《Polymers for Pharmaceutical Application：藥用高分子材料（中文導(dǎo)讀版）》是編者總結(jié)近十年的教學(xué)經(jīng)驗(yàn)，從大量英文原版文獻(xiàn)和書籍中選取適合教學(xué)大綱要求的內(nèi)容編寫而成，并對(duì)關(guān)鍵知識(shí)點(diǎn)配以中文導(dǎo)讀，便于學(xué)生閱讀和理解。全書共分6章，主要內(nèi)容如下：第一章為藥用輔料概述；第二章為高分子材料簡(jiǎn)介；第三章、第四章分別介紹選材于《Handbook of Pharmaceutical Excipients》（Fourth Edition，edited by Raymond C Rowe，Paul J Sheskey and Paul J Weller）中的天然高分子輔料和合成高分子輔料；第五章介紹現(xiàn)代藥物輸送系統(tǒng)研發(fā)中涉及的生物可降解高分子材料；第六章介紹幾類新型的高分子藥物輸送體系，包括：自組裝高分子和納米制劑、藥用水凝膠、高分子-藥物軛合物、高分子基因載體。
近年來(lái)，許多高校開展了采用漢語(yǔ)和英語(yǔ)的雙語(yǔ)教學(xué)實(shí)踐，這對(duì)辦學(xué)國(guó)際化和國(guó)際化辦學(xué)很重要，也是培養(yǎng)具有國(guó)際競(jìng)爭(zhēng)力的高素質(zhì)人才的需要。
隨著藥用新材料的發(fā)展對(duì)藥物輸送系統(tǒng)和技術(shù)的不斷促進(jìn)，國(guó)際上對(duì)藥用高分子材料的研究也越來(lái)越受到人們的關(guān)注。系統(tǒng)學(xué)習(xí)了解藥用高分子材料相關(guān)知識(shí)，是現(xiàn)代藥學(xué)科技工作者、尤其是藥劑學(xué)專業(yè)學(xué)生的迫切需要。但目前，還沒(méi)有一本適合藥用高分子材料課程的雙語(yǔ)教材。國(guó)際上，這一領(lǐng)域符合教學(xué)要求的英文原版書籍也很匱乏，國(guó)外第一本作為教材使用的《P。lymers in Drug]Deliveiy》于2006年才由CRC出版社出版。若在教學(xué)中直接采用英文原版教材，價(jià)格不菲，學(xué)生對(duì)于大量專業(yè)名詞術(shù)語(yǔ)的理解也有困難。本教材《P0lyrners fol Phai了nacelnical AppliCation——藥用高分子材料（中文導(dǎo)讀版）》就是為了適應(yīng)雙語(yǔ)教學(xué)的新形勢(shì)和課程要求而編寫的。希望本書的出版可以填補(bǔ)藥用高分子材料雙語(yǔ)教學(xué)教材的空白，有助于雙語(yǔ)教學(xué)過(guò)程的規(guī)范。學(xué)生閱讀英文版內(nèi)容并對(duì)照關(guān)鍵知識(shí)點(diǎn)的中文導(dǎo)讀，可以接觸和掌握大量專業(yè)詞匯，對(duì)藥學(xué)專業(yè)本科生的專業(yè)英文水平提高一定有所裨益。
編者先后在復(fù)旦大學(xué)和上海交通大學(xué)藥學(xué)院講授藥用高分子材料課程1。余年。本教材以編者多年的教學(xué)經(jīng)驗(yàn)為基礎(chǔ)，參考大量英文原版文獻(xiàn)和書籍，根據(jù)我國(guó)教學(xué)大綱的要求編寫而成。全書共分6章，王要內(nèi)容如下：第1章為藥用輔料概述；第2章為高分子材料概述；第3章、第4章分別介紹選材于《Handbook of Phalmaceu ticalExcipientS》（6th Edltion， edited by Raymond C Rowe，Paul J Sheskey andPaul Weller）中的天然高分子輔料和合成高分子輔料，包括它們的結(jié)構(gòu)、性質(zhì)及其在藥劑學(xué)中的應(yīng)用；第5章介紹現(xiàn)代藥物輸送系統(tǒng)研發(fā)中涉及的合成類生物可降解高分子材料；第6章介紹功能高分子材料在新型藥物輸送體系中應(yīng)用進(jìn)展的幾個(gè)熱點(diǎn)方向，包括：藥用水凝膠材料、納米制劑與自組裝高分子、高分子一藥物軛合物、高分子基因載體。每章／節(jié)的重點(diǎn)內(nèi)容均有中文導(dǎo)讀，便于學(xué)生閱讀和理解。
在本書編寫過(guò)程中，上海交通大學(xué)藥學(xué)院藥物控釋技術(shù)與醫(yī)藥用高分子課題組的沈園園老師，研究生蔣金均、吳可沁、李敏、汪蕓，參與了資料收集和整理等工作。英文部分內(nèi)容得到了上海交通大學(xué)外國(guó)語(yǔ)學(xué)院劉興華老師的幫助和潤(rùn)色。在此一并表示衷心感謝。
本書可作為藥學(xué)專業(yè)本科生教材和藥劑學(xué)專業(yè)研究生參考教材，也可供藥學(xué)、醫(yī)學(xué)和高分子材料學(xué)等方面的科技工作者參考。
由于藥用高分子材料是一個(gè)涉及化學(xué)、材料、生物、藥學(xué)和醫(yī)學(xué)的交叉領(lǐng)域，資料的收集整理未必全面，若有疏漏和不完善之處，衷心希望廣大讀者批評(píng)指正。
編者
2014年6月
