Introduction to Drugs and Pharmacy

Introduction to Drugs and Pharmacy

A drug is defined as an agent intended.for use in the diagnosis.mitigation.treatment.Cure,or prevention of disease in humans or in other animals.One of the

most astounding qualities of drugs is the diversity of their actions

and effects on the body.This quality enables their selective use in the treatment of a range of common and rare conditions involving virtually every body organ,tissue,and cell.药物被定义为

用于诊断的试剂。缓解。治疗。治疗或预防人或其他动物的疾病。药物最令人震惊的特质之一是它们对身体的作用和影响的多样性。这种质量使其能够选择性地用于治疗涉及几乎每种器官，组织和细胞的一系列常见和罕见病症

Some drugs selectively stimulate the cardiac muscle,the central nervous system,or the gastrointestinal tract,whereas other drugs have the opposite

effect.Mydriatic drugs dilate the pupil of the eye,and miotics constrict or diminish pupillary siz e.Drug can render blood more coagulable or less coagulable;they can increase the hemoglobin reduce serum cholesterol,or expand blood volume.

一些药物选择性地刺激心肌，中枢神经系统或胃肠道，而其他药物具有相反的效果。散瞳药物扩大眼睛的瞳孔，并且缩瞳收缩或减小瞳孔大小。药物可以使血液更可凝固或更少凝固;他们可以增加血红蛋白降低血清胆固醇，或扩大血容量。

Drugs termed emetics induce vomiting,whereas antiemetic drugs prevent vomitingy Diureti c drugs increase the flow of urine;expectorant drugs increase respiratory tract fluid;and catharti cs or laxatives evacuate the bowel.Other drugs decrease the flow of urine,diminish body secreti ons,or induce constipation.称为催眠药的药物诱导呕吐，而止吐药防止呕吐利尿药增加尿流;祛痰药物增加呼吸道液体;和泻药或泻药排泄肠。其他药物减少尿流，减少身体分泌物，或诱导便秘.

Drugs may be used to reduce pain,fever,thyroid activity,rhinitis.insomnia.gastric acidity,mo tion sickness.blood pressure.and mental depression.Other drugs can elevate mood,blood press ure,or activity of the endocrine glands.Drugs can combat infectious

disease,destroy intestinal worms,or act as antidotes against the poisoning effects Drugs can as sist in smoking cessation or alcohol withdrawal or can modify obsessive-compulsive disorders.

药物可用于减轻疼痛，发热，甲状腺活动，鼻炎。失眠。胃酸性，晕动病。血压。和精神抑郁症。其他药物可以提高心情，血压或内分泌腺的活动。药物可以抵抗传染病，破坏肠道蠕虫，或作为解毒剂对抗中毒作用药物可以帮助戒烟或戒酒，或可以修改强迫性强迫症. Drugs are used to treat common infections.AIDS,benign prostatic hyperplasia,cancer,cardiov ascular disease.asthma,glaucoma,Alzheimer's disease,and male impotence.They

can protect against the rejection of transplanted tissues and organs and reduce the incidence of measles and mumps.Antineoplastic drugs provide one means of attacking the cancerous process; radioactive pharmaceuticals provide another.药物用于治疗常见感染。AIDS，良性前列腺增生，癌症，心血管疾病。哮喘，青光眼，阿尔茨海默病和男性阳痿。它们可以防止移植的组织和器官的排斥，并降低麻疹和腮腺炎的发病率。抗肿瘤药物提供了一种攻击癌症过程的方法;放射性药物提供另一种。

Drugs may be used to diagnose diabetes,liver malfunction,tuberculosis,or pregnancy.They c an replenish a body deficient in antibodies,vitamins,hormones,electrolytes,protein,enzymes,o r blood.Drugs can prevent pregnancy,assist fertility,and sustain life itself.药物可用于诊断糖尿

病，肝功能障碍，结核病或怀孕。他们可以补充缺乏抗体，维生素，激素，电解质，蛋白质，酶或血液的身体。药物可以预防怀孕，协助生育，维持生命本身。

Certainly the vast array,of effective medicinal agents available today is one of our greatest scienti fic accomplishments.It

is difficult to conceive our civilization devoid of these remarkable and beneficial agents.Through their use,many of the diseases that have plagued humans throughout history,such

as smallpox and poliomyelitis,are now virtually extinct.Illnesses such as

diabetes,hypertension,and mental depression are effectively controlled with modem

drugs.Today’s surgical procedures would be virtually

impossible without the benefit of anesthetics,analgesics,antibiotics.blood transfusions,and intra venous fluids.当然，今天可用的大量有效的药物是我们最伟大的科学成就之一。很难想象我们的文明没有这些显着和有益的药剂。通过他们的使用，许多疾病，在整个历史中困扰人类，作为天花和脊髓灰质炎，现在几乎灭绝。糖尿病，高血压和精神抑郁症等疾病可用现代药物有效控制。今天的手术操作如果没有麻醉剂，止痛剂，抗生素，输血和静脉注射液的益处，实际上是不可能的

