1、b-吡啶 yriie 巴比妥酸:barbitucacid 比电导conductance不规则得:iegular 崩解剂disnteranc-萃取 tracti 成团:agglomeration 测量仪easurement肠液:intinal ludd胆固醇olesero 对映体:nantiomer 电极elerd 代谢:mtlif-反相渗透rverse osmois分布:isiing-构象:nomation 固化:sliize-甲苯toue 静脉注:intravenou inetin 挤压:press 聚集:ageae 胶囊cpull粒子:arcl 立体选择性:sterseltivt 利用率:
2、availabili m灭菌产品sterilproducts n-粘合剂adsivep偏振光:polarizd ligh 片剂tabe 配剂lixir 排泄:excreti-起始原料sarti mterals(raw aterals) q醛 aldeye 溶解度:olubilit 乳剂emulio 润滑剂lubricas释放:releas 渗液soltion 生物膜:bilogi mem 生物碱akao, t-糖浆syrup 甜味剂weteerw-丸剂pll 微生物irooganis 胃液:gastrcflui 稳定态:teady-stat x旋光异构现象:tical omerism悬浮液su
3、spnson 香味剂fvor 稀释剂dluet 形状:shape 吸收:absion 消除:limitn y-胰岛素 nsuln 压片:tbletpression z中间体itermediate 重结晶 talliztion 左旋:levorotation 蒸馏distlltin 组织tissua-symetic can不对称碳 bsrptn吸收 cion动作 dsiv粘合剂cominatin污染 chiraly:手性 es压缩 poit合成得 pesiblity:可压缩性 paco:压紧 contamaon pecializ特殊污染 nductivity电导率 control:控制 clin
4、cl:临床得d- desin:设计 dry:干燥 deliery:传送e-extend:延长 epoxide:环氧化物 fomuio:制剂 flidt:流动性 functin:功能g-gemet imersm:几何异构h-horme激素 hydolyss diatereiser:水解非对映异构体heterogeneocatalst多相催化剂, iriatng冲洗 m- metbolite代谢物 edcatio药物治疗 medici内服药 mll:研磨measr尺寸 ix:混合 mcroganiss微生物 o- ohthalm眼药p osccaide多糖 eptid肽plsma血浆penicil
5、lin青霉素, recursor:前体 prtitio coficient:狭义分配系数 pharmacutical制药得 pentra注射药物 pycg热源 prcedure:程序 q- qualt性质 quantity数量 s- strd甾类 tericffect:空间效应 sereoelectivity:立体选择性screnin:过筛 ssin :维持t- ea治疗 therapy:治疗u-fomit目标 v-vaccine疫苗Unit 1、 Answ thfolloin uestons:(1) How many roups n paceutica agns be st nto deen
6、din n their produion ogin?otllystheic materias(syheics)natur prododcts fomparti syntess(seisynthetic oduct)(2)Can yo illutte a sigiiant exals of parmeutical agens btand y otal sythss? Lamne,chlraphomical,caffne,Dopamie,Epiephrin,eda,epie,ormes、Prstglaning,PPuricollmne,incamine,(3)Wh is he diferec bt
7、wee th sythet drgs an traitionl Chinese hbl meicine? ynteticdugs incluehe most important of synthetics nd semi-sytheti pods, we, tral prducts re freqntlnede as starinteria orntrmediates r mportant yntetc rodut、 2、生物碱、Introucton of Nuclic cidicaid are plyaionic mlecules o igh olecur eight、 Thes olyme
8、re sd fasequeof sbunit or nuclotides s thatthe woleisusually trmedapouetide、e nuclic acids are of tw a varitie, iboucc (RA) ddeoxibonucleic (DNA)、 DNAs fou primaily n thechrotthe ce nucles, wheras 9 f RNA i preseted n te cll coplasm nd 10inth uclols、 Th to lsses of nucleicaids ae ditigsheprmary on a
9、ss of e fivecarbo atmsugar o enterent、 To gena knds of besarfundn all nucleicacids、 Onetpeis a ervtiv ofparnt poudpine、 Pinciple emple are uninendadeine、 e secon cas of asesnd all cei cd is ivefrom e rn pon pyrimidin、 介绍核酸核酸就是超高分子量聚阴离子分子。这些聚合物组成,亚基或核苷酸,使整个通常称为多核苷酸序列。核酸有两种,主要品种核糖核酸(RNA)与脱氧核糖核酸(NA)得。D
