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Drug bioavailability [[electronic resource] ] : estimation of solubility, permeability, absorption and bioavailability / / edited by Han van de Waterbeemd, Hans Lennernäs and Per Artursson
| Drug bioavailability [[electronic resource] ] : estimation of solubility, permeability, absorption and bioavailability / / edited by Han van de Waterbeemd, Hans Lennernäs and Per Artursson |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH, c2003 |
| Descrizione fisica | 1 online resource (605 p.) |
| Disciplina |
615.1
615.19 615/.7 |
| Altri autori (Persone) |
WaterbeemdHan van de
LennernäsHans ArturssonPer |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Drugs - Bioavailability
Drugs - Solubility |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-280-52024-8
9786610520244 3-527-60515-0 3-527-60147-3 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Drug Bioavailability Estimation of Solubility, Permeability, Absorption and Bioavailability; Contents; Preface; Foreword; List of Authors; I Studies of Membrane Permeability and Oral Absorption; 1 Physico-chemical Approaches to Drug Absorption; Abbreviations; Symbols; 1.1 Introduction; 1.2 Drug-like Properties; 1.3 Dissolution and Solubility; 1.3.1 Calculated Solubility; 1.4 Ionization (pK(a)); 1.5 Lipophilicity; 1.5.1 Calculated log P; 1.6 Molecular Size and Shape; 1.6.1 Calculated Size Descriptors; 1.7 Hydrogen Bonding; 1.7.1 Calculated Hydrogen-Bonding Descriptors; 1.8 Amphiphilicity
1.9 Permeability1.9.1 Artificial Membranes; 1.9.2 IAM, ILC, MEKC, and BMC; 1.9.3 Liposome Partitioning; 1.9.4 Biosensors; 1.9.5 Ghost Erythrocytes and Diffusion Constants; References; 2 High-throughput Measurement of log D and pK(a); Abbreviations; Symbols; 2.1 Introduction; 2.2 Relationship between Ionization and Lipophilicity; 2.3 Measuring log D; 2.3.1 Shake-flask Method; 2.3.2 pH-metric Method; 2.3.3 Direct Chromatographic Methods; 2.3.3.1 Chromatographic Hydrophobicity Index (CHI); 2.3.3.2 Microemulsion Electrokinetic Chromatography (MEEKC) 2.3.3.3 Chromatography in the Presence of Octanol2.3.3.4 Reversed-Phase Chromatography; 2.3.3.5 Liquid-Liquid Partition Chromatography; 2.4 Measuring pK(a); 2.4.1 Review of Methods; 2.4.2 The Effect of Co-solvents on pK(a); 2.4.3 pH-Metric Titration; 2.4.4 Hybrid pH-Metric/UV Method; 2.4.5 Other Methods; 2.4.6 pH Gradient Titration; 2.5 Some Thoughts about High-throughput Analytical Chemistry; Acknowledgments; References; 3 High-throughput Measurement of Permeability Profiles; Abbreviations; Symbols; 3.1 Introduction 3.2 Key Historical Developments in Artificial-Membrane Permeability Measurement3.3 The Ideal in vitro Artificial Membrane Permeability Model; 3.3.1 Lipid Compositions in Biological Membranes; 3.3.2 Permeability-pH Considerations; 3.3.3 Role of Serum Proteins; 3.3.4 Effects of Cosolvents, Bile Acids, and other Surfactants; 3.3.5 Components of the Ideal; 3.4 New Directions in PAMPA; 3.4.1 Concentrated and Charged Phospholipid Membranes; 3.4.2 Gradient-pH Permeability Equation; 3.4.3 Permeability Measurements: High-phospholipid in Surfactant-free Solutions 3.4.4 Membrane Retention Measurements: High-phospholipid in Surfactant-free Solutions3.4.5 Egg Lecithin and the Degree of Negative Charge; 3.4.6 Summary: Increasing Phospholipid Content in the Absence of Sink Conditions; 3.4.7 Effects of Surfactant on High-phospholipid Membrane Permeability and Retention; 3.4.8 Quality and Usefulness of the UV Spectra; 3.4.9 Iso-pH and Gradient-pH Mapping in 2% DOPC-Dodecane; 3.4.10 Iso-pH Mapping in 20% Soy Lecithin-Dodecane, with Surfactant 3.4.11 Predictions of in vivo Human Jejunal Permeabilities using the Improved 20% Soy Lecithin with Surfactant in vitro PAMPA Technique |
