Physicochemical Principles of Pharmacy : In Manufacture, Formulation and Clinical Use.
Florence, Alexander T.
Physicochemical Principles of Pharmacy : In Manufacture, Formulation and Clinical Use. - 6th ed. - 1 online resource (665 pages)
Intro -- Contents -- Preface -- About the authors -- Introduction -- Physical chemistry and pharmacy -- The clinical relevance of physical pharmacy: clinical pharmaceutics -- Adjuvants or excipients -- Arrangement of the book -- Objectives -- 'Reading' structures and formulae -- Chemical structures -- Physical equations -- 1 Solids -- 1.1 Classification of solids -- 1.2 Crystalline solids: structure and properties -- 1.2.1 Crystal structure -- Miller indices -- 1.2.2 Crystal form -- Crystallisation and factors affecting crystal form2 -- Precipitation -- Habit modification -- 1.2.3 Polymorphism4 -- Pharmaceutical implications of polymorphism -- Transformations -- Analytical issues -- Consequences -- 1.2.4 Multicomponent crystals -- Crystal hydrates and solvates -- Pharmaceutical consequences of solvate formation -- Cocrystals -- 1.3 Amorphous solids -- 1.4 Dissolution of solid drugs -- 1.5 Biopharmaceutical importance of particle size -- 1.6 Wetting of powders -- 1.6.1 Contact angle and wettability of solid surfaces -- 1.6.2 Wettability of powders -- 1.7 Freeze drying -- 1.8 Solid-dosage forms: formulation and manufacture -- 1.8.1 Excipients -- Filler/diluent -- Disintegrants -- Binders -- Lubricants -- Glidants -- Flavouring agents and colourants -- 1.8.2 Powder flow -- 1.8.3 Particle size reduction -- 1.8.4 Powder mixing and demixing -- 1.8.5 Granulation -- Wet granulation -- Stage 1: Granule formation -- Extrusion/spheronisation techniques -- Bonding mechanisms in wet granulation -- Stage 2: Drying and milling -- Dry granulation -- Bonding mechanisms in dry granulation -- 1.8.6 Tablet manufacture -- Compression and compaction of powders -- The compression process -- Mechanisms of compression -- Tablet coating -- Film coating -- Film-coating formulations -- Solvent -- Polymer -- Plasticiser -- Colourant -- Surfactant -- Film-coating techniques. Drum or pan coating -- Fluidised-bed coating -- Dry coating -- Liquid-assisted coating -- Thermal adhesion -- Electrostatic coating -- 1.8.7 Capsule manufacture -- Chemical and physicochemical properties of gelatin -- Hard-capsule manufacture and filling -- Manufacture -- Filling of powder formulations -- Filling of pellets and tablets -- Filling of liquids and semisolids -- Soft gelatin (softgel) capsule manufacture and filling -- Manufacture and filling -- 1.9 Solid dispersions -- 1.9.1 Eutectic mixtures -- 1.9.2 Solid solutions -- 1.9.3 Eutectics and drug identification -- Summary -- References -- 2 Physicochemical properties of drugs in solution -- 2.1 Concentration units -- 2.1.1 Weight or volume concentration -- 2.1.2 Molarity and molality -- 2.1.3 Milliequivalents -- 2.1.4 Mole fraction -- 2.2 Thermodynamics: a brief introduction -- 2.2.1 Energy -- 2.2.2 Enthalpy -- 2.2.3 Entropy -- 2.2.4 Free energy -- 2.3 Activity and chemical potential -- 2.3.1 Activity and standard states -- 2.3.2 Activity of ionised drugs -- 2.3.3 Solvent activity -- Water activity and inhibition of bacterial growth -- Water activity and assessment of pharmaceutical products -- 2.3.4 Chemical potential -- Chemical potential of a component in solution -- 2.4 Osmotic properties of drug solutions -- 2.4.1 Osmotic pressure -- 2.4.2 Osmolality and osmolarity -- 2.4.3 Clinical relevance of osmotic effects -- Tonicity -- Volatile anaesthetics -- Rehydration solutions -- Oral rehydration therapy -- 2.4.4 Preparation of isotonic solutions -- 2.5 Ionisation of drugs in solution -- 2.5.1 Clinical relevance of drug ionisation -- 2.5.2 Dissociation of weakly acidic and basic drugs and their salts -- 2.5.3 The effect of pH on the ionisation of weakly acidic or basic drugs and their salts -- Weak acids -- Weak bases -- 2.5.4 Ionisation of amphoteric drugs -- Ordinary ampholytes. Zwitterionic ampholytes -- Large ΔpKa -- Small ΔpKa -- 2.5.5 Ionisation of polyprotic drugs -- 2.5.6 Microdissociation constants -- 2.5.7 pKa values of proteins -- 2.5.8 Calculation of the pH of drug solutions -- Weakly acidic drugs -- Weakly basic drugs -- Drug salts -- 2.5.9 Buffer solutions -- Buffer capacity -- Physiological regulation of acid-base balance -- Universal buffers -- 2.6 Diffusion of drugs in solution -- Summary -- References -- 3 Drug stability -- 3.1 The chemical decomposition of drugs -- 3.1.1 Hydrolysis -- Drugs susceptible to hydrolytic degradation -- Controlling drug hydrolysis in solution -- Optimisation of formulation -- Modification of chemical structure of drug -- 3.1.2 Oxidation4 -- Oxidation processes -- Drugs susceptible to oxidation -- Stabilisation against oxidation -- Antioxidants -- 3.1.3 Isomerisation -- 3.1.4 Photochemical decomposition10 -- Stabilisation against photochemical decomposition -- 3.1.5 Polymerisation -- 3.2 Kinetics of chemical decomposition in solution -- 3.2.1 Classifying reactions: the order of reaction -- 3.2.2 Zero-order reactions -- 3.2.3 First-order reactions -- 3.2.4 Second-order reactions -- 3.2.5 Third-order reactions -- 3.2.6 Determination of the order of reaction -- 3.2.7 Complex reactions -- Reversible reactions -- Parallel reactions -- Consecutive reactions -- 3.3 Solid-dosage forms: kinetics of chemical decomposition -- 3.3.1 Solids that decompose to give a solid and a gas -- 3.3.2 Solids that decompose to give a liquid and a gas -- 3.4 Factors influencing drug stability -- 3.4.1 Liquid-dosage forms -- pH -- Temperature -- Ionic strength -- Solvent effects -- Oxygen -- Light -- Surfactants -- 3.4.2 Semisolid-dosage forms -- 3.4.3 Solid-dosage forms -- Moisture -- Excipients -- Temperature -- Light and oxygen -- 3.5 Stability testing and prediction of shelf-life. 3.5.1 Effect of temperature on stability -- Suspensions -- Solid state -- 3.5.2 Other environmental factors affecting stability -- Light -- Oxygen -- Moisture content -- 3.5.3 Protocol for stability testing -- Drug substances -- Drug product -- Summary -- Some final points on the stability of drugs -- References -- 4 The solubility of drugs -- 4.1 Definitions -- 4.1.1 Expressions of solubility -- 4.2 Factors influencing solubility -- 4.2.1 Structural features and aqueous solubility -- Size and shape -- Melting point and boiling point -- Substituents -- Steroid solubility -- 4.2.2 Hydration and solvation -- Hydration of non-electrolytes -- Hydration of ionic species: water structure breakers and structure makers -- Hydration numbers -- Hydrophobic hydration -- The solubility of inorganic materials in water -- 4.2.3 The effect of simple additives on solubility -- Solubility products -- Common ion effect -- Salting in and salting out -- 4.2.4 The effect of pH on the solubility of ionisable drugs -- Acidic drugs -- Basic drugs -- Amphoteric drugs -- Rule of thumb -- 4.3 Measurement of solubility -- 4.4 The solubility parameter -- 4.4.1 Solubility parameters and biological processes -- 4.5 Solubility in mixed solvents: use of cosolvents -- Outline placeholder -- Room-temperature ionic liquids -- 4.6 Cyclodextrins as solubilising agents -- Outline placeholder -- Calixarenes -- 4.7 Solubility problems in formulation -- 4.7.1 Mixtures of acidic and basic compounds -- 4.7.2 Choice of drug salt to optimise solubility -- 4.7.3 Drug solubility and biological activity -- 4.8 Partitioning -- 4.8.1 The partition coefficient -- 4.8.2 Free energies of transfer -- 4.8.3 Octanol as a non-aqueous phase -- 4.9 Biological activity and partition coefficients: thermodynamic activity and Ferguson's principle -- 4.10 Using log P. 4.10.1 The relationship between lipophilicity and behaviour of tetracyclines -- 4.10.2 Sorption -- 4.10.3 A chromatographic model for the