10、A就是主要存在于细胞核内得染色质,而9得RNA在细胞质现在与%得核仁。核酸类得两个主要得区别在于对目前得五个戊糖碳原子得糖基础.一般两个种基地发现,在所有核酸。一类就是母体化合物嘌呤得衍生物.原理就是鸟嘌呤与腺嘌呤得例子.在所有发现核酸碱基第二类就是来自母体化合物嘧啶。Unt2 31、Anser e folloing question:(1) Wha is quantatve structurctivity retinship (QA) of harmcoloi gnts?untttv sripions f phsical rpertis o und and thespose of te bi
11、logial sysem undecoserain、(2) w man er factr ifluence on he phaacoloc actiity?Thre ajor hadings、(1)Opticaland eomti sorim Pharmacologi Ativty、()Cnfrontaionl IsomerismndPrmali ctiity、()Isomersm and Pamacologic Atty、(3) ho eaniohi pair(optca isomers) exhibt differe biological actiiies?diffencin bioogi
12、c ctiiy may be uet diferencein tedistribution of he ers ortoa fference t proertesofthe dug-reptr binatoof less them he optml nmeof bidin groups is sitably ocatedfobinding、2、静脉注射4、hefini f a novldu lecles aln, epese, and tuus pcess witno guaraneefsces、 lealy, out o e lmoti fnie numberof posie pus,nly
13、 fiite(few, small) nmber can eer eelece fo ttin ihin gn time a hekil of mdcial chist is indeciing wichof tos pouds to mae fist、 f core, here i thnthe jopobem f howt sythesizethem! In orde tomakthat dcisin, the mas of bioloicaldta produced or pounsalrtdnees tob aalyed inh awy tht eatures hichr imrtan
14、t for hologicaatviy/actvitis a b idntiiedand ef tue molecue、 he goalof quanitative structreactvity retionh (QSA)is o find predicativfct bwen qunitative descrptionphysicalrotiesof ounds ath rspone of th biolgcl sstem under cosidatio、 Hopefult reultin SARwil lad toan deiniin of t moleclar erspropertie
15、s mst imotant n dertrmg activity, adgui h rseahof iologial activit ti thpou ee、发现了新得药物分子就是一个长期得,昂贵得,曲折得过程没有成功得保证。显然,出了几乎无限多得可能,只有有限得(很少,小)数量能被选定为测试在给定得时间与技能得药用化学家在决定哪些就是这些化合物使第一。当然,有那么主要问题就是如何合成!为了使这一决定,大规模得生物数据产生得化合物已经测试需要分析得方式,特点,就是重要得生物活性/活动可确定,然后为未来得分子.目得定量构效关系(构效关系)就是找到预测作用之间得定量描述化合物得物理性质与反应得生物
16、系统得思考。希望由此产生得构效关系将导致一个定义得分子功能性能最重要得ertmig活动,并指导研究生物活性得化合物系列。Unit1 120、ner theollowig quetions: (1)Hma kinds of th rotof ru dministationar hre?aloutepateral routopical rout()anou esent these sual osaefor s te drug tht a adminitered oally?talecpsulslqui oral(3)Hw i an eaain of a tabets properie made?T
17、heacul phsicl design, mfacrng pracss, and plete heical makeup of th ablet cn hea profunffectothe eficacy ofh drug ben amered2、Solid oraldos formae deliverysyems rsented a soliddosunits readly dminiteed b mou、The group inldes aet,css,pills,an turuna(spotry), swe as bulk rnitdos poder an gaules、 hgrop
18、 costtue themot plar form of eentaion, and aletsa capsulesaccn f th gretest numbr of preparatin nths category、 e i reasons or hispopuarity nludes: easyo acurat (t vesate) sumet, goodpysica adcemic stbiy, ptitv unit producto cos, anda elgnt dtinciv appeaan resulti ina hghveof patet accptbilty、 o thep
19、otntil disadvantgesae iriantefectson the gastrointetinal moa by om soi and the posiilit o biavaabiliy problems casedy hefacthat bt ectivy(n most cause)ad stability mtak pace beore te drugisa availble orabsrption、固体口服剂型得运载系统作为固体剂量单位容易管理得嘴。该集团包括片剂,胶囊,丸,与栓剂(栓),以及体积或单位剂量得粉末与颗粒。该组得最流行得形式,介绍,与片剂与胶囊占最大数量得筹
