Chapter 1 Fundamentals of Pharmaceutical Polymer Chemistry 1
1.1 The Concept of a Polymer 1
1.2 Addition Polymerization 4
1.3 Chain Branching; Graft and Block Copolymers 15
1.4 Polymer Structure and Properties 18
1.5 Technology of Polymerization 24
1.6 The Principal Monomers and Their Polymers 27
1.7 Physical Properties of Monomers 37
References 41
Chapter 2 Pharmaceutical Polymers： Principles and Structures 42
2.1 Introduction 42
2.2 Intra and Inter Polymer Molecular Interactions 45
2.3 Molecular Mass： Polydispersivity and Effects on Polymer Viscosity 47
2.4 Thermal Properties： Effect of Crystalline and Amorphous Phases 51
2.5 Mechanical Properties of Polymers 54
2.6 Pharmaceutical Polymers： Principles, Structures, and Applications of Pharmaceutical Delivery Systems 61
References 80
Chapter 3 Polymers as Drugs 81
3.1 Introduction 81
3.2 Polymers for Molecular Sequestration 83
3.3 Polyvalent Interactions and Anti-Infective Polymeric Drugs 95
3.4 Polymeric Drugs for the Treatment of Autoimmune Diseases 105
3.5 Polymeric Anti-Obesity Drugs 107
3.6 Polymer Therapy for Sickle Cell Disease 111
3.7 Conclusions and Outlook on Polymers as Drugs 112
References 113
Chapter 4 Pharmaceutical Applications of Natural Polymers 114
4.1 Introduction 114
4.2 Portals of Drug Administration in the Human Body 116
4.3 Transdermal Drug Delivery Devices 117
4.4 Topical Drug Delivery 124
4.5 Oral Drug Delivery System 131
4.6 Parenteral Drug Delivery Systems 132
4.7 Nasal Drug Delivery Systems 134
4.8 Hydrogel-Based Drug Delivery Systems 136
References 147
Chapter 5 Hydrophobic Polymers of Pharmaceutical Significance 149
5.1 Introduction 149
5.2 Examples of Hydrophobic Polymers and Their Drug Delivery Applications 150
5.3 Conclusions 167
References 168
Chapter 6 Polymers in Drug Delivery 169
6.1 Evolution of Drug Dosage Forms 169
6.2 Polymer Excipients 172
6.3 Polymers as Manufacture Aids and Sustained Release 174
References 200
Chapter 7 Pharmaceutical Nanotechnology： Overcoming Drug Delivery Challenges in Contemporary Medicine 202
7.1 Challenges in Delivery of Contemporary Therapeutics 202
7.2 Nanotechnology Solutions 207
7.3 Illustrative Examples of Nanotechnology Products 211
7.4 Multifunctional Nanotechnology 218
7.5 Regulatory Issues in Nano-pharmaceuticals 225
7.6 Conclusions and Future Outlook 235
References 235
Chapter 8 Thermal Analysis of Pharmaceutical Polymers 237
8.1 Introduction 237
8.2 Theoretical Background of Thermal Analysis 238
8.3 Physical and Chemical Phenomena Commonly Investigated Using Thermal Approaches 244
8.4 Applications of Thermal Analysis for the Characterisation of Pharmaceutical Raw Materials 248
8.5 Applications of Thermal Analysis for the Characterisation of Pharmaceutical Dosage Forms 250
8.6 Conclusion 255
References 255
Chapter 9 Applications of AFM in Pharmaceutical Polymers 256
9.1 Introduction 256
9.2 Use of AFM in Pharmaceutical Sciences 263
9.3 AFM Combined With Optical or Spectroscopic Techniques 271
9.4 Summary 271
References 273
Chapter 10 Rheology in Pharmaceutically Used Polymers 274
10.1 Introduction 274
10.2 Theoretical Background and Fundamental Concepts 275
10.3 Practical Issues of Rheological Measurements 289
10.4 Application of the Technique 292
10.5 Summary 297
References 297
內容試閱：
前言药用高分子（Pharmaceutical polymers）是具有生物相容性、经过安全评价且应用于药物制剂的一类高分子量药用辅料。药用高分子作为药物缓释载体，包覆在药物表面保护小分子药物使其在短时间内不会被生命体吸收，同时随血液流动到特定区域，在特定区域药物表面的高分子材料溶解到血液中，释放出药物，而本身最终随体液排出。药用高分子的主要应用有：①载体，用以控制药物缓慢释放，一般由有机硅橡胶、聚甲基丙烯酸酯类等制成封闭细管、微囊或薄膜。②主药，有长效的特点，其结构有三类：（a）在高分子侧基上连接小分子药物，这类结构最受重视，即高分子亲和药物，在高分子侧链上除含有药物结构外，在较远端侧链上还含有亲水结构、配基或酶，以提高药用高分子在体内分布的专一性；（b）在高分子主链中含小分子药物；（c）高分子中不含小分子药物，其本身可作为药物或功能试剂。本书结合现代药剂学的发展以及作者多年来的教学科研实践，根据国内外最新资料，简述了有关高分子化学和物理的基本内容，概述了与药剂学相关的高分子材料基本知识，重点介绍国际上经法定程序验证及实际生产中已被采用的药用高分子材料的原理和应用，充实了国外近年来备受瞩目的给药系统用天然来源药用高分子及可生物降解的合成药用高分子和复合物的有关内容，此外，还对热分析、原子力显微镜和流变学在药用高分子领域中的应用进行了阐述。本书可供普通高等医药院校药学、药物制剂、制药工程、高分子材料与工程等相关专业学生及从事药物制剂生产、研究的人员参考使用。全书共分为十章，参与本书编写的人员及具体编写分工如下：第一章由孙红、王者辉编写；第二章由张宏志、孙立平编写；第三章由巩学勇、刘凤霞编写；第四章由李庆杰、常海涛编写；第五章由郑超、张倩编写；第六章由刘光耀、江栋编写；第七章由卫振华、刘爱军编写；第八章由王者辉、李宝庆编写；第九章由杜江山、刘振亮编写；第十章由姜洪丽、孟宪锋编写；全书由王者辉统一整理并任主编。由于水平所限，书中不足之处在所难免，诚恳希望广大读者加以批评指正。