.5 Current Themes for Industrial MR Product Evaluation: (2) Hydro- ethanolic Studies 447\u003c\/p\u003e \u003cp\u003e25.6 Conclusion 449\u003c\/p\u003e \u003cp\u003eReferences 449\u003c\/p\u003e \u003cp\u003eIndex 455\u003c\/p\u003e \u003cp\u003e\u003cb\u003eEdmund S. Kostewicz, PhD\u003c\/b\u003e is at the Fraunhofer Institute for Translational Medicine and Pharmacology in Frankfurt, Germany.\u003c\/p\u003e \u003cp\u003e\u003cb\u003eMaria Vertzoni, PhD\u003c\/b\u003e is an Assistant Professor of Pharmaceutical Technology and Biopharmaceutics at National and Kapodistrian University of Athens, Greece. \u003c\/p\u003e\u003cp\u003e\u003cb\u003eHeather A.E. Benson, PhD \u003c\/b\u003eis an adjunct Associate Professor at the Curtin Medical School, Curtin University, Australia, where she leads the Skin Delivery Research Group. \u003c\/p\u003e\u003cp\u003e\u003cb\u003eMichael S. Roberts, PhD \u003c\/b\u003eis a Professor of Therapeutics \u0026amp; Pharmaceutical Science at the University of South Australia, and a Professor of Clinical Pharmacology \u0026amp; Therapeutics at the University of Queensland, Australia.  \u003c\/p\u003e\u003cp\u003e\u003cb\u003eProvides pharmaceutical development scientists with a detailed reference guide for the development of MR formulations\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003ci\u003eOral Drug Delivery for Modified Release Formulations \u003c\/i\u003eis 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. \u003c\/p\u003e\u003cp\u003eDivided 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: \u003c\/p\u003e\u003cul\u003e\n\u003cli\u003eProvides authoritative coverage of physiology, physicochemical determinants, and in-vitro in-vivo correlation (IVIVC)\u003c\/li\u003e \u003cli\u003eExplains the different types of MR formulations and defines the key terms used in the field\u003c\/li\u003e \u003cli\u003eDiscusses the present status of MR technologies and identifies current gaps in research\u003c\/li\u003e \u003cli\u003eIncludes a summary of regulatory guidelines from both the US and the EU\u003c\/li\u003e \u003cli\u003eShares industrial experiences and perspectives on the evaluation of MR dosage formulations\u003c\/li\u003e\n\u003c\/ul\u003e  \u003cp\u003e\u003ci\u003eOral Drug Delivery for Modified Release Formulations\u003c\/i\u003e 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.\u003c\/p\u003e","brand":"Wiley","offers":[{"title":"Default Title","offer_id":47989724905701,"sku":"NP9781119772699","price":242.95,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/1842\/7735\/files\/9781119772699.jpg?v=1761785259","url":"https:\/\/k12savings.com\/es\/products\/oral-drug-delivery-for-modified-release-formulations-isbn-9781119772699","provider":"K12savings","version":"1.0","type":"link"}