20、备工作在这个类别.主要原因包括:容易普及准确(但多才多艺)测量,物理与化学稳定性好,具有竞争力得单位生产成本,与优雅得独特得外观,导致高水平得病人接受。其中潜在得缺点就是刺激性影响胃肠粘膜得某些固体与可能得生物利用度得问题造成得事实,既有效性(在大多数得原因)与稳定之前必须发生得药物就是一种可吸收。4、片剂Un12 P1271、An te following qustons: (1)Hveyou evr knothe enrl ethods d prcesses oft manufatu oftablt?Yes(2)What is te imortaeofmanufacture ganulat
21、in which tblearemade fom?Such as tness, psical stailing, r pruton, apublt cemica saty andefia,are in ge disttd pririlby heqalities of heamationfr hh t s md(3)What ponent ae inued ingeera eciins in a tlet fml?Al norug ponents(4) Hayo unrstood herinciple ofabe pressin operatin?、e the monly sedsag form
22、 ora i ablet,he poens in tblets formultonicludegneral duent, binder, disintegrat,lubrcant, an mkng the anulaion i imprtantprocesof tablet anuftue,the haaeistcs fatblt pend ascaly on thequaliies ofhe graulatin, whic mst posse tohaaerisi: fluid tyandprsib lty、The wetg ranlaton i amly sed ethod of gran
23、tion, wicilves we msing of th powers, et szn or millng andrying、 heids hysicafomoftabet mateia sphre 、unfrtuatel, mo mtrils do notal rm shere, whch mut be rcese by granulaton or formig phee like oreguarly shape ag regate、一个常用得剂型口服片剂,片剂得配方成分包括稀释剂,粘合剂,崩解剂,润滑剂,与造粒得过程就是一个重要得片得制作,特色得一片基本上取决于质量得造粒,其必须具备得特
24、征:流动性与可压缩性.湿造粒方法常用得就是肉芽组织,其中包括湿集结得权力,或研磨与干燥得湿上浆。理想得物理形式得片材料领域。不幸得就是,大多数材料不容易形成领域,必须处理得肉芽组织形成球形或定期形成聚集体.4 粒子、There a reessenialmthods of the manfacure o grnulatio fr tablet presion,ha are they?Unit1 P135(1)Ca ou diferenein qyonrobeten theoraltalet aserile rouctjed?Thy ae iected thoug h sin or mucous
25、membanes ito trnal o pamen (2)o s te ualit of serle puts asred in-proess?assurein process :No extempornu angsre permited tbe maei thee proce, n hangemust gothrougth am approval steps s he original written sop、 urther, xensive recods st bekpt t gie assanc at the en of the ductioprocess that lseps hae
26、 been prefomas psried, n spect emhasized in the FDAs ood Manufarin Patice(3)at is h tanr operatn procedure(OPs)?o enhance the ssurance ouccessfu manufatuing operatn,l process steps must b creflly recdtowrting fteingshon t fctiv(4)w i te atr fornjecton usuly prepre?Pducing highuritywate isillationan
27、vers osmosi, canbeped to reoe unissociatd ubstacs along wththose tha aredisscaedubstnces suh yognus, heve, oldbe presentin e bsenof ions ad ot b diclosby the st2、leethe ssagbelo:Strie prouctare dage fomso theraeuti aen thtare free fiable mioognisms, tes ilu arenteral,ohtalmi and rrgatin prparions,be
28、cas the a injctethrough he skin ormucuus mebanesinto iterna o,parerl producsms be ree fo mirobil contamaion nd fromtoxi ponnts 、 teil pducts re motrquntl soions r sspesion,h mst feqetlyempdhicle for serile produc iswer the qualit f war for inection(WFI) is requiredby araopeia,whi issurior qality req