New drugs may be derived from plant or animal sources.as byproducts of microbial growth,or t hrough chemical synthesis,molecular modification,or https://www.wendangku.net/doc/fb1423183.html,puter libraries and data banks of chemical compounds and sophisticated methods of screening for potential biologic activity assist drug discovery.新药可以源自植物或动物来源。作为微生物生长的副产物，或通过化学合成，分子修饰或生物技术。化学化合物的计算机图书馆和数据库以及筛选潜在生物活性的复杂方法有助于药物发现。

The process of drug discovery and development is complex.It entails the collective contributions of many scientific specialists,including organic,physical,and analytical chemists;biochemists;m olecular biologists;bacteriologists;physiologists;pharmacologists',toxicologists;hematologists;i mmunologists;endocrinologists;pathologists;biostatisticians;pharmaceutical scientists;clinical pharmacists;physicians;and many others.药物发现和开发的过程是复杂的。它需要许多科学专家的共同贡献，包括有机，物理和分析化学家;生物化学家分子生物学家;细菌学家生理学家药理学家，毒理学家;血液学家;免疫学家内分泌学家病理学家生物统计学家制药科学家;临床药剂师;医生;和许多其他。

After a potential new drug substance is discovered and undergoes definitive chemical and physic al characterization,a great deal of biologic information must be gathered.The basic pharmacolog y,or the nature and mechanism of action of the drug on the biologic system,must be determine d including toxicologic features.The drug's site and rate of absorption,its pattern of distribution and concentration within the body,its duration of action,and the method and rate of its elimina tion or excretion must be https://www.wendangku.net/doc/fb1423183.html,rmation on the drug's metabolic degradation and the activ ity of any of its metabolites must be obtained.A comprehensive study of the short-term and long -term effects of the drug on various body cells,tissues,and organs must be made.Highly specific information,such as the effect of the drug on the fetus of a pregnant animal or its ability to pass to a nursing baby through the breast milk of its mother,may be obtained.Many a promising new drug has been abandoned because of its potential to cause excessive or hazardous adverse effec ts.在发现潜在的新药物并进行确定的化学和物理表征后，必须收集大量的生物信息。必须确定药物对生物系统的基本药理学或作用的性质和机制，包括毒理学特征。必须研究药物的位点和吸收速率，其在体内的分布和浓度模式，其作用持续时间，以及其消除或排泄的方法和速率。必须获得药物的代谢降解和其任何代谢物的活性的信息。必须对药物对各种体细胞，

组织和器官的短期和长期影响进行全面研究。可以获得高度特异性信息，例如药物对怀孕动物胎儿的作用或其通过其母亲的母乳传递给哺乳婴儿的能力。许多有希望的新药已被放弃，因为其潜在的引起过度或危险的不良反应。

The most effective routes of administration(e.g.,oral,rectal,parenteral,topical)must be determined,and guidelines for the dosages recommended for persons of varying ages(e.g.,neona tes,children.adults,geriatrics),weights,and states of illness have to be established_It has been said that the only difference between a drug and a poison is the.dose.To facilitate administration of the drug by the selected routes,appropriate dosage forms,such as tablets,ca psules,injections,suppositories,ointments,aerosols,and others,are formulated and prepared. Each of these dosage units is designed to contain a specified quantity of medication for ease and accuracy of dosage administration.These dosage forms are highly sophisticated delivery systems. Their design,development,production,and use are the product of application of the pharmaceu tical sciences the blending of the basic,applied,and clinical sciences with pharmaceutical t echnology.必须确定最有效的给药途径（例如口服，直肠，胃肠外，局部），并且推荐用于不同年龄的人（例如新生儿，儿童，成人，老年病）的剂量指南，体重和疾病状态必须建立-据说，药物和毒药之间的唯一区别是药物。为了便于通过所选择的途径给药，配制和制备适当的剂型，例如片剂，胶囊，注射剂，栓剂，软膏剂，气雾剂等。这些剂量单位中的每一个被设计为包含特定量的药物以便于剂量施用的容易性和准确性。这些剂型是高度复杂的递送系统。他们的设计，开发，生产和使用是药物科学应用的基础，应用和临床科学的混合与制药技术的产物。

