《Polymers for Pharmaceutical Application:药用高分子材料(中文导读版)》是编者总结近十年的教学经验,从大量英文原版文献和书籍中选取适合教学大纲要求的内容编写而成,并对关键知识点配以中文导读,便于学生阅读和理解。全书共分6章,主要内容如下:第一章为药用辅料概述;第二章为高分子材料简介;第三章、第四章分别介绍选材于《Handbook of Pharmaceutical Excipients》(Fourth Edition,edited by Raymond C Rowe,Paul J Sheskey and Paul J Weller)中的天然高分子辅料和合成高分子辅料;第五章介绍现代药物输送系统研发中涉及的生物可降解高分子材料;第六章介绍几类新型的高分子药物输送体系,包括:自组装高分子和纳米制剂、药用水凝胶、高分子-药物轭合物、高分子基因载体。
近年来,许多高校开展了采用汉语和英语的双语教学实践,这对办学国际化和国际化办学很重要,也是培养具有国际竞争力的高素质人才的需要。
随着药用新材料的发展对药物输送系统和技术的不断促进,国际上对药用高分子材料的研究也越来越受到人们的关注。系统学习了解药用高分子材料相关知识,是现代药学科技工作者、尤其是药剂学专业学生的迫切需要。但目前,还没有一本适合药用高分子材料课程的双语教材。国际上,这一领域符合教学要求的英文原版书籍也很匮乏,国外第一本作为教材使用的《P。lymers in Drug]Deliveiy》于2006年才由CRC出版社出版。若在教学中直接采用英文原版教材,价格不菲,学生对于大量专业名词术语的理解也有困难。本教材《P0lyrners fol Phai了nacelnical AppliCation——药用高分子材料(中文导读版)》就是为了适应双语教学的新形势和课程要求而编写的。希望本书的出版可以填补药用高分子材料双语教学教材的空白,有助于双语教学过程的规范。学生阅读英文版内容并对照关键知识点的中文导读,可以接触和掌握大量专业词汇,对药学专业本科生的专业英文水平提高一定有所裨益。
编者先后在复旦大学和上海交通大学药学院讲授药用高分子材料课程1。余年。本教材以编者多年的教学经验为基础,参考大量英文原版文献和书籍,根据我国教学大纲的要求编写而成。全书共分6章,王要内容如下:第1章为药用辅料概述;第2章为高分子材料概述;第3章、第4章分别介绍选材于《Handbook of Phalmaceu ticalExcipientS》(6th Edltion, edited by Raymond C Rowe,Paul J Sheskey andPaul Weller)中的天然高分子辅料和合成高分子辅料,包括它们的结构、性质及其在药剂学中的应用;第5章介绍现代药物输送系统研发中涉及的合成类生物可降解高分子材料;第6章介绍功能高分子材料在新型药物输送体系中应用进展的几个热点方向,包括:药用水凝胶材料、纳米制剂与自组装高分子、高分子一药物轭合物、高分子基因载体。每章/节的重点内容均有中文导读,便于学生阅读和理解。
在本书编写过程中,上海交通大学药学院药物控释技术与医药用高分子课题组的沈园园老师,研究生蒋金均、吴可沁、李敏、汪芸,参与了资料收集和整理等工作。英文部分内容得到了上海交通大学外国语学院刘兴华老师的帮助和润色。在此一并表示衷心感谢。
本书可作为药学专业本科生教材和药剂学专业研究生参考教材,也可供药学、医学和高分子材料学等方面的科技工作者参考。
由于药用高分子材料是一个涉及化学、材料、生物、药学和医学的交叉领域,资料的收集整理未必全面,若有疏漏和不完善之处,衷心希望广大读者批评指正。
编者
2014年6月
郭圣荣,上海交通大学药学院,教授,浙江大学高分子化学与物理专业博士,曾赴美国佐治亚理工大学从事博士后研究。现任上海交通大学药学院药物控制释放技术与医用高分子课题组负责人,博士生导师。兼职上海市医药卫生青年联合会委员,世界中医药学会联合会第一届中药新型给药系统专业委员会常务理事。研究方向为:1.新型药物输送系统制备和体内外表征,如微、纳米尺度药剂,原位凝胶剂,植入剂等;2.新型药用高分子材料的设计、制备、性状和自组装行为,如生物降解性、两亲性、离子性高分子材料;3. 医疗器械与药剂结合,如载药消化道支架等。近5年来已完成和正在承担的国家和省市级研究项目20项,发表研究性论文100余篇,其中SCIE收录论文60多篇。主编专著二本,主译专著一本,参加编写和编译专著多本。申请中国发明专利18项,授权8项。先后获明治乳业生命科学最高奖(杰出奖)、国家科技进步二等奖、上海市自然科学三等奖和中国药学会科技三等奖。