biophase -- 4.10.4 Calculating log& -- thinsp -- P from molecular structures -- 4.10.5 Drug distribution into human milk -- Summary -- References -- 5 Surfactants -- 5.1 Amphipathic compounds -- 5.2 Surface and interfacial properties of surfactants -- 5.2.1 Effects of amphiphiles on surface and interfacial tension -- 5.2.2 Change of surface tension with surfactant concentration: the critical micelle concentration -- 5.2.3 Gibbs adsorption equation -- Application of the Gibbs equation to surfactant solutions -- 5.2.4 The influence of the surfactant structure on surface activity -- 5.2.5 Surface activity of drugs -- 5.2.6 Insoluble monolayers -- Experimental study of insoluble films -- Monolayer states -- Solid or condensed monolayers -- Gaseous monolayers -- Expanded monolayers -- Factors influencing monolayer state -- Visualisation of monolayer structures -- Polymer monolayers -- Lung surfactant monolayers -- 5.2.7 Pharmaceutical applications of surface film studies -- Study of polymers used as packaging materials and film coatings -- Cell membrane models -- 5.2.8 Adsorption at the solid-liquid interface -- Adsorption isotherms -- Langmuir equation -- Freundlich equation -- Factors affecting adsorption -- Solubility of the adsorbate -- pH -- Nature of the adsorbent -- Temperature -- Some medical and pharmaceutical applications and consequences of adsorption -- Adsorption of poisons/toxins -- Taste masking -- Haemoperfusion -- Adsorption in drug formulation -- 5.3 Micellisation -- 5.3.1 Water structure and hydrophobic bonding -- 5.3.2 Theories of micelle formation -- 5.3.3 Micellar structure -- Critical packing parameter -- Ionic micelles -- Non-ionic micelles. 5.3.4 Factors affecting the critical micelle concentration and micellar size.
This established textbook covers every aspect of drug properties from the design of dosage forms to their delivery by all routes to sites of action in the body.
9780857112590
Pharmaceutical chemistry.
Electronic books.
RS403 -- .F567 2016eb
615.19
Physicochemical Principles of Pharmacy : In Manufacture, Formulation and Clinical Use. - 6th ed. - 1 online resource (665 pages)
Intro -- Contents -- Preface -- About the authors -- Introduction -- Physical chemistry and pharmacy -- The clinical relevance of physical pharmacy: clinical pharmaceutics -- Adjuvants or excipients -- Arrangement of the book -- Objectives -- 'Reading' structures and formulae -- Chemical structures -- Physical equations -- 1 Solids -- 1.1 Classification of solids -- 1.2 Crystalline solids: structure and properties -- 1.2.1 Crystal structure -- Miller indices -- 1.2.2 Crystal form -- Crystallisation and factors affecting crystal form2 -- Precipitation -- Habit modification -- 1.2.3 Polymorphism4 -- Pharmaceutical implications of polymorphism -- Transformations -- Analytical issues -- Consequences -- 1.2.4 Multicomponent crystals -- Crystal hydrates and solvates -- Pharmaceutical consequences of solvate formation -- Cocrystals -- 1.3 Amorphous solids -- 1.4 Dissolution of solid drugs -- 1.5 Biopharmaceutical importance of particle size -- 1.6 Wetting of powders -- 1.6.1 Contact angle and wettability of solid surfaces -- 1.6.2 Wettability of powders -- 1.7 Freeze drying -- 1.8 Solid-dosage forms: formulation and manufacture -- 1.8.1 Excipients -- Filler/diluent -- Disintegrants -- Binders -- Lubricants -- Glidants -- Flavouring agents and colourants -- 1.8.2 Powder flow -- 1.8.3 Particle size reduction -- 1.8.4 Powder mixing and demixing -- 1.8.5 Granulation -- Wet granulation -- Stage 1: Granule formation -- Extrusion/spheronisation techniques -- Bonding mechanisms in wet granulation -- Stage 2: Drying and milling -- Dry granulation -- Bonding mechanisms in dry granulation -- 1.8.6 Tablet manufacture -- Compression and compaction of powders -- The compression process -- Mechanisms of compression -- Tablet coating -- Film coating -- Film-coating