郭圣榮，上海交通大學(xué)藥學(xué)院，教授，浙江大學(xué)高分子化學(xué)與物理專業(yè)博士，曾赴美國(guó)佐治亞理工大學(xué)從事博士后研究。現(xiàn)任上海交通大學(xué)藥學(xué)院藥物控制釋放技術(shù)與醫(yī)用高分子課題組負(fù)責(zé)人，博士生導(dǎo)師。兼職上海市醫(yī)藥衛(wèi)生青年聯(lián)合會(huì)委員，世界中醫(yī)藥學(xué)會(huì)聯(lián)合會(huì)第一屆中藥新型給藥系統(tǒng)專業(yè)委員會(huì)常務(wù)理事。研究方向?yàn)椋?.新型藥物輸送系統(tǒng)制備和體內(nèi)外表征，如微、納米尺度藥劑，原位凝膠劑，植入劑等；2.新型藥用高分子材料的設(shè)計(jì)、制備、性狀和自組裝行為，如生物降解性、兩親性、離子性高分子材料；3. 醫(yī)療器械與藥劑結(jié)合，如載藥消化道支架等。近5年來(lái)已完成和正在承擔(dān)的國(guó)家和省市級(jí)研究項(xiàng)目20項(xiàng)，發(fā)表研究性論文100余篇，其中SCIE收錄論文60多篇。主編專著二本，主譯專著一本，參加編寫和編譯專著多本。申請(qǐng)中國(guó)發(fā)明專利18項(xiàng)，授權(quán)8項(xiàng)。先后獲明治乳業(yè)生命科學(xué)最高獎(jiǎng)（杰出獎(jiǎng)）、國(guó)家科技進(jìn)步二等獎(jiǎng)、上海市自然科學(xué)三等獎(jiǎng)和中國(guó)藥學(xué)會(huì)科技三等獎(jiǎng)。
Chapter 1. Introduction to Pharmaceutical Excipients
藥用輔料概述
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
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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
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References
Chapter 3. Natural Polymers as Pharmaceutical Excipients
天然來(lái)源的藥用高分子輔料
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
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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
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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
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References
Chapter 4. Synthetic Polymers as Pharmaceutical Excipients
合成的藥用高分子敷料
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
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4.2 Polymers based on polyether
4.2.1 Polyethylene glycol
4.2.2 Poloxamer
4.2.3 Polysorbates
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References
Chapter 5. Novel Synthetic Biodegradable Polymers as Drug
Delivery Carrier
新型可生物降解的合成藥用高分子材料
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
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References
Chapter 6. Advanced Applications of Functional Polymer in Drug Delivery
功能高分子材料在藥物輸送中的應(yīng)用進(jìn)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
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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
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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
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6.4 Polymers for gene delivery
6.4.1 Introduction to gene delivery
6.4.2 Polymeric vectors
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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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