| Record Nr. | UNINA-9910146243203321 |
| Weinheim, : Wiley-VCH, c2003 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Drug bioavailability : estimation of solubility, permeability, absorption and bioavailability / / edited by Han van de Waterbeemd, Hans Lennernäs and Per Artursson
| Drug bioavailability : estimation of solubility, permeability, absorption and bioavailability / / edited by Han van de Waterbeemd, Hans Lennernäs and Per Artursson |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH, c2003 |
| Descrizione fisica | 1 online resource (605 p.) |
| Disciplina |
615.1
615.19 615/.7 |
| Altri autori (Persone) |
WaterbeemdHan van de
LennernäsHans ArturssonPer |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Drugs - Bioavailability
Drugs - Solubility |
| ISBN |
1-280-52024-8
9786610520244 3-527-60515-0 3-527-60147-3 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Drug Bioavailability Estimation of Solubility, Permeability, Absorption and Bioavailability; Contents; Preface; Foreword; List of Authors; I Studies of Membrane Permeability and Oral Absorption; 1 Physico-chemical Approaches to Drug Absorption; Abbreviations; Symbols; 1.1 Introduction; 1.2 Drug-like Properties; 1.3 Dissolution and Solubility; 1.3.1 Calculated Solubility; 1.4 Ionization (pK(a)); 1.5 Lipophilicity; 1.5.1 Calculated log P; 1.6 Molecular Size and Shape; 1.6.1 Calculated Size Descriptors; 1.7 Hydrogen Bonding; 1.7.1 Calculated Hydrogen-Bonding Descriptors; 1.8 Amphiphilicity
1.9 Permeability1.9.1 Artificial Membranes; 1.9.2 IAM, ILC, MEKC, and BMC; 1.9.3 Liposome Partitioning; 1.9.4 Biosensors; 1.9.5 Ghost Erythrocytes and Diffusion Constants; References; 2 High-throughput Measurement of log D and pK(a); Abbreviations; Symbols; 2.1 Introduction; 2.2 Relationship between Ionization and Lipophilicity; 2.3 Measuring log D; 2.3.1 Shake-flask Method; 2.3.2 pH-metric Method; 2.3.3 Direct Chromatographic Methods; 2.3.3.1 Chromatographic Hydrophobicity Index (CHI); 2.3.3.2 Microemulsion Electrokinetic Chromatography (MEEKC) 2.3.3.3 Chromatography in the Presence of Octanol2.3.3.4 Reversed-Phase Chromatography; 2.3.3.5 Liquid-Liquid Partition Chromatography; 2.4 Measuring pK(a); 2.4.1 Review of Methods; 2.4.2 The Effect of Co-solvents on pK(a); 2.4.3 pH-Metric Titration; 2.4.4 Hybrid pH-Metric/UV Method; 2.4.5 Other Methods; 2.4.6 pH Gradient Titration; 2.5 Some Thoughts about High-throughput Analytical Chemistry; Acknowledgments; References; 3 High-throughput Measurement of Permeability Profiles; Abbreviations; Symbols; 3.1 Introduction 3.2 Key Historical Developments in Artificial-Membrane Permeability Measurement3.3 The Ideal in vitro Artificial Membrane Permeability Model; 3.3.1 Lipid Compositions in Biological Membranes; 3.3.2 Permeability-pH Considerations; 3.3.3 Role of Serum Proteins; 3.3.4 Effects of Cosolvents, Bile Acids, and other Surfactants; 3.3.5 Components of the Ideal; 3.4 New Directions in PAMPA; 3.4.1 Concentrated and Charged Phospholipid Membranes; 3.4.2 Gradient-pH Permeability Equation; 3.4.3 Permeability Measurements: High-phospholipid in Surfactant-free Solutions 3.4.4 Membrane Retention Measurements: High-phospholipid in Surfactant-free Solutions3.4.5 Egg Lecithin and the Degree of Negative Charge; 3.4.6 Summary: Increasing Phospholipid Content in the Absence of Sink Conditions; 3.4.7 Effects of Surfactant on High-phospholipid Membrane Permeability and Retention; 3.4.8 Quality and Usefulness of the UV Spectra; 3.4.9 Iso-pH and Gradient-pH Mapping in 2% DOPC-Dodecane; 3.4.10 Iso-pH Mapping in 20% Soy Lecithin-Dodecane, with Surfactant 3.4.11 Predictions of in vivo Human Jejunal Permeabilities using the Improved 20% Soy Lecithin with Surfactant in vitro PAMPA Technique |
