Pharmaceutical Dosage Form and Technology(药物剂型与工艺)

Chapter 1 Introduction 1
1.1 Drugs and diseases 1
1.1.1 Treatment of diseases 1
1.1.2 Drug substances and medicines 1
1.1.3 The history of drugs 2
1.1.4 The drug-target interaction 3
1.2 About pharmacy 5
1.2.1 Pharmaceutical sciences 5
1.2.2 Pharmaceutics 5
1.2.3 Dosage forms and drug delivery systems 6
1.2.4 Categories of DDS 9
1.3 The standardization of medicine 11
1.3.1 Why medicine needs standard 11
1.3.2 Pharmacopeia 12
1.4 Clinical using medicine 12
1.4.1 Brand medicine and generic medicine 12
1.4.2 Prescription medicine and over-the-counter medicine 13
1.4.3 Prescription 13
1.4.4 Drug-drug interaction 14
1.4.5 Drug-food interaction 14
References 16

Chapter 2 Solid dosage forms I 17
2.1 Introduction 17
2.2 Powder 18
2.3 Granules 20
2.3.1 Preparation of granules 22
2.3.2 Granulation methods and equipments 22
2.3.3 Quality control of granules 31
References 33

Chapter 3 Solid dosage forms II 34
3.1 Capsules 34
3.1.1 Hard gelatin capsules 34
3.1.2 Soft capsules 36
3.2 Tablets 37
3.2.1 Excipients of tablets 39
3.2.2　Manufacture of tablets 40
3.2.3 Film coating 42
3.2.4 Quality control of tablets 53
3.2.5 Packaging and storing of tablets 58
References 59

Chapter 4 Pulmonary drug delivery system 60
4.1 Introduction 60
4.1.1 Anatomy of lungs 60
4.1.2 Advantages of pulmonary drug delivery 61
4.1.3 Mechanisms of particle deposition in the lung 62
4.2 Pulmonary drug delivery devices 62
4.2.1 Nebulizers 63
4.2.2 pMDIs 64
4.2.3 DPIs 64
4.2.4 Soft mist inhaler 65
4.3 Factors governing aerosol deposition and targeting in the lung 66
4.3.1 Aerodynamic diameter and size distribution 66
4.3.2 Airflow rate 66
4.3.3 Particle shape 67
4.3.4 Particle density 67
4.3.5 Surface roughness 67
4.4 Clinical application of pulmonary drug delivery systems 68
4.5 Perspectives of pulmonary drug delivery 69
References 70

Chapter 5 Transdermal drug delivery system 73
5.1 Introduction 73
5.2 Skin structure and the major obstacles of transdermal permeation 74
5.3 Major transdermal routes 75
5.3.1 Appendageal routes 75
5.3.2 Transcellular routes 75
5.3.3 Intercellular routes 75
5.4 Chemical penetration enhancers 76
5.4.1 Natural chemical penetration enhancers 76
5.4.2 Synthetic chemical penetration enhancers 77
5.4.3 Combination of penetration enhancers 82
5.5 Physical techniques to improve transdermal delivery 83
5.5.1 Microneedle 83
5.5.2 Laser 84
5.5.3 Iontophoresis 86
5.5.4 Sonophoresis 87
5.5.5 Electroporation 89
5.5.6 Magnetophoresis 90
5.5.7 Microwave 90
5.6 Transdermal formulations 91
5.6.1 Liposome 91
5.6.2 Cubic phase 91
5.6.3 Microemulsion 91
5.6.4 Hydrogel 91
5.6.5 Transfersome 92
5.7 Device-assisted or wearable transdermal delivery systems 92
5.7.1 Development stages 92
5.7.2 Device 93
5.7.3 Application 94
5.7.4 Prospect 94
References 94

Chapter 6 Liquid dosage forms 101
6.1　Introductions 101
6.1.1　Solubilities 101
6.1.2　Solvents 102
6.1.3　Enhancements 103
6.2　Syrups 103
6.3　Elixirs 104
6.4　Suspensions 105
6.4.1　Sedimentation of particles in suspension 105
6.4.2　Preparation of suspensions 107
6.4.3　Colloidal dispersions 108
6.5　Emulsions 109
6.5.1　Pharmaceutical emulsions 110
6.5.2　Emulsion formation theory 111
6.5.3　Emulsion identification 112
6.5.4　Emulsion preparation 112
6.5.5　The HLB system 116
6.5.6　Emulsion stability 117
6.5.7　Nanoemulsions 120
6.6　Creams 121
6.7 Gels and magmas 122
References 123

Chapter 7 Sterilized preparations 124
7.1 Principles of sterilization 124
7.1.1 Introduction 124
7.1.2　Sterilization parameters 124
7.1.3　Principles of sterilization processes 125
7.1.4　Gaseous sterilization 127
7.1.5　Radiation sterilization 128
7.1.6　Filtration sterilization 129
7.1.7 High-level disinfection 129
7.2　Parenteral 130
7.2.1　Introduction 130
7.2.2　Injections 130
7.2.3　Large-volume parenterals 131
7.3　Biologics 131
7.3.1　Introduction 131
7.3.2　Types of immunity 132
7.3.3　Production of biologics 132
7.4　Ophthalmic solution and suspensions 133
7.4.1　Introduction 133
7.4.2　Pharmaceutical requirements 134
References 136

Chapter 8 Modified-release oral drug delivery 138
8.1 Introduction of modified-release oral drug delivery 138
8.1.1　Sustained-release preparation 138
8.1.2　Controlled-release preparation 138
8.1.3　Delayed-release preparation 138
8.2　Theories of extended-release oral drug delivery 139
8.2.1　Theory of dissolution-controlled 139
8.2.2　Theory of diffusion-controlled 140
8.2.3　Combination of erosion and diffusion theory 141
8.2.4 Osmotic pressure theory 142
8.2.5　Ion exchange theory 143
8.3　Design of extended-release oral drug delivery systems 144
8.3.1　Properties of drugs 144
8.3.2　Design requirements 147
8.4　Quality assessment 149
8.4.1　In vitro assessment 149
8.4.2　In vivo assessment 150
8.4.3　In vitro correlation 150
8.5 Application of extended-release oral drug delivery systems 154
8.6　Oral chronopharmacologic and oral site-specific drug delivery system 160
8.6.1　Overview 160
8.6.2　Theories 161
8.6.3　Brief introductions 163
8.6.4 Applications 166
References 171

Chapter 9 Suppositories 173
9.1　Introduction 173
9.2 Suppository bases 174
9.2.1　Fatty or oleaginous bases 174
9.2.2　Water-soluble or water-miscible bases 174
9.3 Preparation of suppositories 175
9.3.1 Manufacturing procedure 175
9.3.2　Displacement value 176
9.3.3 Quality control 177
9.3.4　Examples 177
9.4　Packing and storage 178
9.5　Special types of suppositories 178
References 179

Chapter 10 Paediatric and geriatric drug developent 180
10.1 Introduction 180
10.2　Physiological changes 180
10.3　Excipient safety 181
10.4　Taste 183
10.5　Formulation choices 184
10.5.1　Tablets 184
10.5.2　Liquids 185
10.5.3　Multiparticulates 186
10.5.4　Dispersible and orally dispersible formulations 186
10.5.5　Chewable tablets 187
References 188

Indexes 190