编者2018年5月PrefacePharmaceutical polymers both synthetic and natural-based polymers have found their way into the pharmaceutical industries and their applications are growing at a fast pace. The desirable polymer properties in pharmaceutical applications are film forming coating, thickening rheological modifier, gelling controlled release, adhesion binding, pH-dependent solubility controlled release, solubility in organic solvents taste masking, and barrier properties protection and packaging. Major applications of polymers in current pharmaceutical field are for controlled drug release. From the solubility point of view, pharmaceutical polymers can be classified as water-soluble and water-insoluble oil soluble or organic soluble. Many water-soluble pharmaceutical polymers including polyethylene glycol, polyvinyl alcohol, polyethylene oxide, polyvinyl pyrrolidone, polyacrylate or polymethacrylate esters, cellulose based polymers, hydrocolloids, and many plastics and rubbers will be tabulated and their anionic and cationic functionalities are summarized and discussed. PEGylation is defined as the covalent attachment of poly ethylene glycol PEG chains to bioactive substances. Pharmaceutical polymer, a kind of macromolecular compound with bioco- mpatibility, safety evaluation, is used as a kind of high molecular mass pharma- ceutical excipients for drug preparation. As a sustained release drug carrier, the pharmaceutical polymer is coated on the surface of the drug to protect small molecular weight drugs not to be absorbed by the living body in a short time. At the same time, with the flow of blood in a specific area, the polymer materials on the specific area of the drug dissolve into the blood and release the drug, and the drug itself is eventually discharged with the body fluid. The main applications of pharmaceutical polymers include： 1 the carrier, which is used to control the slow release of drugs, usually made of organosilicon rubber, polymethacrylate and others in the form of closed tubes, microcapsules or films. 2 the main drug with characteristic long time efficacy has three kinds of structures： i polymeric affinity drug, with the hydrophilic groups, the ligands or enzymes on the far end of the chain, have small molecular drugs connecting on the side of the polymer chains, which is the most important structure with pharmaceutical polymer uniform distribution inside the body; ii polymeric drug contains small molecule drugs in the main chain; iii polymers do not contain small molecular drugs, it act as medicine or functional reagent. This book, combined with the development of modern pharmaceutics and many years practice of teaching and scientific research, briefly describes the founda- mentals of polymer chemistry and physics, and summarizes the basic knowledge of polymers related to pharmaceutics. According to the latest information at home and abroad, this book mainly introduces the principles and applications of pharma- ceutical polymers that have been used in international legal procedure verification and actual production, and enriches the related contents of natural sources of pharmaceutical polymers and biodegradable synthetic pharmaceutical polymers and complexes in recent years. The applications of thermal analysis, atomic force microscopy and rheology in the field of pharmaceutical polymers are included. This book can be used as a reference for readers of pharmaceutical engineering, polymer materials and engineering and related majors and people engaged in the production and research of pharmaceutical preparations.The personnel involved in this book include： the first chapter by Hong Sun and Zhehui Wang; the second chapter by Hongzhi Zhang and Liping Sun; the third chapter by Xueyong Gong and Fengxia Liu; the fourth chapter by Qingjie Li and Haitao Chang; the fifth chapter by Chao Zheng and Qian Zhang; the sixth chapter by Guangyao Liu and Dong Jiang; the seventh chapter by Zhenhua Wei and Aijun Liu; the eighth chapter by Zhehui Wang and Baoqing Li; the ninth chapter by Jiangshan Du and Zhenliang Liu; the tenth chapter by Hongli Jiang and Xianfeng Meng; this whole book is edited by Zhehui Wang. As to the limitation of the authors level, all kinds of criticisms are welcome for various mistakes in the book, and we sincerely hope that readers will be able to inform us for correction.Zhehui Wang2018.5
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