Pharmaceutical emulsions and suspensions

Contents......Page 13
Preface......Page 11
Contributors......Page 17
1. Main Surfactants Used in the Pharmaceutical Field......Page 20
I. Introduction......Page 21
II. Anionic Surfactants......Page 22
III. Cationic Surfactants......Page 25
IV. Nonionic Surfactants......Page 26
V. Additional Surfactants......Page 30
VI. Conclusion......Page 32
References......Page 35
2. Formulation Concepts for the Emulsion Maker......Page 38
I. Introduction and Definitions......Page 39
II. Emulsion Making: Importance of Formulation......Page 42
III. Formulation Influence on Phase Behavior......Page 46
IV. Empirical Approach to Formulation Quantification......Page 59
V. Experimental Methods Applied to Real Cases......Page 76
References......Page 87
3. Emulsion Properties and Related Know-How to Attain Them......Page 92
I. Emulsion Characteristics and Properties......Page 93
II. Influence of Formulation on Emulsion Properties......Page 117
III. Formulation/Composition Map......Page 123
IV. Dynamic Phenomena in Emulsion Modification......Page 134
References......Page 141
4. Suspension Formulation......Page 146
I. Introduction......Page 147
II. Thermodynamic Description of an Interface......Page 149
III. Wetting Phenomena: Hydrophobicity and Hydrophilicity of a Dispersed Solid......Page 152
IV. Surface Free Energy of Solids: Measurement and Applications......Page 155
V. Electrical Properties: The ζ Potential......Page 168
VI. Experimental Determination of ζ Potential: Some Examples of  Pharmaceutical Interest......Page 175
VII. Adsorption of Surfactants and Polymers......Page 182
VIII. Stability of Suspensions......Page 194
IX. Summary......Page 204
References......Page 205
5. Emulsions as Drug Delivery Systems......Page 210
 I. Introduction......Page 211
II. Biodistribution of Drug Carriers......Page 213
Ill. Influence of Particle Size and Particle Dose......Page 214
IV. Surface Characteristics......Page 216
V. Effect of Surface Charge......Page 219
VI. Stability Concerns......Page 222
VII. Structure of Emulsion Carriers......Page 223
VIII. In Vivo Behavior of Emulsion Systems......Page 226
IX. Clinical Applications of Emulsion Systems......Page 227
X. Cancer Chemotherapy......Page 232
XI. Antimicrobial Therapy......Page 235
XII. Immunological Adjuvant......Page 236
XIII. Diagnostic Imaging......Page 237
XIV. Perfluorochemical Emulsions......Page 239
XV. Emulsions for Ocular Delivery of Drugs......Page 240
XVI. Multiple Emulsions......Page 241
XVII. Conclusions......Page 242
References......Page 243
6. Parenteral Fat Emulsions: Structure, Stability, and Applications......Page 248
II. Definitions......Page 249
III. Physical Structure of Parenteral Fat Emulsions......Page 250
IV. Physical Stability......Page 251
V. Parenteral Fat Emulsions......Page 254
VII. Total Parenteral Nutrition......Page 257
VIII. Drug Carrier Systems......Page 259
X. In Vivo Behavior of Intravenous Fat Emulsions......Page 262
References......Page 264
7. Use of Emulsions as Topical Drug Delivery Systems......Page 278
I. Introduction......Page 279
III. Absorption Through the Skin......Page 280
IV. Use of Emulsion Formulations in Dermatology......Page 282
V. Drug Diffusion Across the Stratum Corneum......Page 283
VI. Effect of the Emulsion on Transdermal Delivery......Page 287
References......Page 288
I. Introduction......Page 290
II. Lipid Organization in Stratum Corneum......Page 292
III. Liposomes Affect Drug Transport Through the Skin......Page 295
IV. Conclusions......Page 315
References......Page 316
I. Introduction......Page 322
II. Emulsion Systems for Ophthalmic Use......Page 324
III. Ophthalmic Suspensions......Page 330
References......Page 337
10. Administration of Emulsions to the Gastrointestinal Tract......Page 342
I. Introduction......Page 343
II. Self-Emulsifying Drug-Delivery Systems......Page 344
Ill. The Fate of Emulsions in the Gastrointestinal Tract......Page 353
IV. Bioavailability of Drugs from Oily Delivery Systems......Page 359
V. Factors Influencing Drug Uptake from Oils......Page 362
VI. Drug Absorption from Emulsions and SEDDS......Page 367
VII. Conclusions......Page 371
References......Page 373
11. Dry Adsorbed Emulsions......Page 380
I. Preparation of a Dry Adsorbed Emulsion......Page 381
II. Physicochemical Structure of the Form......Page 384
III. Drug Release......Page 385
IV. Particle Size Effect......Page 389
V. Oil Phase Effect......Page 390
VI. Role of Hydrophilic Silica......Page 391
VII. Preparation Aging......Page 393
VIII. Pharmaceutical Applications......Page 394
IX. Conclusions and Future Outlook......Page 398
References......Page 400
12. Nanosuspensions for the Formulation of Poorly Soluble Drugs......Page 402
I. Introduction......Page 403
III. Production of Nanosuspensions (DissoCubes®) by High-Pressure Homogenization......Page 405
IV. Size Distributions of Nanosuspensions......Page 408
V. Sterilization of Nanosuspensions......Page 414
VI. Physical Long-Term Stability of Aqueous Nanosuspensions......Page 416
VII. Electron Microscopic Characterization of Nanosuspensions......Page 417
VIII. Physicochemical Properties of Nanosuspensions......Page 418
IX. Dosage Forms Based on Nanosuspensions......Page 420
XI. Large-Scale Production of Nanosuspensions......Page 422
XII. Nanosuspensions (DissoCubes) vs. NanoCrystals......Page 424
References......Page 425
13. Pharmaceutical Suspensions and Their Applications......Page 428
I. Introduction......Page 429
II. Special Features of Pharmaceutical Suspensions......Page 433
III. Typical Constituents of Pharmaceutical Suspensions......Page 437
IV. Applications of Pharmaceutical Suspensions......Page 457
V. Suspensions as Drug Delivery Systems......Page 465
References......Page 476
14. Experimental Design in Emulsion and Suspension Formulations: Theoretical Aspects......Page 484
I. Experimental Methodological Approach......Page 485
II. Study of the Effects of the Factors......Page 502
III. Response Surface Methodology......Page 518
IV. Mixtures......Page 540
References......Page 551
I. Introduction......Page 554
II. Screening Approach and Factor Study......Page 555
III. Optimization......Page 562
IV. Conclusion......Page 571
References......Page 572
I. Introduction......Page 576
II. Basic Concepts......Page 578
III. Rheology of Suspensions and Emulsions......Page 599
IV. Application of Rheology to Product Formulation......Page 615
References......Page 623
17. Determination of Size Distributions of Submicrometer Particle Dispersions by Photon Correlation Spectroscopy......Page 628
I. Introduction......Page 629
II. Basic Physics......Page 630
III. Experimental Methods......Page 632
IV. Mean Particle Diameter and Polydispersity......Page 635
V. Higher Order Moments......Page 637
VI. Polydispersity Analysis......Page 638
VII. lnteracting Particles......Page 640
VIII. Turbid \'\'White\'\' Media: Multiple Scattering......Page 641
X. Applications......Page 642
References......Page 647
C......Page 650
D......Page 652
E......Page 653
F......Page 655
H......Page 656
I......Page 657
M......Page 658
O......Page 659
P......Page 660
R......Page 662
S......Page 664
T......Page 667
W......Page 668
Z......Page 669