Each particular pharmaceutical product is a formulation unique unto itself.In addition to the active therapeutic ingredients.a

pharmaceutical formulation contains a number of nontherapeutic or pharmaceutical ingredien ts.It is through their use that a formulation achieves its unique composition and characteristic ph ysical appearance.Pharmaceutical ingredients include such materials as fillers.thickeners,solven ts,suspending agents,tablet coatings and disintegrants,penetration enhancers,stabilizing agents. antimicrobial preservatives,flavors,colorants,and sweeteners.每种药物制剂产品是独特的制剂。除了有助于治疗成分。药物制剂支持多种非疗法或药物成分。通过它们的使用，制剂实现其独特的组成和特征物理外观。药物成分包括诸如填充剂的材料。增稠剂，溶剂，悬浮剂，片剂包衣和崩解剂。渗透促进剂，稳定剂。抗微生物防腐剂，调味剂，着色剂和甜味剂。

To ensure the stability of a drug in a formulation and the continued effectiveness of the drug pro duct throughout its usual shelf life.the principles of chemistry,physical pharmacy.microbiology, and pharmaceutical technology must be applied.The formulation must be such that all compone nts are physically and chemically compatible,including the active therapeutic agents,the pharma ceutical ingredients,and the packaging materials.The formulation must be preserved against dec omposition due to chemical degradation and protected from microbial contamination and the de structive influences of excessive heat,light,and moisture.The therapeutic ingredients must be r eleased from the dosage form in the proper quantity and in such a manner that the onset and du ration of the drug's action is that which is desired.The pharmaceutical product must lend itself to efficient administration and must possess attractive features of flavor,odor,color,and texture t hat enhance acceptance by the patient.Finally,the product must be effectively packaged and cl early and completely labeled according to legal regulations.以确保药物在制剂中的稳定性和药物制剂在其通常的保质期内的持续有效性。化学，物理药学的原则。微生物学和制药技术。

制剂必须是所有组分在物理和化学上相容的，包括活性治疗剂，药物成分和包装材料。该制剂必须防止由于化学降解而分解并防止微生物污染和过热，光和湿气的破坏性影响。治疗成分必须以适当的量和以药物作用的起始和持续时间是所需的方式从剂型中释放。药物产品必须有助于有效给药，并且必须具有增强患者接受的风味，气味，颜色和质地的吸引力特征。最后，产品必须有效包装，并根据法律法规清晰，完整地标记。

Once prepared,the pharmaceutical product must be properly administered if the patient is to receive maximum benefit.The medication must be taken in sufficient quantity,at specified in tervals.and for an indicated duration to achieve the desired therapeutic outcomes.The effective ness of the medication in achieving the prescriber’s objectives should be reevaluated at regular i ntervals and necessary adjustments made in the dosage,regimen,schedule.or from,or indeed,i n the choice of the drug administered.Patients'expressions of disappointment in the rate of pro gress or complaints of side effects to the prescribed drug should be evaluated and decisions mad e as to the continuance,Adjustment,or major change in drug therapy.Before initially taking a m edication,a patient should be advised of any expected side effects and of foods,beverages.and/ or other drugs that may interfere with the effectiveness of the medication.一旦制备，如果患者要获得最大的益处，则必须适当地施用药物产品。药物必须以指定的间隔以足够的量服用。并持续指定的持续时间以实现所需的治疗结果。药物在实现处方者目标方面的有效性应定期重新评估，并在剂量，方案，时间表中进行必要的调整。或来自或实际上选择所施用的药物。应评估患者对进展速度表示失望或对处方药物产生副作用的投诉，并对药物治疗的持续，调整或重大变化做出决定。在开始服用药物之前，应告知患者任何预期的副作用和食物，饮料。和/或可能干扰药物有效性的其它药物。

Through professional interaction and communication with other health professionals the phar macist can contribute greatly to patient care.An intimate knowledge of drug actions,pharmacot herapeutics.formulation and dosage form design.available pharmaceutical products.and drug i nformation sources makes the pharmacist a vital member of the health care team.The pharmaci st is entrusted with the legal responsibility for the procurement,storage,control,and distributio n of effective pharmaceutical products and for the compounding and filling of prescription orders. Drawing on extensive training and knowledge,the pharmacist saves the patient as an advisor on drugs and encourages their safe and proper use.The pharmacist delivers pharmaceutical services in a variety of community and institutional health care environments and effectively uses medic ation records,patient monitoring,and assessment techniques in safeguarding the public health.通过与其他卫生专业人员的专业交流和沟通，药剂师可以大大有助于病人护理。亲密的药物作用知识，药物治疗。制剂和剂型设计。可用的药品。和药物信息源使药剂师成为卫生保健团队的重要成员。药剂师受托负有有效药品的采购，储存，控制和分配以及处方订单的复合和填充的法律责任。借助广泛的培训和知识，药剂师将病人作为一个顾问，保护药物，并鼓励他们安全和正确使用。药剂师在各种社区和机构保健环境中提供药物服务，并有效地使用药物记录，患者监测和评估技术来保护公众健康。