Chapter 1. Introduction to Pharmaceutical Excipients
药用辅料概述
1.1 Definition of pharmaceutical excipients
1.2 What are excipients doing in medicines?
1.3 Quality and safty of excipients
1.4 Relationship between polymers and pharmaceutical excipients
1.5 Specific notes for polymers used in drug delivery system
本章中文导读
References
Chapter 2. Introduction to Polymers
高分子材料概述
2.1 What are polymers?
2.2 Polymer structure and morphology
2.2.1 Molecular weight
2.2.2 Configuration and conformation
2.2.3 Chain structure
2.2.4 Crystalline
2.3 Synthesis
2.3.1 Addition polymerization
2.3.2 Condensation polymerization
2.3.3 Cross-linking reaction
2.4 Characteristic properties of polymers
2.4.1 Thermal properties
2.4.2 Mechanical properties
2.4.3 Viscoelastic properties
2.5 Characterization techniques
2.5.1 Determination of molecular weight
2.5.2 Determination of structure
2.5.3 Differential scanning calorimetry
2.6 Fabrication and processing
2.6.1 Injection molding
2.6.2 Extrusion
2.6.3 Spinning
本章中文导读
References
Chapter 3. Natural Polymers as Pharmaceutical Excipients
天然来源的药用高分子辅料
3.1 Starch and its derivates
3.1.1 Starch
3.1.2 Pregelatinized starch
3.1.3 Dextrin
3.1.4 Cyclodextrin
3.1.5 Sodium carboxymethyl starch
本节中文导读
3.2 Cellulose and its derivates
3.2.1 Microcrystalline cellulose
3.2.2 Powdered cellulose
3.2.3 Methylcellulose
3.2.4 Ethylcellulose
3.2.5 Hydroxyethyl cellulose
3.2.6 Hydroxypropyl cellulose
3.2.7 Hydroxypropyl methylcellulose
3.2.8 Carboxymethylcellulose sodium
3.2.9 Carboxymethylcellulose calcium
3.2.10 Cellulose acetate phthalate
本节中文导读
3.3 Other natural polymers in pharmaceutics
3.3.1 Chitin/chitosan
3.3.2 Alginate and sodium/calcium alginate
3.3.3 Acacia
3.3.4 Xanthan gum
3.3.5 Gelatin
3.3.6 Albumin
本节中文导读
References
Chapter 4. Synthetic Polymers as Pharmaceutical Excipients
合成的药用高分子敷料
4.1 Polymers based on polyvinyl
4.1.1 Polyvinyl alcohol
4.1.2 Polymethacrylates
4.1.3 Polyvinylpyrrolidone (Povidone)
4.1.4 Crospovidone
4.1.5 Carbomer
本节中文导读
4.2 Polymers based on polyether
4.2.1 Polyethylene glycol
4.2.2 Poloxamer
4.2.3 Polysorbates
本节中文导读
References
Chapter 5. Novel Synthetic Biodegradable Polymers as Drug
Delivery Carrier
新型可生物降解的合成药用高分子材料
5.1 Introduction
5.2 Polymers based on polyester
5.2.1 Poly(lactic acid) and poly(lactic-co-glycolic acid) copolymers
5.2.2 Polycaprolactone
5.2.3 Poly(β-hydroxybutyrate)
5.3 Other biodegradable polymers
5.3.1 Poly(orthoesters)
5.3.2 Poly(phosphate esters)
5.3.3 Polyanhydrides
5.3.4 Poly(amino acids)
5.3.5 Polyphosphazenes
本章中文导读
References
Chapter 6. Advanced Applications of Functional Polymer in Drug Delivery
功能高分子材料在药物输送中的应用进展
6.1 Hydrogels for pharmaceutical application
6.1.1 Introduction
6.1.2 Preparation of hydrogels
6.1.3 Properties of hydrogels
6.1.4 Pharmaceutical applications of hydrogels
本节中文导读
6.2 Polymer-based nanomedicine and self-assemblying polymers
6.2.1 Introduction to nanomedicine
6.2.2 Micellation of self-assemblying polymers
6.2.3 Biological significance of polymeric micelles
6.2.4 Drug release from polymeric micelles
6.2.5 Examples of polymeric micelles for drug delivery
本节中文导读
6.3 Polymer-drug conjugates
6.3.1 Introduction
6.3.2 Design and development of polymer-drug conjugates
6.3.3 Examples for polymer-drug conjugates
本节中文导读
6.4 Polymers for gene delivery
6.4.1 Introduction to gene delivery
6.4.2 Polymeric vectors
本节中文导读
References
2.3 Synthesis
Polymer synthesis is a complex procedure and carl take place in a variety of ways.Usually,methods of polymer synthesis fall into two categories:addition polymerization(chain reaction)and condensation polymerization(stepwise growth).Ring opening isanother type of polymerization and will be discussed in more detail in the section ondegradable polymers.
2.3.1 Addition polymerization
Addition polymerization describes the method where unsaturated monomers areadded one by one to an active site on the growing chain.There are three sigui~antreactions that take place in addition polymerization:in~iation(birth),propagation(igrowth),and termination(death).The initiators can be free radicals,cations,anions,orstereospecific catalysts.The initiator opens the double bond of the monomer,presenting another‘.'initiation'’’site on the opposite side of the monomer bond forcontinuing growth.During the propagation step,rapid chain growth ensues until thereaction is terminated by reaction with another radical,a solvent molecule,anotherpolymer molecule,an initiator,or an added chain transfer agent。
The most common type of addition polymerization is free radical polymerization.As shown in Figure 2.8.free radicals are often created by the division of a molecule(known as an initiator)into two fragments along a single bond.In this case,benzoylperoxide acts as initiator to produce a radical.The radical attacks one monomer,andthe electron migrates to another part of the molecule.Then in the propagation stage,this newly formed radical attacks another monomer and the process is repeated.Thusthe active center moves down the chain as the polymerization occurs.Here,in freeradical polymerization,the entire propagation reaction usually takes place within afraction of a second.Thousands of monomers are added to the chain within thds time.The entire process stops when the termination reaction OCCurS.
In theory,the propagation reaction could continue until the supply of monomers isexhausted..However,most often the growth of a polymer chain is halted by thetermination reaction.Termination typically occurs in two ways:combination anddisproportionation,as jllu,,strated in Figure 2—8.Combination OCCurS when thepolymer’S growth is stopped by free electrons from two growing chains that join andform a single chain.Disproportionation halts the propagation reaction when a freeradical strips a hvdrogen atom from an active chain.A carbon.
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