| Record Nr. | UNINA-9910877382003321 |
| Weinheim, : Wiley-VCH, c2003 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Formulating poorly water soluble drugs / / edited by Robert O. Williams, Daniel A. Davis, and Dave A. Miller
| Formulating poorly water soluble drugs / / edited by Robert O. Williams, Daniel A. Davis, and Dave A. Miller |
| Edizione | [Third edition.] |
| Pubbl/distr/stampa | Cham, Switzerland : , : Springer, , [2022] |
| Descrizione fisica | 1 online resource (701 pages) |
| Disciplina | 615.19 |
| Collana | AAPS Advances in the Pharmaceutical Sciences |
| Soggetto topico |
Drugs - Solubility
Drug development |
| ISBN | 3-030-88719-7 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Intro -- Preface -- Contents -- 1: Route-Specific Challenges in the Delivery of Poorly Water-Soluble Drugs -- 1.1 Introduction -- 1.2 Oral Route of Administration -- 1.2.1 Challenges in Oral Delivery of Poorly Water-Soluble Drugs -- 1.3 Parenteral Route of Administration -- 1.3.1 Challenges in Parenteral Delivery of Poorly Water-Soluble Drugs -- 1.4 Ocular Route of Administration -- 1.4.1 Challenges in Ocular Delivery of Poorly Water-Soluble Drugs -- 1.5 Nasal Route of Administration -- 1.5.1 Challenges in Nasal Delivery of Poorly Water-Soluble Drugs -- 1.6 Pulmonary Route of Administration -- 1.6.1 Challenges in Pulmonary Delivery of Poorly Water-Soluble Drugs -- 1.7 Summary -- References -- 2: Optimizing the Formulation of Poorly Water-Soluble Drugs -- 2.1 Introduction -- 2.1.1 Solubility Studies -- Solubility Prediction -- 2.1.2 Experimental Aqueous Solubility Determination -- Solubility Measurement on Amorphous Drugs and Limited Amounts of Materials Using Single Particle Analysis -- 2.1.3 pH-Solubility Profiles -- 2.1.4 Solubility Prediction Using Machine and Deep Learning -- 2.1.5 Intrinsic Dissolution -- Compact Preparation -- Intrinsic Dissolution Testing -- 2.2 Solid-State Characterization -- 2.2.1 Thermal Analysis -- Differential Scanning Calorimetry -- Parameter Selection Method -- Thermal Events -- Polymorphic Transformations -- Drug-Excipient Interactions -- Flory-Huggins -- Thermogravimetric Analysis -- Thermal Decomposition -- Excipient Interactions -- Dynamic Mechanical Analysis (DMA) -- 2.2.2 Fourier Transform Infrared Spectroscopy and Raman Spectroscopy -- Sample Preparation -- Polymorph Screening -- Excipient Interactions -- 2.2.3 X-Ray Diffraction -- Parameter Selection -- Polymorph Screening -- Excipient Interactions -- Pair Distribution Function (PDF) -- 2.2.4 Atomic Force Microscopy (AFM) -- 2.2.5 Specific Surface Area.
BET Surface Area Analysis -- Sample Preparation -- Sample Analysis -- 2.2.6 Solid-State Nuclear Magnetic Resonance (ssNMR) -- 2.2.7 Residual Solvent Analysis -- Residual Solvent Guidelines -- Analytical Determination of Residual Solvent Levels -- 2.3 Stability Testing -- 2.3.1 Stability Monitoring -- 2.3.2 Chemical Stability -- 2.3.3 Stability Testing Conditions -- 2.3.4 Predicting Stability Using Machine and Deep Learning -- 2.4 Dissolution Testing -- 2.4.1 Dissolution Studies -- Sample Handling -- Excipient Screening for Supersaturation Maintenance Ability -- Supersaturation Dissolution Studies -- Alternative Dissolution Studies -- Predicting Dissolution Performance Using Machine and Deep Learning -- 2.4.2 In Vivo Testing -- Administration via Inhalation -- Oral Administration -- 2.5 Conclusions -- References -- 3: Solid-State Techniques for Improving Solubility -- 3.1 Introduction -- 3.2 Pharmaceutical Salts -- 3.2.1 Pharmaceutical Salt Selection -- 3.2.2 Solubility