To appreciate the progress that has been made in drug discovery and development and to pro vide background for the study of modern drugs and pharmaceutical dosage forms,it is important to examine pharmacy's heritage.为了欣赏在药物发现和开发方面取得的进展，并为现代药物和药物剂型的研究提供背景，重要的是检查药学的遗产。

The Heritage of Pharmacy

Drugs,in the form of vegetation and minerals have existed as long as humans.Human dis ease and the instinct to survive have led to their discovery through the ages.The use of drugs,cr

ude though they may have been,undoubtedly began long before recorded history,for the instinc t of primitive man to relieve the pain of a wound by bathing it in cool water or by soothing rt wit h a fresh leaf or protecting it with mud is within the realm of belief.From experience.early huma ns would learn that certain therapy was more effective than others,and from these beginnings c ame the practice of drug therapy.药物，以植被和矿物质的形式存在，只要人类。人类疾病和生存的本能导致他们的发现，在年龄。使用药物，尽管他们可能已经，无疑开始很久以前记录的历史，原始人的本能通过沐浴在凉水中或通过舒缓rt与新鲜的叶子或保护它减轻伤口的痛苦泥是在信仰的领域。从经验。早期人类将了解到某些疗法比其他疗法更有效，并且从这些开始出现药物治疗的实践。

Among many early races,disease was believed to be caused by the entrance of demons or evil sp irits into the body.The treatment naturally involved ridding the body of the super-natural intrud ers.From the earliest records,the primary methods of removing spirits were through the use of spiritual incantations,the application of noisome materials,and the administration of specific he rbs or plant materials.在许多早期种族中，疾病被认为是由恶魔或邪灵进入体内造成的。治疗自然涉及消除超自然入侵者的身体。从最早的记录，清除精神的主要方法是通过使用精神咒语，使用噪音材料，以及施用特定的草药或植物材料。

The First Apothecary

Before the days of the priestcraft,the wise man or woman of the tribe,whose knowledge of th e healing qualities of plants had been gathered through experience or handed down by word of mouth,was called upon to attend to the sick or wounded and prepare the remedy.It was in the preparation of the medicinal materials that the art of the apothecary originated.在神职人员的

日子之前，部落的聪明人或女人，他们对植物的愈合品质的知识是通过经验收集或用口碑传下来的，被要求照顾病人或受伤者，并准备补救。它是在药剂的艺术起源的药材的制备。

The art of the apothecary has always been associated with the mysterious,and its practit ioners were believed to have connection with the world of spirits and thus performed as interme diaries between the seen and the unseen.The belief that a drug had magical associations meant t hat its action,for good or

for evil,did not depend upon its natural qualities alone.The compassion of a god.the observance of ceremonies,the absence of evil spirits,and the healing intent of the dispenser were individual ly and collectively needed to make the drug therapeutically effective:Because of this,the tribal a pothecary was one to be feared,respected,trusted,sometimes mistrusted,worshiped,and rever ed.for it was through his potions that spiritual contact was made,and upon that contact the cur es or failures depended.药剂师的艺术一直与神秘有关，并且其实践者被认为与精神世界有联系，因此作为看到的和未见的之间的中介。相信一种药物有神奇的协会意味着它的行动，善良或邪恶，不依赖于它的自然素质单独一个神的同情。遵守仪式，没有邪灵和分配器的愈合目的是个别和共同地需要使药物治疗有效：因为这一点，部落药剂师是一个可怕，尊重，信任，有时不信任，崇拜和敬仰。因为它是通过他的药剂，精神接触，并在这种接触，治愈或失败依赖。

Throughout history,the knowledge of drugs and their application to disease has always mea nt power.In the Homeric epics.the term pharmakon(Gr.),from which our word pharmacy was derived,connotes a charm or a drug that can be used for good or for evil.Many of the tribal ap othecary's failures were doubtless due to impotent or inappropriate medicines,underdosage,ov erdosage,and even poisoning.Successes may be attributed to experience,mere coincidence of appropriate drug selection,natural healing,inconsequential effect of the drug.or placebo effects,

that is,successful treatment due to psychologic rather than therapeutic effects.Even today,pla cebo therapy with inert or inconsequential chemicals is used successfully to treat individual patie nts and is a routine practice in the clinical evaluation of new drugs,in which subjects'respouses to the effects of the actual drug and the placebo are compared and evaluated.纵观历史，药物的知识及其对疾病的应用总是意味着权力。在荷马史诗。我们的词药房派生的术语pharmakon （Gr。）意味着可以用于善良或邪恶的魅力或药物。许多部落药剂师的失败无疑是由于无能或不适当的药物，剂量不足，过量，甚至中毒。成功可能归因于经验，只是巧合的适当的药物选择，自然愈合，药物的无关紧要的效果。或安慰剂效应，即由于心理而不是治疗效果的成功治疗。即使在今天，使用惰性或无关紧要的化学物质的安慰剂治疗成功地用于治疗个体患者，并且是新药物的临床评价中的常规实践，其中比较和评价受试者对实际药物和安慰剂的影响的响应。