formulations -- Solvent -- Polymer -- Plasticiser -- Colourant -- Surfactant -- Film-coating techniques. Drum or pan coating -- Fluidised-bed coating -- Dry coating -- Liquid-assisted coating -- Thermal adhesion -- Electrostatic coating -- 1.8.7 Capsule manufacture -- Chemical and physicochemical properties of gelatin -- Hard-capsule manufacture and filling -- Manufacture -- Filling of powder formulations -- Filling of pellets and tablets -- Filling of liquids and semisolids -- Soft gelatin (softgel) capsule manufacture and filling -- Manufacture and filling -- 1.9 Solid dispersions -- 1.9.1 Eutectic mixtures -- 1.9.2 Solid solutions -- 1.9.3 Eutectics and drug identification -- Summary -- References -- 2 Physicochemical properties of drugs in solution -- 2.1 Concentration units -- 2.1.1 Weight or volume concentration -- 2.1.2 Molarity and molality -- 2.1.3 Milliequivalents -- 2.1.4 Mole fraction -- 2.2 Thermodynamics: a brief introduction -- 2.2.1 Energy -- 2.2.2 Enthalpy -- 2.2.3 Entropy -- 2.2.4 Free energy -- 2.3 Activity and chemical potential -- 2.3.1 Activity and standard states -- 2.3.2 Activity of ionised drugs -- 2.3.3 Solvent activity -- Water activity and inhibition of bacterial growth -- Water activity and assessment of pharmaceutical products -- 2.3.4 Chemical potential -- Chemical potential of a component in solution -- 2.4 Osmotic properties of drug solutions -- 2.4.1 Osmotic pressure -- 2.4.2 Osmolality and osmolarity -- 2.4.3 Clinical relevance of osmotic effects -- Tonicity -- Volatile anaesthetics -- Rehydration solutions -- Oral rehydration therapy -- 2.4.4 Preparation of isotonic solutions -- 2.5 Ionisation of drugs in solution -- 2.5.1 Clinical relevance of drug ionisation -- 2.5.2 Dissociation of weakly acidic and basic drugs and their salts -- 2.5.3 The effect of pH on the ionisation of weakly acidic or basic drugs and their salts -- Weak acids -- Weak bases -- 2.5.4 Ionisation of amphoteric drugs -- Ordinary ampholytes. Zwitterionic ampholytes -- Large ΔpKa -- Small ΔpKa -- 2.5.5 Ionisation of polyprotic drugs -- 2.5.6 Microdissociation constants -- 2.5.7 pKa values of proteins -- 2.5.8 Calculation of the pH of drug solutions -- Weakly acidic drugs -- Weakly basic drugs -- Drug salts -- 2.5.9 Buffer solutions -- Buffer capacity -- Physiological regulation of acid-base balance -- Universal buffers -- 2.6 Diffusion of drugs in solution -- Summary -- References -- 3 Drug stability -- 3.1 The chemical decomposition of drugs -- 3.1.1 Hydrolysis -- Drugs susceptible to hydrolytic degradation -- Controlling drug hydrolysis in solution -- Optimisation of formulation -- Modification of chemical structure of drug -- 3.1.2 Oxidation4 -- Oxidation processes -- Drugs susceptible to oxidation -- Stabilisation against oxidation -- Antioxidants -- 3.1.3 Isomerisation -- 3.1.4 Photochemical decomposition10 -- Stabilisation against photochemical decomposition -- 3.1.5 Polymerisation -- 3.2 Kinetics of chemical decomposition in solution -- 3.2.1 Classifying reactions: the order of reaction -- 3.2.2 Zero-order reactions -- 3.2.3 First-order reactions -- 3.2.4 Second-order reactions -- 3.2.5 Third-order reactions -- 3.2.6 Determination of the order of reaction -- 3.2.7 Complex reactions -- Reversible reactions -- Parallel reactions -- Consecutive reactions -- 3.3 Solid-dosage forms: kinetics of chemical decomposition -- 3.3.1 Solids that decompose to give a solid and a gas -- 3.3.2 Solids that decompose to give a liquid and a gas -- 3.4 Factors influencing drug stability -- 3.4.1 Liquid-dosage forms -- pH -- Temperature -- Ionic strength -- Solvent effects -- Oxygen -- Light -- Surfactants -- 3.4.2 Semisolid-dosage forms -- 3.4.3 Solid-dosage forms -- Moisture -- Excipients -- Temperature -- Light and oxygen -- 3.5 Stability testing and prediction of shelf-life. 3.5.1 Effect of temperature on stability -- Suspensions -- Solid state -- 