《Polymers for Pharmaceutical Application:藥用高分子材料(中文導讀版)》是編者總結近十年的教學經(jīng)驗,從大量英文原版文獻和書籍中選取適合教學大綱要求的內(nèi)容編寫而成,并對關鍵知識點配以中文導讀,便于學生閱讀和理解。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,許多高校開展了采用漢語和英語的雙語教學實踐,這對辦學國際化和國際化辦學很重要,也是培養(yǎng)具有國際競爭力的高素質(zhì)人才的需要。
隨著藥用新材料的發(fā)展對藥物輸送系統(tǒng)和技術的不斷促進,國際上對藥用高分子材料的研究也越來越受到人們的關注。系統(tǒng)學習了解藥用高分子材料相關知識,是現(xiàn)代藥學科技工作者、尤其是藥劑學專業(yè)學生的迫切需要。但目前,還沒有一本適合藥用高分子材料課程的雙語教材。國際上,這一領域符合教學要求的英文原版書籍也很匱乏,國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。若在教學中直接采用英文原版教材,價格不菲,學生對于大量專業(yè)名詞術語的理解也有困難。本教材《P0lyrners fol Phai了nacelnical AppliCation——藥用高分子材料(中文導讀版)》就是為了適應雙語教學的新形勢和課程要求而編寫的。希望本書的出版可以填補藥用高分子材料雙語教學教材的空白,有助于雙語教學過程的規(guī)范。學生閱讀英文版內(nèi)容并對照關鍵知識點的中文導讀,可以接觸和掌握大量專業(yè)詞匯,對藥學專業(yè)本科生的專業(yè)英文水平提高一定有所裨益。
編者先后在復旦大學和上海交通大學藥學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經(jīng)驗為基礎,參考大量英文原版文獻和書籍,根據(jù)我國教學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,包括它們的結構、性質(zhì)及其在藥劑學中的應用;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用進展的幾個熱點方向,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)的重點內(nèi)容均有中文導讀,便于學生閱讀和理解。
在本書編寫過程中,上海交通大學藥學院藥物控釋技術與醫(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外國語學院劉興華老師的幫助和潤色。在此一并表示衷心感謝。
本書可作為藥學專業(yè)本科生教材和藥劑學專業(yè)研究生參考教材,也可供藥學、醫(yī)學和高分子材料學等方面的科技工作者參考。
由于藥用高分子材料是一個涉及化學、材料、生物、藥學和醫(yī)學的交叉領域,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指正。
編者
2014年6月
郭圣榮,上海交通大學藥學院,教授,浙江大學高分子化學與物理專業(yè)博士,曾赴美國佐治亞理工大學從事博士后研究。現(xiàn)任上海交通大學藥學院藥物控制釋放技術與醫(yī)用高分子課題組負責人,博士生導師。兼職上海市醫(yī)藥衛(wèi)生青年聯(lián)合會委員,世界中醫(yī)藥學會聯(lián)合會第一屆中藥新型給藥系統(tǒng)專業(yè)委員會常務理事。研究方向為:1.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計、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)療器械與藥劑結合,如載藥消化道支架等。近5年來已完成和正在承擔的國家和省市級研究項目20項,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。申請中國發(fā)明專利18項,授權8項。先后獲明治乳業(yè)生命科學最高獎(杰出獎)、國家科技進步二等獎、上海市自然科學三等獎和中國藥學會科技三等獎。
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
本章中文導讀
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
本章中文導讀
References
Chapter 3. Natural Polymers as Pharmaceutical Excipients
天然來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
本節(jié)中文導讀
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
本節(jié)中文導讀
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
本節(jié)中文導讀
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
本節(jié)中文導讀
4.2 Polymers based on polyether
4.2.1 Polyethylene glycol
4.2.2 Poloxamer
4.2.3 Polysorbates
本節(jié)中文導讀
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
本章中文導讀
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用進展
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
本節(jié)中文導讀
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
本節(jié)中文導讀
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
本節(jié)中文導讀
6.4 Polymers for gene delivery
6.4.1 Introduction to gene delivery
6.4.2 Polymeric vectors
本節(jié)中文導讀
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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