As time passed,the art of the apothecary combined with priestly functions,and among the ear ly civilizations,the priest-magician or priest-physician became the healer of the body as well as of the soul.Pharmacy and medicine are indistinguishable in their early history because their practic e was the combined function of the tribal religious leaders.随着时间的流逝，药剂师的艺术与神职人员的功能，以及在早期的文明，牧师，魔术师或牧师医生成为身体和灵魂的治疗者。药学和药物在他们的早期历史上是无法区分的，因为他们的实践是部落宗教领袖的组合功能。

Tables

Tablets are solid dosage forms usually prepared with the aid of suitable pharmaceutical excipient s.They may vary in size.shape,weight.hardness,thickness,disintegration,and dissolution chara cteristics and in other aspects,depending on their intended use and method of manufacture.Mo st tablets are used in the oral administration of drugs.Many of these are prepared with colorants and coatings of various types.Other tablets,such as those administered sublingually,buccally,o r vaginally,are prepared to have features most applicable to their particular route of administrati on.Advantages of tablets for oral administration are presented in an earlier chapter.片剂是通

常在合适的药物赋形剂的帮助下制备的固体剂型。它们的大小可能不同。形状，重量。硬度，厚度，崩解和溶解特性，在其它方面，取决于它们的预期用途和制造方法。大多数片剂用于药物的口服给药。许多这些是用各种类型的着色剂和涂层制备的。其它片剂，例如舌下，口腔或阴道给药的那些，被制备成具有最适用于其特定给药途径的特征。用于口服给药的片剂的优点在前面的章节中给出.

Tablets are prepared primarily by compression,with a

limited number prepared by https://www.wendangku.net/doc/fb1423183.html,pressed tablets are manufactured with tablet machine s capable of exerting great pressure in compacting the powdered or granulated material.Their sh ape and dinmensions are determined by use of various shaped punches and dies.Molded tablets are prepared on a large-scale by tablet machinery or on a small-scale by manually forcing dampe ned powder material into a mold from which the formed tablet is then ejected and allowed to dr y.片剂主要通过压制制备，通过模制制备有限数量。压制片由能够在压实粉末状或颗粒状材料中施加巨大压力的压片机制造。它们的形状和尺寸通过使用各种形状的冲头和模具来确定。模制片剂通过片剂机械大规模制备或小规模制备，通过手动迫使阻尼的粉末材料进入模具中，然后将形成的片剂从模具中取出并使其干燥.

Types of Tables类型的表

The various types of tablets are described as follows,with their common abbreviations in parent heses.各种类型的片剂描述如下，其括号中的通用缩写。

Compressed Tablets.压缩片

In addition to the medicinal agent or agents,compressed tablets usually contain a number o f pharmaceutical adjuncts.including the following:除了一种或多种药物之外，压制片剂通常含有许多药物添加剂。包括以下内容:

Diluents or fillers.which add the necessary bulk to a formulation(o prepare tablets of the desir ed size

Binders or adhesives,which promote adhesion of the particles of the formulation,allowing a gra nulation to be prepared and maintaining the integrity of the final tablet.稀释剂或填料。其向制剂中加入必要的松厚度（o制备所需尺寸的片剂）

粘合剂或粘合剂，其促进制剂的颗粒的粘附，允许制备颗粒并保持最终片剂的完整

性

Disintegrants or disintegrating agents,which promote administration to smaller particles for read y drug availability崩解剂或崩解剂，其促进对较小颗粒的给药以便即时获得药物Antiadherents,glidants,lubricants,or lubricating agents,which enhance the flow of the mat erial into the tablet dies,minimize wear of the punches and dies,prevent fill material from sticki ng to the punches and dies,and produce tablets with a sheen增强材料流入片剂模具中的抗粘附剂，助流剂，润滑剂或润滑剂使冲头和模具的磨损最小化，防止填充材料粘到冲头和模具上，并产生具有光泽的片剂

After compression,tablets may be coated with various materials as described later.Tablets for or al,buccal,sublingual,or vaginal administration may be prepared by compression.压缩后，片剂可以用如下所述的各种材料包衣。用于口服，口腔，舌下或阴道给药的片剂可通过压制制备.

