The physicochemical basis of pharmaceuticals / Humphrey A. Moynihan, Abina M. Crean.

Enhanced descriptions from Syndetics:

What are the physical and chemical properties that determine how a drug interacts with the body? What determines which dosage form is best, if it will reach its intended target, and how it will be metabolised once it has entered the body?The Physicochemical Basis of Pharmaceuticals explores the phenomena which affect the formulation and bio-availability of drug substances to give a straightforward, accessible treatment of the essential concepts affecting the absorption and distribution of drugs. It provides the reader with the conceptual 'tool-kit' necessary to understand the physicochemical aspects of drug design and action, and shows how these concepts apply in practice. The book introduces key underlying physical chemistry principles before exploring pharmaceutical solutions, the pharmaceutical solid phase, solid - liquid dispersal systems, biological interfaces, absorption, distribution, metabolism and excretion, to give a complete view of the field.Focusing at all times on the essential principles and concepts, The Physicochemical Basis of Pharmaceuticals avoids excessive detail, presenting the key facts, backed up with pertinent examples and easy-to-digest illustrations, making it the ideal primer for those who need to understand physicochemical issues in the context of their broader field of study.

Table of contents provided by Syndetics

• List of Abbreviations (p. xvii)
• 1 Pharmaceuticals and Medicines (p. 1)
• 1.1 Introduction to the essential properties of pharmaceuticals (p. 1)
• 1.1.1 Some key concepts (p. 2)
• 1.2 Classes of pharmaceutical compounds (p. 3)
• 1.2.1 Active pharmaceutical ingredients (p. 4)
• 1.2.2 Excipients (p. 7)
• 1.3 Drug delivery: getting the active pharmaceutical ingredient to the site of action (p. 8)
• 1.3.1 Routes of administration (p. 10)
• 1.3.2 Pharmaceutical dosage forms (p. 11)
• 1.3.3 Factors influencing dosage form choice (p. 18)
• 1.4 Summary (p. 20)
• References (p. 21)
• Further Reading (p. 21)
• 2 Pharmaceutical Solutions (p. 22)
• 2.1 Definitions and expressions of solubility (p. 22)
• 2.1.1 Measurement of solubility and solubility curves (p. 25)
• 2.2 Solvent structure (p. 27)
• 2.2.1 Hydrogen bonding and the structure of water (p. 27)
• 2.2.2 Lipid-based media (p. 29)
• 2.3 Dissolution and solvation (p. 31)
• 2.4 Factors affecting solubility (p. 34)
• 2.4.1 Molecular weight (p. 34)
• 2.4.2 Hydrogen bonding (p. 35)
• 2.4.3 Hydrophobic and hydrophilic groups (p. 36)
• 2.5 Acidity and basicity (p. 37)
• 2.5.1 pKa and pKb (p. 38)
• 2.5.2 Acidity and environment (p. 42)
• 2.5.3 Buffer solutions (p. 46)
• 2.6 Salt selection and formation (p. 48)
• 2.7 Hydrolytic degradation (p. 51)
• 2.8 Summary (p. 54)
• References (p. 55)
• Exercises (p. 55)
• 3 Pharmaceutical Equilibria (p. 56)
• 3.1 Essential concepts in thermodynamics (p. 58)
• 3.1.1 Internal energy, enthalpy and the first law of thermodynamics (p. 59)
• 3.1.2 Entropy and the second and third laws of thermodynamics (p. 62)
• 3.1.3 Free energy, chemical potential and equilibrium (p. 65)
• 3.2 Phase equilibria (p. 73)
• 3.2.1 One-component systems and the phase rule (p. 74)
• 3.2.2 Two-component systems (p. 78)
• 3.2.3 Three-component systems (p. 84)
• 3.3 Drug delivery: Phase transitions (p. 86)
• 3.3.1 Examples of phase transitions during drug delivery (p. 87)
• 3.3.2 Using phase transitions to understand drug delivery (p. 89)
• 3.3.3 Diffusion (molecular movement within a phase) (p. 91)
• 3.3.4 Dissolution (solid-liquid transition) (p. 93)
• 3.3.5 Partitioning (liquid-liquid transition) (p. 98)
• 3.3.6 Gas absorption (gas-liquid phase transition) (p. 100)
• 3.4 Summary (p. 102)
• References (p. 104)
• Further Reading (p. 104)
• Exercises (p. 104)
• 4 The Pharmaceutical Solid Phase (p. 106)
• 4.1 Crystalline and amorphous solids (p. 107)
• 4.2 The essentials of pharmaceutical crystal structure (p. 109)
• 4.2.1 Unit cells, crystal systems and lattices (p. 109)
• 4.2.2 Space groups and space-group notation (p. 112)
• 4.2.3 Crystal planes and faces (p. 117)
• 4.3 Crystal polymorphism of pharmaceuticals (p. 118)
• 4.3.1 Relative stabilities of polymorphs (p. 120)
• 4.3.2 Solvates and hydrates (p. 123)
• 4.4 Methods of characterizing pharmaceutical solids (p. 123)
• 4.4.1 X-ray diffraction methods (p. 124)
• 4.4.2 Thermal methods (p. 129)
• 4.4.3 Other methods of analysis (p. 133)
• 4.5 Pharmaceutical crystallization (p. 135)
