LEADER 05743nam 2200589 450 001 9910639877503321 005 20230510220410.0 010 $a3-031-20025-X 035 $a(MiAaPQ)EBC7165772 035 $a(Au-PeEL)EBL7165772 035 $a(CKB)25913872000041 035 $a(PPN)267817142 035 $a(EXLCZ)9925913872000041 100 $a20230423d2023 uy 0 101 0 $aeng 135 $aurcnu|||||||| 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aRevising oral pharmacokinetics, bioavailability and bioequivalence based on the finite absorption time concept /$fPanos Macheras and Athanasios A. Tsekouras 210 1$aCham, Switzerland :$cSpringer,$d[2023] 210 4$d©2023 215 $a1 online resource (137 pages) 311 08$aPrint version: Macheras, Panos Revising Oral Pharmacokinetics, Bioavailability and Bioequivalence Based on the Finite Absorption Time Concept Cham : Springer International Publishing AG,c2023 9783031200243 320 $aIncludes bibliographical references. 327 $aIntro -- Foreword -- Preface -- Contents -- Part I: Oral Pharmacokinetics -- Chapter 1: From Bateman (1910) to Dost (1953) -- 1.1 Harry Bateman: First-Order Kinetics in Physics (1910) -- 1.2 Friedrich Hartmut Dost: First-Order Kinetics in Pharmacokinetics (1953) -- 1.3 Simulations Based on Bateman´s Equation -- 1.4 The Fundamental Metrics of Bioavailability/Bioequivalence Studies -- References -- Chapter 2: The Unphysical Hypothesis of Infinite Absorption Time -- 2.1 The Biopharmaceutical-Pharmacokinetic Basis of the Bateman Equation -- 2.2 State of the Art in Oral Drug Absorption -- 2.2.1 The PK Route -- 2.2.1.1 Questioning the Absorption Rate Constant, ka -- 2.2.1.2 PBPK Models -- 2.2.2 The Bioph Route -- 2.2.3 The Absorption Rate Constant (ka) Links the Bioph and PK Routes -- 2.3 The Unphysical Hypothesis of Infinite Absorption Time -- 2.4 Concluding Remarks -- References -- Chapter 3: The Finite Absorption Time (FAT) Concept -- 3.1 Sink Conditions Imply Zero-Order Kinetics -- 3.2 Finite Absorption Time -- 3.2.1 Modeling Work: Combining BCS with Absorption Kinetics -- 3.3 Simulations -- 3.3.1 Physiological Considerations -- 3.3.2 Drug Absorption: Reconsidered in Terms of the FAT -- 3.4 Fits to Data -- 3.5 Epilogue -- References -- Chapter 4: The Rise of Physiologically Based Finite Time Pharmacokinetic (PBFTPK) Models -- 4.1 Models -- 4.2 Simulations -- 4.3 Fits to Data -- 4.4 Toward a Biopharmaceutics-Pharmacokinetic Classification System (BPCS) -- 4.5 Future Work -- References -- Part II: Bioavailability-Bioequivalence -- Chapter 5: History of the Bioavailability-Bioequivalence Concepts -- 5.1 Early 1900s-Today: Variations in Response to Xenobiotics -- 5.2 1950s: The First Pharmacokinetic-Pharmacodynamic Correlations -- 5.3 1953: The Publication of Dost´s First Pharmacokinetics Book in History. 327 $a5.4 1960s: Biopharmaceutics-Pharmacokinetics at Its Infancy -- 5.5 ``The Bioavailability Problem´´ -- 5.6 The Introduction of an Official Dissolution Test in 1970 (USP Apparatus 1) -- 5.7 FDA (1977): Bioavailability Is the Rate and Extent to Which the Active Ingredient or Active Moiety Is Absorbed from a Drug... -- 5.7.1 A Persisting Problem: The Use of Cmax as a Metric of Rate of Absorption -- References -- Chapter 6: Therapeutic Equivalence Based on Bioequivalence Studies -- 6.1 From 1977 to Now: Bioequivalence Criteria and Issues -- 6.2 Highly Variable Drugs or Drug Products (HVD) -- 6.3 Epilogue -- References -- Chapter 7: Bioavailability Under the Prism of Finite Absorption Time -- 7.1 The Columbus´ Egg: Drug Absorption Takes Place Under Sink Conditions for Finite Time -- 7.2 A Paradigm Shift in Oral Drug Absorption -- 7.3 Bioavailability Parameters Under the Prism of Finite Absorption Time Concept -- 7.3.1 One Compartment Model with One Constant Input Rate Operating for Time ? -- 7.3.2 One Compartment Model with More than One Constant Input Rates Operating for a Total Time ? -- 7.3.3 One Compartment Model with First-Order Absorption Lasting for Time ? and First-Order Elimination -- 7.4 Extent (Exposure) and Rate Metrics -- 7.5 Extent and Rate of Absorption Metrics Under the Prism of Finite Absorption Time (FAT) -- 7.6 Scientific-Regulatory Implications -- 7.7 Toward the Unthinkable: Estimation of Absolute Bioavailability from Oral Data Exclusively -- References -- Chapter 8: Bioequivalence Under the Prism of Finite Absorption Time -- 8.1 Reconsidering Digoxin Bioavailability/Bioequivalence Studies in the Light of Finite Absorption Time Concept -- 8.2 Is the Proper Metric for Drug´s Extent of Absorption -- 8.3 Toward the Revision of Bioequivalence Assessment -- 8.4 Does FDA´s Bioavailability Definition of 1977 Require Reconsideration?. 327 $aReferences. 606 $aDrugs$xBioavailability 606 $aDrugs$xAbsorption and adsorption 606 $aOral medication 606 $aPharmacokinetics 606 $aBiological Availability 606 $aBiopharmaceutics 606 $aDrug Therapy 615 0$aDrugs$xBioavailability. 615 0$aDrugs$xAbsorption and adsorption. 615 0$aOral medication. 615 2$aPharmacokinetics. 615 2$aBiological Availability. 615 2$aBiopharmaceutics. 615 2$aDrug Therapy. 676 $a615.7 700 $aMacheras$b P$g(Panos),$01351088 702 $aTsekouras$b Athanasios A. 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910639877503321 996 $aRevising oral pharmacokinetics, bioavailability and bioequivalence based on the finite absorption time concept$93090580 997 $aUNINA