Multiply Compressed Tablets多重压缩片剂

Multiply compressed tablets are prepared by subjecting the fill material to more than a single compression.The result may be a multiple layer tablet or a tablet within a tablet,the inner tablet being the core and the outer portion being the https://www.wendangku.net/doc/fb1423183.html,yered tablets are prepared by initial com paction of a portion of fill material in a die followed by additional fill material and compression to form two-or three-layered tablets.depending on the number of separate fills.Each layer may co ntain a different medicinal agent,separated for reasons of chemical or physical incompatibility,s taged drug release.or simply for the unique appearance of the layered https://www.wendangku.net/doc/fb1423183.html,ually,each porti on of fill is a different color to produce a distinctive-looking tablet.In preparation of tablets withi n tablets,special machines are required to place the preformed core tablet precisely within the d ie for application of surrounding fill material.通过使填充材料经受多于单次压缩来制备多重压缩片剂。结果可以是多层片剂或片剂内的片剂，内片剂是核心，外部分是外壳。通过在模具中初始压实填充材料的一部分，然后通过另外的填充材料并压缩以形成两层或三层的片剂来制备层状片剂。取决于单独填充的数量。每个层可以包含不同的药剂，由于化学或物理不相容性的原因分开，分阶段的药物释放。或简单地用于层状片剂的独特外观。通常，填充的每个部分是不同的颜色以产生独特的平板。在片剂内制备片剂中，需要特殊的机器将预成形的片剂片剂精确地放置在模具内用于施加周围的填充材料.

Sugarcoated Tablets糖衣片

Compressed tablets may be coated with a colored or an uncolored sugar layer.The coating i s water soluble and quickly dissolves after swallowing.The sugarcoat protects the enclosed drug

from the environment and provides a barrier to objectionable taste or odor.The sugarcoat also e nhances the appearance of the compressed tablet and permits imprinting of identifying manufac turer's information.Among the disadvantages to sugarcoating tablets are the time and expertise required in the coating process and the increase in size.weight,and shipping costs.Sugarcoating may add50%to the weight and bulk of the uncoated tablet.压制片可以用有色或未着色的糖

层包衣。涂层是水溶性的，并且在吞咽后快速溶解。糖衣保护封闭的药物免受环境的影响，并提供对令人不快的味道或气味的屏障。糖衣还增强了压缩片剂的外观，并允许识别制造商的信息的印记。包衣片的缺点是包衣过程中所需的时间和专业知识以及尺寸的增加。重量和运输成本。糖衣可以为未包衣片剂的重量和体积增加50%.

Film-Coated Tablets薄膜包衣片

Film-coated tablets are compressed tablets coated with a thin layer of a polymer capable of forming a skinlike film.The film is usually colored and has the advantage over sugarcoatings in that it is more durable,less bulky,and less time consuming to apply.By its composition,the coati ng is designed to rupture and expose the core tablet at the desired location in the gastrointestina l tract.膜包衣片剂是用能够形成皮肤膜的聚合物的薄层包衣的压制片剂。该膜通常是有色的并且具有优于糖衣的优点，因为它更耐用，体积更小，并且施用时间更少。通过其组成，涂层被设计成在胃肠道中的期望位置破裂并暴露片芯片。

Gelatin-Coated Tablets明胶包衣片

A recent innovation is the gelatin-coated tablet.The innovator product.the gelcap,is a caps ule-shaped compressed tablet that allows the coated product to be about one-third smaller than a capsule filled with an equivalent amount of powder.The gelatin coating facilitates swallowing, and gelatin-coated tablets are more tamper evident than unsealed capsules.最近的创新是明胶包衣片剂。创新产品。凝胶帽是胶囊形压片，其允许包衣产品比填充有等量粉末的胶囊小约三分之一。明胶包衣有利于吞咽，并且明胶包衣片剂比未包封的胶囊更容易被篡改。Enteric-Coated Tablets包衣片

Enteric-

coated tablets have delayed-release features.They are designed to pass unchanged through the stomach to the intestines,where tablets disintegrate and allow drug dissolution and absorption a nd/or effect.Enteric coatings are employed when the drug substance is destroyed by gastric acid or is particularly irritating to the gastric mucosa or when bypass of the stomach substantially enh ances drug absorption.肠溶片具有延迟释放特征。它们被设计成不变地通过胃到肠，其中片剂崩解并允许药物溶解和吸收和/或效果。当药物被胃酸破坏或对胃粘膜特别刺激或当绕过胃显着增强药物吸收时，使用肠溶包衣。

