Discussing comprehensive range of topics, Advanced Pharmaceutics: Physicochemical Principles reviews all aspects of physical pharmacy. The book explains the basic, mechanistic, and quantitative interpretation skills needed to solve physical pharmacy related problems. The author supplies a strong fundamental background and extensively covers thermodynamics, ionic equilibria, solutions and distribution, surface chemistry and colloids, kinetics, diffusion, and polymer science. He outlines the latest research on diffusion through a membrane and the use of polymers in dosage forms.Packed with formulae and models, the book demonstrates the development of each and then describes the use of those models for a variety of formulation situations. The author's detailed explanation of the evolution of the formulae provides a clear understanding of when and how they are used. This bottom-up approach delineates the evolution of the formulae and gives a clear understanding of when and how they should be used. The book provides an in-depth review and analysis of dosage form design criteria that you can rapidly implement in your day-to-day work.
Author(s): Cherng-ju Kim
Edition: 1
Publisher: CRC Press
Year: 2004
Language: English
Pages: 498
Advanced Pharmaceutics: Physicochemical Principles......Page 2
Preface......Page 4
Author......Page 5
Contents......Page 6
1.1 IDEAL GASES......Page 12
Table of Contents......Page 0
1.2 REAL GASES......Page 15
1.3.1 T HE F IRST L AW OF T HERMODYNAMICS......Page 17
1.3.2 ENTHALPY (HEAT CONTENT) AND HEAT CAPACITY......Page 21
1.3.3 THERMOCHEMISTRY......Page 23
1.3.4 HEAT ENGINE AND THE CARNOT CYCLE......Page 27
1.3.5 THE SECOND LAW OF THERMODYNAMICS AND ENTROPY......Page 30
1.3.6 THE THIRD LAW OF THERMODYNAMICS......Page 33
1.4 FREE ENERGY......Page 34
1.4.1 FREE ENERGY FUNCTIONS......Page 35
1.4.2 FUNDAMENTAL EQUATIONS OF THERMODYNAMICS AND THEIR USES......Page 38
1.4.3 FREE ENERGY OF FORMATION AND STANDARD FREE ENERGY CHANGE......Page 41
1.4.4 FREE ENERGY AND CHEMICAL EQUILIBRIUM......Page 44
1.4.5 THE THERMODYNAMICS OF MIXING......Page 50
PROBLEMS......Page 53
2.1.1 P H OF THE S OLUTION OF A S TRONG A CID OR S TRONG B ASE......Page 56
2.1.2 T ITRATION C URVE OF A S TRONG B ASE WITH A S TRONG A CID......Page 57
2.2.1 P H OF THE S OLUTION OF A M ONOPROTIC W EAK A CID OR W EAK B ASE......Page 59
2.2.2 TITRATION CURVE OF A WEAK ACID WITH A STRONG BASE......Page 64
2.2.3 PH OF THE SOLUTION OF SALTS OF WEAK ACIDS OR WEAK BASES......Page 66
2.2.4 PH OF THE SOLUTION OF A MIXTURE OF CONJUGATE ACIDS AND BASES: HENDERSON–HASSELBALCH EQUATION......Page 69
2.2.5 BUFFER SOLUTIONS AND BUFFER CAPACITY......Page 76
2.2.6 EFFECT OF IONIC STRENGTH ON BUFFERS......Page 80
2.2.7 SOLUBILITY OF WEAK ELECTROLYTES AND AMPHOLYTES......Page 86
2.3.1 PH OF THE SOLUTION OF A DIPROTIC WEAK ACID, WEAK BASE, OR AMPHOLYTE......Page 90
2.3.2 PH OF THE SOLUTION OF A TRIPROTIC WEAK ACID, WEAK BASE, OR POLYPROTIC AMINO ACID......Page 97
2.3.3 TITRATION CURVES OF A POLYPROTIC WEAK ACID, WEAK BASE, OR POLYAMPHOLYTE......Page 110
2.3.4 BUFFER CAPACITY OF A BUFFER SOLUTION CONTAINING A POLYPROTIC WEAK ACID OR WEAK BASE AND ITS CONJUGATE BASE OR ACID......Page 113
2.4.1 SOLUBILITY PRODUCT CONSTANT AND SOLUBILITY OF SPARINGLY SOLUBLE SALTS......Page 115
2.4.2 SOLUBILITY OF SPARINGLY SOLUBLE SALTS OF WEAK ACIDS OR WEAK BASES......Page 116
2.4.3 EFFECT OF IONIC STRENGTH ON SOLUBILITY OF SPARINGLY SOLUBLE SALTS......Page 119
SUGGESTED READINGS......Page 121
