Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water-Soluble Drugs (Drugs and the Pharmaceutical Sciences)

Oral lipid-based formulations are attracting considerable attention due to their capacity to facilitate gastrointestinal absorption and reduce or eliminate the effect of food on the absorption of poorly water-soluble, lipophilic drugs. Despite the obvious and demonstrated utility of these formulations for addressing a persistent and growing problem of major significance, the pharmaceutical industry has been slow to apply and further develop this technology. This title provides a comprehensive summary of the theoretical and practical aspects of oral lipid-based formulations for use in industry, and provides further insights into a developing technology expected to assume increasing prominence in years to come. Front cover 1 Preface 18 Contents 20 Contributors 22 Chapter 1. Currently Marketed Oral Lipid-Based Dosage Forms: Drug Products and Excipients 24 Chapter 2. Lipid-Based Excipients for Oral Drug Delivery 56 Chapter 3. Feasibility Assessment and Considerations for Scaling Initial Prototype Lipid-Based Formulations to Phase I/II Clinical Trial Batches 86 Chapter 4. Materials, Process, and Manufacturing Considerations for Lipid-Based Hard-Capsule Formats 102 Chapter 5. Liquid Self-Microemulsifying Drug Delivery Systems 130 Chapter 6. Lipid-Based Isotropic Solutions: Design Considerations 152 Chapter 7. Lipid-Based Self-Emulsifying Solid Dispersions 172 Chapter 8. Oral Lipid-Based Formulations: Using Preclinical Data to Dictate Formulation Strategies for Poorly Water-Soluble Drugs 208 Chapter 9. Physiological Processes Governing the Gastrointestinal Absorption of Lipids and Lipophilic Xenobiotics 230 Chapter 10. Characterizing Release from Lipid-Based Formulations 264 Chapter 11. Using In Vitro Dynamic Lipolysis Modeling as a Tool for Exploring IVIVC Relationships for Oral Lipid-Based Formulations 280 Chapter 12. Case Studies: Rational Development of Self-Emulsifying Formulations for Improving the Oral Bioavailability of Poorly Soluble, Lipophilic Drugs 296 Chapter 13. Design and Development of Supersaturatable Self-Emulsifying Drug Delivery Systems for Enhancing the Gastrointestinal Absorption of Poorly Soluble Drugs 326 Index 352 Back cover 370 Currently marketed oral lipid-based dosage forms : drug products and excipients / Robert Strickley Feasibility assessment for scaling bench-top prototype lipid-based formulations to initial phase I/II clinical trial batches / Paul Sirois Lipid-based excipients for oral drug delivery / Lowell Gibson Process and manufacturing considerations and final characterization of oral lipid-based formulations / Bill Bowtie Liquid self-micro-emulsifying drug delivery systems (SMEDDS) / Annette Mullertz Lipid based isotropic solutions : design considerations / Navnit Shah Lipid-based self-emulsifying solid dispersions / Abu Serajuddin Preclinical in vivo evaluation of oral lipid-based formulations / Chris Porter, Bill Charman Physiological processes governing the gastrointestinal absorption of lipids and lipophilic xenobiotics / Patrick Tso Characterizing release from lipid-based formulations / Jennifer Dressman Using in vitro dynamic lipolysis modeling as a tool for exploring IVIVC relationships for oral lipid-based formulations / Annette Mullertz Case study: rational development of self-emulsifying formulations for improving the oral bioavailability of poorly soluble, lipophilic drugs / Ping Gao Design and development of supersaturatable SEDDS (S-SEDDS) formulations for enhancing the gastrointestinal absorption of poorly soluble drugs / Ping Gao.