Buccal and Sublingual Tablets

Buccal and sublingual tablets are flat oval tablets intended to be dissolved in the buccal pouch(b uccal tablets)or beneath the tongue(sublingua tablets)for absorption through the oral mucosa. They enable oral absorption of drugs that are destroyed by the gastric juice and/or are poorly ab sorbed from the gastrointestinal tract.Buccal tablets are designed to erode slowly,,whereas tho se for sublingual use(such as nitroglycerin)dissolve promptly and provide rapid drug effects.Loz enges or troches are disc-shaped solid dosage forms containing a medicinal agent and generally a flavoring substance in a hard candy or sugar base.They are intended to be slowly dissolved in th e oral cavity,usually for local effects,although some are formulated for systemic absorption.颊

和舌下片是旨在溶解在口腔袋（颊含片）或舌下（舌下片）的扁平椭圆形片，用于通过口腔粘膜吸收。它们能够口服吸收被胃液破坏和/或从胃肠道吸收不良的药物。颊片设计为缓

慢侵蚀，而舌下使用（例如硝酸甘油）的那些片剂迅速溶解并提供快速的药物效果。锭剂或锭剂是在硬糖或糖基中含有药剂和通常为调味物质的盘状固体剂型。它们旨在缓慢溶解在口腔中，通常用于局部效果，尽管一些被配制用于全身吸收。

Chewable Tabtets

Chewable tablets,which nave a smooth,rapid disintegration when chewed or allowed Lo dissolv e in the mouth,have a creamy base,usually of specially flavored and colored mannitol Chewable tablets are especially useful for a-ministration of large tablets to children and adults who have dif ficulty swallowing solid dosage forms.咀嚼片，当咀嚼或允许时具有平滑，快速崩解在口中溶解，具有乳脂状基质，通常具有特别调味和着色的甘露糖醇咀嚼片特别用于将大片剂分配给儿童和成人难以吞咽固体剂型

Effervescent Tablets

Effervescent tablets are prepared by compressing granular effervescent salts that release gas wh en in contact with water.These tablets generally contain medicinal substances that dissolve rapi dly when added to water.通过压缩当与水接触时释放气体的颗粒状泡腾盐来制备泡腾片剂。这些片剂通常含有当加入水时迅速溶解的药物物质。

Molded Tablets

Certain tablets.such as tablet tritumtes.mayhe prepared by molding rather,by compression.T he resultant tablets are very soft and soluble and are designed for rapid dissolution.某些片。例如片剂研磨剂。而是通过压缩而成型。所得片剂非常软且可溶并且设计用于快速溶解. Tablet Triturates

Tablet triturates are https://www.wendangku.net/doc/fb1423183.html,ually cylindrical,molded or compressed tablets containing

small amounts of usually potent drug.Today only a few tablet triturate products are available co mmercially,with most of these produced by tablet compression.Since tablet triturates must be r eadily and completely soluble in water,only a minimal amount of pressure is applied during their manufacture.A combination of sucrose and lactose is usually the diluent.The few tablet triturate s that remain are used sublingually.such as nitroglycerin tablets.片剂研磨小。通常为圆柱形，含有少量通常有效药物的模制或压制片剂。今天只有几种片剂研磨产品可商购，其中大部分是通过片剂压片产生的。由于片剂研磨剂必须容易且完全溶于水，在其制造过程中仅施加最小量的压力。蔗糖和乳糖的组合通常是稀释剂。保留的少量片剂研磨剂是舌下使用的。如硝酸甘油片。

Pharmacists also employ tablet triturates in compounding.For example.triturates are inserted into capsules or dissolved in liquid to provide accurate amounts of potent drug substances.药剂师还聘请研制片剂配制。例如.研制插入胶囊或溶解在液体提供强效的药物准确数量Hypodermic Tablets

Hypodermic tablets are no longer available in the United States.They were originally used by phy sicians in extemporaneous preparation of parenteral solutions.The required number of tablets w as dissolved in a suitable vehicle,sterility attained,and the injection performed.The tablets were a convenience,since they could be easily carried in the physician's medicine bag and injections p repared to meet the needs of the individual patients.However.the difficulty in achieving sterility, and the availability of prefabricated injectable products,Some in disposable syringes,have elimi nated the need for hypodermic tablets.皮下注射片在美国已不再可用。它们最初由医生临时制备胃肠外溶液使用。将所需数量的片剂溶解在合适的载体中，达到无菌，并进行注射。片剂是方便的，因为它们可以容易地携带在医生的药袋中并且注射剂被制备以满足个体患者的