• 4.5.1 Supersaturation (p. 135)
• 4.5.2 Nucleation, growth and crystal morphology (p. 137)
• 4.5.3 Ripening and the rule of stages (p. 138)
• 4.6 Solid-state properties of powder particles (p. 139)
• 4.6.1 Particle shape (p. 140)
• 4.6.2 Particle size (p. 141)
• 4.6.3 Particle-size measurement (p. 142)
• 4.6.4 Particle surface properties (p. 144)
• 4.6.5 Moisture adsorption (p. 150)
• 4.6.6 Particle mechanical strength (p. 151)
• 4.7 (p. 152)
• References (p. 154)
• Further Reading (p. 154)
• Exercises (p. 155)
• 5 The Theory of Disperse Systems (p. 156)
• 5.1 Drug distribution in pharmaceutical disperse systems (p. 158)
• 5.2 Molecular, colloidal and coarse disperse systems (p. 159)
• 5.3 The physical stability of disperse systems (p. 162)
• 5.4 Kinetic properties of disperse systems (p. 164)
• 5.4.1 Brownian motion (p. 164)
• 5.4.2 Sedimentation (p. 165)
• 5.5 Viscosity (p. 167)
• 5.5.1 Newtonian and non-Newtonian fluids (p. 169)
• 5.5.2 Colloidal dispersion viscosity (p. 172)
• 5.6 Interfacial properties (p. 174)
• 5.6.1 Interfacial tension (p. 175)
• 5.6.2 Interfacial free energy (p. 176)
• 5.6.3 Surfactants (p. 177)
• 5.6.4 Role of interfacial properties in emulsion formation (p. 181)
• 5.7 Electrical properties of disperse systems (p. 184)
• 5.7.1 Energies of repulsion and attraction-DLVO theory (p. 187)
• 5.8 Summary (p. 190)
• References (p. 191)
• Further Reading (p. 191)
• Exercises (p. 191)
• 6 Pharmaceutical Disperse Systems (p. 193)
• 6.1 Pharmaceutical suspensions (p. 193)
• 6.1.1 Factors that influence the stability of pharmaceutical suspensions (p. 195)
• 6.2 Pharmaceutical gels (p. 196)
• 6.2.1 Gel formation (p. 197)
• 6.2.2 Drug-loaded gel systems (p. 199)
• 6.2.3 Stability of pharmaceutical gels (p. 200)
• 6.3 Pharmaceutical emulsions (p. 200)
• 6.4 Pharmaceutical microemulsions (p. 202)
• 6.5 Pharmaceutical micellar systems (p. 202)
• 6.6 Pharmaceutical liposomes (p. 204)
• 6.7 Pharmaceutical aerosols (p. 208)
• 8.8 Pharmaceutical foams (p. 210)
• 6.9 Summary (p. 210)
• Further Reading (p. 211)
• 7 Drug Partitioning and Transport across Biological Barriers (p. 212)
• 7.1 Drug-receptor interactions (p. 213)
• 7.1.1 Types of drug receptor (p. 214)
• 7.1.2 Thermodynamics of drug-receptor interactions (p. 215)
• 7.2 Partitioning and partition coefficients (p. 216)
• 7.2.1 Log P values (p. 217)
• 7.3 Determination of partition coefficients (p. 220)
• 7.3.1 Experimental determination of log P (p. 220)
• 7.3.2 Computational determination of log P (p. 222)
• 7.4 Ionization and distribution coefficients (p. 224)
• 7.4.1 Distribution coefficients of zwitterionic compounds (p. 227)
• 7.5 Cellular and epithelial barriers (p. 228)
• 7.5.1 Cellular membrane structure (p. 228)
• 7.5.2 Epithelial barriers (p. 230)
• 7.6 Transport of drug molecules across cellular barriers (p. 232)
• 7.6.1 Paracellular transport (p. 232)
• 7.6.2 Transcellular transport (p. 233)
• 7.7 Transport of drug molecules in the systemic circulation (p. 235)
• 7.7.1 The structure of blood vessels (p. 235)
• 7.7.2 Drug transport across the blood/brain barrier (p. 236)
• 7.8 Gastrointestinal drug absorption (p. 237)
• 7.8.1 The small intestine (p. 238)
• 7.8.2 The large intestine (p. 239)
• 7.8.3 Challenges to drug absorption in the GI tract (p. 240)
• 7.9 The skin barrier (p. 242)
• 7.9.1 Structure of the skin (p. 242)
• 7.9.2 Transport of drug molecules across the skin (p. 244)
• 7.10 Other routes of drug administration (p. 245)
• 7.10.1 Drug absorption in the lungs (p. 245)
• 7.10.2 Drug absorption in the nasal cavity (p. 248)
• 7.10.3 Drug absorption in the oral cavity (p. 248)
• 7.11 Summary (p. 250)
• References (p. 252)
• Further Reading (p. 252)
• Exercises (p. 252)
• 8 Physicochemical Aspects of Pharmacokinetics (p. 255)
• 8.1 Absorption, distribution, metabolism and elimination (p. 256)
• 8.2 Bioavailability (p. 257)
• 8.3 Distribution (p. 259)
• 8.4 Drug metabolism (p. 263)
• 8.4.1 Phase I metabolism (p. 264)
• 8.4.2 Phase II metabolism (p. 266)
• 8.5 Excretion (p. 269)
• 8.5.1 Excretion processes (p. 269)
• 8.5.2 Pharmacokinetic aspects of elimination (p. 271)
• 8.6 Summary (p. 276)
• Further Reading (p. 277)
• Exercises (p. 277)
• A.1 Comprehensive List of Routes of Administration (p. 278)
• A.2 Brief Review of Logarithms (p. 280)
• A.3 Activities of Ions in Solution (p. 281)
• A.4 Osmotic Pressure (p. 284)
• A.5 Solutions to æEnd of ChapterÆ Exercises (p. 286)
• Glossary (p. 288)
• Index (p. 290)

Author notes provided by Syndetics