3.5.2 Other environmental factors affecting stability -- Light -- Oxygen -- Moisture content -- 3.5.3 Protocol for stability testing -- Drug substances -- Drug product -- Summary -- Some final points on the stability of drugs -- References -- 4 The solubility of drugs -- 4.1 Definitions -- 4.1.1 Expressions of solubility -- 4.2 Factors influencing solubility -- 4.2.1 Structural features and aqueous solubility -- Size and shape -- Melting point and boiling point -- Substituents -- Steroid solubility -- 4.2.2 Hydration and solvation -- Hydration of non-electrolytes -- Hydration of ionic species: water structure breakers and structure makers -- Hydration numbers -- Hydrophobic hydration -- The solubility of inorganic materials in water -- 4.2.3 The effect of simple additives on solubility -- Solubility products -- Common ion effect -- Salting in and salting out -- 4.2.4 The effect of pH on the solubility of ionisable drugs -- Acidic drugs -- Basic drugs -- Amphoteric drugs -- Rule of thumb -- 4.3 Measurement of solubility -- 4.4 The solubility parameter -- 4.4.1 Solubility parameters and biological processes -- 4.5 Solubility in mixed solvents: use of cosolvents -- Outline placeholder -- Room-temperature ionic liquids -- 4.6 Cyclodextrins as solubilising agents -- Outline placeholder -- Calixarenes -- 4.7 Solubility problems in formulation -- 4.7.1 Mixtures of acidic and basic compounds -- 4.7.2 Choice of drug salt to optimise solubility -- 4.7.3 Drug solubility and biological activity -- 4.8 Partitioning -- 4.8.1 The partition coefficient -- 4.8.2 Free energies of transfer -- 4.8.3 Octanol as a non-aqueous phase -- 4.9 Biological activity and partition coefficients: thermodynamic activity and Ferguson's principle -- 4.10 Using log P. 4.10.1 The relationship between lipophilicity and behaviour of tetracyclines -- 4.10.2 Sorption -- 4.10.3 A chromatographic model for the biophase -- 4.10.4 Calculating log& -- thinsp -- P from molecular structures -- 4.10.5 Drug distribution into human milk -- Summary -- References -- 5 Surfactants -- 5.1 Amphipathic compounds -- 5.2 Surface and interfacial properties of surfactants -- 5.2.1 Effects of amphiphiles on surface and interfacial tension -- 5.2.2 Change of surface tension with surfactant concentration: the critical micelle concentration -- 5.2.3 Gibbs adsorption equation -- Application of the Gibbs equation to surfactant solutions -- 5.2.4 The influence of the surfactant structure on surface activity -- 5.2.5 Surface activity of drugs -- 5.2.6 Insoluble monolayers -- Experimental study of insoluble films -- Monolayer states -- Solid or condensed monolayers -- Gaseous monolayers -- Expanded monolayers -- Factors influencing monolayer state -- Visualisation of monolayer structures -- Polymer monolayers -- Lung surfactant monolayers -- 5.2.7 Pharmaceutical applications of surface film studies -- Study of polymers used as packaging materials and film coatings -- Cell membrane models -- 5.2.8 Adsorption at the solid-liquid interface -- Adsorption isotherms -- Langmuir equation -- Freundlich equation -- Factors affecting adsorption -- Solubility of the adsorbate -- pH -- Nature of the adsorbent -- Temperature -- Some medical and pharmaceutical applications and consequences of adsorption -- Adsorption of poisons/toxins -- Taste masking -- Haemoperfusion -- Adsorption in drug formulation -- 5.3 Micellisation -- 5.3.1 Water structure and hydrophobic bonding -- 5.3.2 Theories of micelle formation -- 5.3.3 Micellar structure -- Critical packing parameter -- Ionic micelles -- Non-ionic micelles. 5.3.4 Factors affecting the critical micelle concentration and micellar size.
This established textbook covers every aspect of drug properties from the design of dosage forms to their delivery by all routes to sites of action in the body.
9780857112590
Pharmaceutical chemistry.
Electronic books.
RS403 -- .F567 2016eb
615.19