29、rd,t natual watercontin generallyissiated and udistdorganic and inrganic subsane whchtheymst b essntaly removedand set apmitd limit,ontamint ae products of mataols of mirorganims,the emoval of proens s vimortan forter fr njecion、Wtefor ijecto is prpae by stllation or rere mosis、无菌产品剂型得治疗剂,就是免费得,可行得微
30、生物,其中包括肠外,眼科与灌溉得筹备工作,因为她们就是通过皮肤或粘膜进入人体内部,肠外产品必须免受微生物污染与有毒成分。无菌产品就是最常见得溶液或悬浮液,最经常使用得车辆为无菌产品水水质注射(注射用水)所需得药典,就是上乘得质量要求,自然含水量一般分离与udsscated有机与无机物质,它们必须就是基本上消除,设置一个允许得限度,污染物产品代谢得微生物,去除热原就是非常重要得注射用水.注射用水得制备蒸馏水或反渗透.、灭菌产品、Wh emoal ofpcoens is very mportntf WFI?Usually by a era eh, n conti thaths dissol som
31、etnt in the water、 herere, the solids conent il e greer ha forthenonsterllzdproct、Unit14 P12、(1)What is t ustaiedelease cnct?Sustad rese, susainedactio, proge action, cntroed reea, extnd action, ime release,epot, and reposit doae foms rtrmsedto idenify drugdelivr sts t a digned t achee apolongedteae
32、utic efc bycontiuousy rleasg medition ove an extnded erir oi afr adiitraion f sinle doe、(2)Wa are te advantages of sustain rase dsage orms?Sice the fequencof drug admnstration isreduced, patentsliance cabe improved, anrugaministation can be de mre cneienas well、s thahe total amountf drug dinistee cn
33、 reduced, ths mxiizi availabliy ith a mini dose、 In adition, bettr control of drug absrio can betaind, ince th hg lod level peas tht ay be observ ater aministaton ofa doe of hih availablity drg ae redce byfrmulion inanexen ion fr、 he aft margin of high otency dugs c eincreasd a the incidenceof bot o
34、cal ad systemic avre si efft c be reded in seniive atients、 Oerall, adminiationof sustaindelease fomsenble ncreae reiabiltyof hrapy、(3)Whatmehods are eploedfor in itr asemen o rug ailablity? sin eie the rtting ket, hepdde, r the mdified disneraion testng aparatus、2、et th psaebeo、 Thefectieneofrugs h
35、erapyorelat in eneral with availabiit ofin vivo dug, wchareiuence by abrption,dispsition, metaoi, exction, nd eimintiono dug intenal body、Sustained releas and sutainedatirtermsusd to ienity rugdeiry syste that are designed toaciee proloned therapeuticffct by continuusly rlaing medctin r an extended
36、peiod of tim、 Trm“controle rlease” hs caed to dlieracatomc predeiedatesver ong priod oftim、 uring h developent stage, the effcto susine relesessimuate by n cito tstingwthte specfication emisil fpharmacopoeia、药物得有效性得治疗相关得一般可用性体内得药物,这就是影响吸收,处置,代谢,排泄,与消除药物在人体内部. 缓释与持续得行动就是用来识别药物输送系统,目得就是实现长期治疗效果得持续释放药物
37、在一段长时间。 术语“控释”相关得救助自动预定率在很长一段时间. 在发展阶段,持续得影响释放模拟在目标测试规范允许得药典。4、吸收Unt16 P1. Anet ollwngquesion:()Wha kn f therector re oten usdin hrmaceutcl fctrie ?All eatos have in monseetechrcterisics offourbai ecor tps:theellstrred bach eor, esemibch reactr, e ntinuous-flow stirred-tank reor, and th tubular cto(Fi、1)、(2)ha ar th advantes ad disadvntges of tetuousl StiredTank eacto?e CSTR is the idealie oposite the welstirredbatch ad ublaugflowretor、 nalysis of selce binaion of hese rac