Enhancement -- 3.3 Polymorphs and Amorphous Forms -- 3.3.1 Polymorph Preparation -- 3.3.2 Amorphous Form Preparation -- Glass-Forming Ability -- Determination of Glass-Forming Ability -- The Importance of Glass-Forming Ability -- 3.3.3 Thermodynamics of Metastable Solids -- 3.3.4 Solubility and Bioavailability Enhancement -- 3.4 Pharmaceutical Cocrystals -- 3.4.1 Cocrystal Preparation -- 3.4.2 Solubility of Cocrystals -- 3.5 Summary -- References -- 4: Mechanical Particle-Size Reduction Techniques -- 4.1 Introduction -- 4.2 Rationale Behind the Reduction of Particle Size -- 4.3 Milling -- 4.3.1 Dry Milling -- Fluidized Bed Jet Milling -- Spiral Jet ``Pancake´´ Mill -- Geometry Dependence -- Nozzle Dependence -- Working Conditions -- Pin Mill -- Environmental Limitations of Dry Milling -- 4.3.2 Wet Milling -- Rotor-Stator Wet Milling -- Media (Bead) Wet Milling -- Cryogenic Milling. 4.4 High-Pressure Homogenization Techniques -- 4.4.1 Piston-Gap Homogenizers -- 4.4.2 Microfluidizer -- 4.5 Combination of Top-Down and Bottom-Up in a Single Process for the Manufacture of Drug Nanosuspensions -- 4.5.1 NANOEDGE -- 4.5.2 smartCrystal Technology -- H 69 Technology -- H 42 Technology -- H 96 Technology -- 4.5.3 CT Technology -- 4.6 Conclusion -- References -- 5: Cosolvent and Complexation Systems -- 5.1 Introduction -- 5.2 Theoretical Modeling of Solubility in Cosolvents -- 5.3 Oral Absorption of Drug Substances -- 5.4 Cosolvent-Based Formulations -- 5.4.1 Development of Cosolvent-Based Solubilized Formulations -- 5.5 Polyethylene Glycol-Based Solid Dispersion -- 5.5.1 Development of PEG-Based Solubilized Formulations -- 5.5.2 Fusion Method for the Preparation of Solid Dispersion -- 5.5.3 Solvent Method for the Preparation of PEG Dispersion -- 5.6 Other Solubilized Systems -- 5.6.1 Drug-Cyclodextrins Complex -- Complexation Techniques -- 5.6.2 Self-Emulsifying Formulation -- 5.6.3 Amorphous Solid Dispersion in Polymer Matrices -- 5.7 Dosage Form Manufacturing of Solubilized Formulations -- 5.7.1 Soft Gelatin Capsule -- 5.7.2 Hard Gelatin Capsules -- 5.7.3 Spray Congealing -- 5.7.4 Fluidized Bed Melt Granulation -- 5.7.5 Powered Solution Technology -- 5.8 Summary -- References -- 6: Injectable Formulations of Poorly Water-Soluble Drugs -- 6.1 Introduction -- 6.2 Target Product Profile -- 6.3 Routes of Administration -- 6.3.1 Intravenous -- 6.3.2 Subcutaneous -- 6.3.3 Intramuscular -- 6.3.4 Intrathecal -- 6.3.5 Intra-Articular -- 6.3.6 Other Injectable Routes -- 6.4 Formulation Considerations for Injectable Products -- 6.4.1 pH -- 6.4.2 Buffer Systems -- 6.4.3 Tonicity and Biological Implications -- 6.4.4 Sterility and Endotoxin Requirements -- 6.4.5 Particulate Matter -- 6.4.6 Preservatives -- 6.4.7 Device and Diluent Compatibility. 6.4.8 Packaging and Manufacturing Considerations -- 6.5 Vehicle Selection and Solubilization -- 6.5.1 pH Adjustment -- 6.5.2 Salt Formation -- 6.5.3 Cosolvents -- 6.5.4 Surfactants -- 6.5.5 Cyclodextrins -- 6.5.6 Nonaqueous and Oily Vehicles -- 6.6 Dispersed Systems -- 6.6.1 Emulsions -- 6.6.2 Coarse Suspensions -- 6.6.3 Liposomes and Other Colloidal Systems -- Liposomes -- Nanosuspensions -- Nanoparticles -- Micelles -- 6.6.4 Hydrogels and In-Situ Implants -- 6.7 Strategies for Improving Stability -- 6.7.1 Addition of Stabilizing Excipients -- 6.7.2 Adjustment in Processing Techniques -- 6.8 Injectable Product Development Workflow -- References -- Capsule References -- 7: Lipid-Based Formulations -- 7.1 Introduction -- 7.2 Classification and Components of Lipid-Based Formulations -- 7.2.1 Triglycerides and Mixed Glycerides -- 7.2.2 Surfactants -- 7.2.3 Hydrophilic Cosolvents -- 7.3 Characterization of Lipid-Based