PROBLEMS......Page 122
3.1.1 I DEAL S OLUTIONS......Page 124
3.1.2 N ONIDEAL S OLUTIONS AND THE S OLUBILITY P ARAMETER......Page 127
3.1.3 INTERMOLECULAR AND INTRAMOLECULAR INTERACTIONS BETWEEN MOLECULES......Page 133
3.1.4 PREDICTION OF SOLUBILITY......Page 139
3.1.5 SOLUBILIZATION OF WEAK ACIDS OR WEAK BASES IN COSOLVENT SYSTEMS......Page 143
3.1.6 DISSOLUTION KINETICS OF SOLIDS IN LIQUIDS Total Solubility (mM)......Page 146
3.2.1 RAOULT’S LAW......Page 150
3.2.2 TWO-COMPONENT LIQUID SYSTEMS......Page 152
3.2.3 THREE-COMPONENT LIQUID SYSTEMS......Page 155
3.3 SOLUTIONS OF GASES IN LIQUIDS (HENRY’S LAW)......Page 156
3.4.1 FREEZING POINT DEPRESSION AND BOILING POINT ELEVATION......Page 159
3.4.2 OSMOTIC PRESSURE......Page 163
3.4.3 VAPOR PRESSURE LOWERING......Page 165
3.4.4.1 Freezing Point Method......Page 166
3.4.4.2 NaCl Equivalent Method......Page 168
3.5.1 NONDISSOCIATED AND NONASSOCIATED SYSTEMS......Page 169
3.5.2 ASSOCIATION OF A SOLUTE IN ONE PHASE......Page 171
3.5.3 DISSOCIATION IN AQUEOUS PHASE AND ASSOCIATION IN OIL PHASE......Page 172
3.5.4 DISTRIBUTION AND SOLUBILIZATION OF WEAK ACIDS OR WEAK BASES IN MICELLES AND THE AQUEOUS PHASE......Page 177
3.5.5 DISTRIBUTION AND SOLUBILIZATION OF DRUG CHEMICALS BY INCLUSION COMPLEX FORMATION......Page 180
3.5.6 DISTRIBUTION OF DRUGS IN PROTEINS (PROTEIN BINDING)......Page 189
SUGGESTED READINGS......Page 199
PROBLEMS......Page 200
4.1.1 A DSORPTION P ROCESSES......Page 203
4.1.2.1 Langmuir Isotherm......Page 204
4.1.2.2 Freundlich Isotherm......Page 205
4.1.2.3 BET Isotherm......Page 208
4.1.2.4 Competitive Adsorption......Page 211
4.1.3.1 Nature of the Adsorbent......Page 215
4.1.3.3 pH......Page 216
4.2 LIQUID–LIQUID SYSTEMS (EMULSIONS)......Page 217
4.2.1 LIQUID–LIQUID INTERFACIAL TENSION......Page 218
4.2.2 ADSORPTION OF SURFACTANTS AT INTERFACES......Page 220
4.2.3.1 Surface-Active Materials......Page 224
4.2.3.3 Finely Divided Solids......Page 228
4.2.4 TYPE OF EMULSION AND HLB SYSTEM......Page 229
4.2.5 INSTABILITY OF EMULSIONS......Page 235
4.2.6 MICELLIZATION AND SOLUBILIZATION......Page 236
4.2.7 MICROEMULSIONS......Page 240
4.3.1 WETTING AND WETTING AGENTS......Page 241
4.3.1.1 Surfactants......Page 245
4.3.1.2 Hydrocolloids......Page 246
4.3.1.3 Solvents......Page 247
4.3.2.1 The Electrical Double Layer......Page 248
4.3.2.2 The Stabilization and Destabilization of Colloid Systems......Page 250
4.3.3 SEDIMENTATION OF DILUTE SUSPENSIONS......Page 256
4.3.4 PREVENTION OF CAKE FORMATION......Page 262
SUGGESTED READINGS......Page 264
PROBLEMS......Page 265
5.1.1 H YDROLYSIS......Page 266
5.1.3 PHOTOLYSIS......Page 268
5.2 SINGLE AND MULTIPLE REACTIONS, ELEMENTARY REACTIONS, MOLECULARITY, AND ORDER OF REACTIONS......Page 269
5.3.1 Z ERO -O RDER R EACTIONS......Page 271
5.3.2 F IRST -O RDER R EACTIONS......Page 272
5.3.3 APPARENT ZERO-ORDER REACTIONS......Page 274
5.3.4 SECOND-ORDER REACTIONS......Page 276
5.4.1 DIFFERENTIATION METHOD......Page 279
5.4.2 INTEGRATION METHOD......Page 281
5.5.1 AUTOCATALYTIC REACTIONS......Page 286
5.5.2 PARALLEL REACTIONS ln{[P][A]o/([A][P]o)}......Page 289
5.5.3 CONSECUTIVE REACTIONS......Page 291
5.6.1 REVERSIBLE FIRST-ORDER REACTIONS......Page 294
5.6.2 REVERSIBLE SECOND-ORDER REACTIONS......Page 297
5.7 REVERSIBLE AND SERIES REACTIONS (EIGENVALUE METHOD)......Page 299
5.8.1 DEFINITIONS AND PROPERTIES......Page 305
5.8.2 APPLICATIONS OF LAPLACE TRANSFORMS FOR DRUG DEGRADATION AND BIOTRANSFORMATION......Page 306