Formulations -- 7.3.1 Solubility -- 7.3.2 Dispersion and Digestion Testing -- 7.3.3 In Vivo Characterization -- 7.4 Solid Lipid-Based Formulations-A Current Trend in Lipid-Based Formulation Design -- 7.4.1 Solid Lipid Nanoparticle (SLN) -- 7.5 Conclusion -- References -- 8: Structured Development Approach for Amorphous Systems -- 8.1 Introduction -- 8.2 Ideal Amorphous Formulation: Structured Development -- 8.3 Initial Assessment -- 8.3.1 Initial Assessment in Terms of Bioavailability -- 8.3.2 Initial Assessment in Terms of Stability -- 8.3.3 Initial Assessment in Terms of Manufacturability -- 8.4 Polymer Screening: Part I (Theoretical) -- 8.4.1 Assessing the Miscibility of Drug and Polymer -- Solubility Parameters -- Glass Transition Temperature -- Prediction of Phase Diagrams -- 8.4.2 Specific Interactions -- 8.4.3 Hygroscopicity and Water Activity -- 8.4.4 Further Restriction of Polymers Based on the Manufacturing Technology. 8.4.5 Summary of Initial Assessment -- 8.5 Miniaturized Methods for ASD Screening -- 8.5.1 Supersaturation Screening -- 8.5.2 Solid-State Screening -- 8.5.3 The SPADS (Screening of Polymers for Amorphous Drug Stabilization) Approach: Example for a Combined ASD Screening Approa... -- 8.5.4 Summary of the Small-Scale Experiments: Selection of Polymer and Drug Load -- 8.6 Selection of Most Suitable Technology -- 8.6.1 Overview of Key Manufacturing Technologies -- Spray Drying -- Hot-Melt Extrusion -- Coprecipitation -- 8.7 Downstream Processing and Final Product Properties -- 8.8 Characterization of the Amorphous Systems -- 8.8.1 Detection of Crystallinity in Amorphous System -- X-Ray Powder Diffraction -- IR and Raman Spectroscopy -- Differential Scanning Calorimetry -- Microscopic Technique -- Other Techniques -- 8.8.2 Determination of Molecular Arrangement in Amorphous Systems -- Differential Scanning Calorimetry -- (N)IR and Raman Spectroscopy -- Atomic Force Microscopy -- Solid-State NMR -- Other Techniques -- 8.8.3 Dissolution Method for Amorphous Formulations -- 8.8.4 Stability Prediction -- 8.9 Overall Summary -- References -- 9: Melt Extrusion -- 9.1 Introduction -- 9.2 Equipment Design and Engineering Principles -- 9.2.1 Basic Equipment Description -- Feeders -- 9.2.2 Melt Extrusion Processing -- Steady-State Processing and Production Feedback -- Importance of Specific Mechanical Energy in Melt Extrusion -- Processing Regimes for Pharmaceutical Melt Extrusion -- 9.2.3 Distributive and Dispersive Mixing in HME -- 9.3 Formulation Design for Melt-Extruded Dispersions -- 9.3.1 Preformulation Assessment to Support Hot-Melt Extrusion -- 9.3.2 Assessing Formulation Performance During Early Development -- Manufacturability -- Solid-State Characterization of Melt-Extruded Amorphous Dispersions -- Stability -- Drug-Polymer Incompatibilities. Bioavailability. |
| Record Nr. | UNINA-9910574080603321 |
| Cham, Switzerland : , : Springer, , [2022] | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Mixing Tamiflu® with sweet liquids [[electronic resource]]
| Mixing Tamiflu® with sweet liquids [[electronic resource]] |
| Pubbl/distr/stampa | Atlanta, GA : , : Centers for Disease Control and Prevention, , [2009] |
| Soggetto topico |
Antiviral agents
Pediatric oral medicine Oral medication Capsules (Pharmacy) Drugs - Solubility Influenza - Treatment Swine influenza - Treatment |
| Soggetto genere / forma |
Documentary films.
Streaming videos. |
| Formato | Videoregistrazioni  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Record Nr. | UNINA-9910699216903321 |
| Atlanta, GA : , : Centers for Disease Control and Prevention, , [2009] | ||
| Videoregistrazioni | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