5.9.1 ENZYME--SUBSTRATE REACTIONS WITHOUT INHIBITION......Page 311
5.9.2 ENZYME--SUBSTRATE REACTION WITH INHIBITION......Page 315
5.10.1 ACID--BASE CATALYZED HYDROLYSIS OF NEUTRAL CHEMICALS......Page 320
5.10.2 ACID–BASE CATALYZED HYDROLYSIS OF POLYPROTIC WEAK ACIDS AND WEAK BASES......Page 323
5.11 OXIDATION (FREE RADICAL REACTION)......Page 331
5.12 DEGRADATION KINETICS IN INCLUSION COMPLEXES, MICELLES, AND LIPOSOMES......Page 334
5.13 TEMPERATURE EFFECTS ON THE REACTION RATE CONSTANTS......Page 338
SUGGESTED READINGS......Page 344
PROBLEMS......Page 345
6.1.1 T RANSPORT P ROCESSES......Page 349
6.1.2 D IFFUSION C OEFFICIENTS......Page 354
6.2.1 UNSTEADY-STATE DIFFUSION THROUGH A MEMBRANE......Page 359
6.2.2.1 Constant Activity Reservoir Systems......Page 364
6.2.2.2 Nonconstant Activity Reservoir Systems......Page 365
6.2.3 MULTI-LAYER MEMBRANE DEVICES......Page 368
6.3.1 DISSOLVED DRUG IN POLYMERIC DRUG CARRIERS......Page 370
6.3.2 DISPERSED DRUG IN POLYMERIC DRUG CARRIERS......Page 375
6.4 DIFFUSION IN A MEMBRANE–MATRIX SYSTEM......Page 382
6.5 DIFFUSION DURING THE SWELLING OF A MATRIX......Page 385
6.6.1 HOMOGENEOUS EROSION/DEGRADATION......Page 390
6.6.2 HETEROGENEOUS EROSION/DEGRADATION......Page 393
6.7 DIFFUSION IN A MATRIX SWELLING/EROSION......Page 396
6.8 DIFFUSION WITH CHEMICAL REACTION IN A MEMBRANE......Page 400
6.9 SURFACE AREA AND CONCENTRATION GRADIENT SYSTEMS......Page 404
6.10 OSMOTICALLY CONTROLLED SYSTEMS......Page 408
PROBLEMS......Page 415
7.1 CLASSIFICATION OF POLYMERS......Page 417
7.2 MOLECULAR WEIGHT AND MOLECULAR WEIGHT DISTRIBUTION OF POLYMERS......Page 422
7.3.1 V ISCOSITY M ETHOD......Page 424
7.3.2 OSMOMETRY......Page 428
7.3.3 LIGHT SCATTERING......Page 430
7.3.4 SIZE EXCLUSION CHROMATOGRAPHY (SEC)......Page 433
7.3.4.1 Effective Linear Calibration Method without Peak Broadening Correction......Page 437
7.3.4.2 Effective Linear Calibration Method with Peak Broadening Correction......Page 439
7.3.4.3 Universal Calibration Method......Page 440
7.3.4.4 Multiple Detector System (e.g., Concentration and Light-Scattering Detectors)......Page 442
7.4.1 ADDITION HOMO-POLYMERIZATION (FREE-RADICAL HOMO-POLYMERIZATION)......Page 443
7.4.1.1 Polyvinylpyrrolidone (PVP) and Its Copolymers......Page 451
7.4.1.2 Polyvinylacetate and Its Derivatives......Page 452
7.4.1.4 Polyisobutylene (PIB)......Page 453
7.4.2 FREE-RADICAL COPOLYMERIZATION......Page 454
7.4.2.1 Eudragit® and Kollicoat® series:......Page 461
7.4.2.2 Ion Exchange Resins:......Page 463
7.4.2.3 Carbopol® or Carbomer®......Page 464
7.4.2.4 Poly(ethylene-co-vinyl acetate) (PEVAc)......Page 465
7.4.3 STEP POLYMERIZATION (CONDENSATION POLYMERIZATION)......Page 466
7.4.3.1 Acid-Catalyzed Esterification Polymerization of A--A and B--B......Page 467
7.4.3.2 Self-Catalyzed Condensation Polymerization......Page 468
7.4.3.3 Molecular Weight Control......Page 470
7.4.3.4 Polyanhydrides......Page 472
7.4.3.5 Poly(orthoesters)......Page 475
7.4.3.6 Poly(amino acids)......Page 477
7.4.3.7 Silicone polymers......Page 478
7.4.4.1 Polylactic Acid, Polyglycolic Acid, and Polycaprolactone......Page 481
7.4.4.2 Polyethylene Glycol (PEG), Polyethylene Oxide (PEO), and Block Copolymers of Ethylene Oxide and Propylene Oxide (PEOPO)......Page 483
7.4.4.3 Polyphosphazene (PPP)......Page 487
7.5.1 CELLULOSE......Page 488
7.5.2 CELLULOSE DERIVATIVES......Page 489
7.5.3 CHITOSAN......Page 492
7.5.4 POLYSACCHARIDES......Page 494
7.5.5 GELATIN......Page 497
SUGGESTED READINGS......Page 498