需要。但是。实现无菌的难度和预制的可注射产品的可用性。一次性注射器中的一些消除了对皮下片剂的需要。

Dispensing Tablets

Dispensing tablets are no longer in use.They might better have been termed compounding table ts because the pharmacist used them to compound prescriptions;they were not dispensed as su ch to the patient.The tablets contained large amounts of highly potent drug substances.so that t he pharmacist could rapidly obtain premeasured amounts for compounding multiple dosage units.These tablets had the dangerous potential of being inadvertently dispensed as such to patie nts.药片不再使用。他们可能更好地称为复合片，因为药剂师使用它们复方药;它们不是这样分配给患者。片剂含有大量高度有效的药物物质。使得药剂师可以快速获得用于配制多个剂量单位的预测量。这些片剂具有被无意地分配给患者的危险潜力。

Immediate-Release Tablets

Immediate-release tablets are designed to disintegrate and release their medication with no spec ial rate-controlling features,such as special coatings and other techniques.立即释放片剂被设计为崩解和释放它们的药物，没有特殊的速率控制特征，例如特殊的涂层和其他技术Instantly Disintegraing or Dissolving Tablets

Instant-release tablets(rapidly dissolving tablets disintegrating or dissolving in the mouth within I minute,or RDTs)are characterized by some within l0seconds(e.g.,Claritin Reditabs[Ioraladin e],Schering).Tablets of this type are designed for children and the elderly or for any patient wh o has difficulty in swallowing tablets.They liquefy on the tongue,and the patient swallows the liq uid.A number of techniques are used to prepare these tablets,including lyophilization(e.g.,Zydi s,R.P.Scherer),soft direct compression(e.g.,Wow-Tab,Yamanouchi-Shaklee Pharma),and othe r methods(e.g.,Quicksolv,Janssen).These tablets are prepared using very water-soluble excipie nts designed to wick water into the tablet for rapid disintegration or dissolution.They have the st ability characteristics of other solid dosage forms.速释片（在1分钟内崩解或溶解在口中的快速溶解片剂，或RDT）的特征在于在10秒内有一些（例如，Claritin Reditabs[Ioraladine]，Schering）。这种类型的片剂是为儿童和老年人或任何难以吞咽片剂的患者设计的。它们在舌头上液化，并且患者吞咽液体。许多技术用于制备这些片剂，包括冻干（例如Zydis，R.P.Scherer），软直接压片（例如Wow-Tab，Yamanouchi-Shaklee Pharma）和其它方法（例如Quicksolv，Janssen）。这些片剂使用非常水溶性的赋形剂制备，所述赋形剂设计成将水芯吸入片剂中以快速崩解或溶解。它们具有其他固体剂型的稳定性.

The original fast-dissolving tablets were molded tablets for sublingual use.They generally cons isted of active drug and lactose moistened with an alcohol-water mixture to form a paste.The ta blets were then molded,dried,and packaged.For use,they were simply placed under the tongue to provide a rapid onset of action for drugs such as nitroglycerin.Also,they have been used for d rugs that are destroyed in the gastrointestinal tract,such as testosterone,administered sublingu ally for absorption to minimize the first-pass effect.原来的速溶片剂是用于舌下使用的模制片剂。它们通常由活性药物和用醇-水混合物润湿的乳糖组成以形成糊剂。然后模制，干燥和包装片剂。为了使用，将它们简单地放置在舌下以对诸如硝酸甘油的药物提供快速起效。此外，它们已经用于在胃肠道中被破坏的药物，例如睾酮，舌下给药用于吸收以最小化首过效应。

The new RDTs are designed for oral use by patients who have difficulty swallowing standard tablets and capsules.such as children and the elderly.These RDTs are more convenient to carry a nd administer than an oral liquid.There are no standards that define a RDT.but one possibility is

dissolution in the mouth within approximately15to30seconds;anything slower would not be c ategorized as rapidly dissolving.新的RDT设计用于吞咽标准片剂和胶囊有困难的患者口服使用。如儿童和老人。这些RDT比口服液体携带和施用更方便。没有定义RDT的标准。但一种可能性是在约15至30秒内在口中溶解;任何较慢的不会被归类为快速溶

解。

Not withstanding these advantages,there are a number

of disadvantages and difficulties associated with formulating RDTs.including drug

loading.taste masking,friability,manufacturing costs,and stability of the product.不考虑这些

优点，存在与配制RDT相关的许多缺点和困难。包括药物装载。味道掩蔽，脆性，制造成本和产品的稳定性。

Drug loading is incorporation of the drug into the dosage form.Some RDTs are made as blanks t o which a drug is post loaded,or added after the blank is made.Generally the drug is in solution and is added to the tablet,after Which the solvent evaporates.It is also possible for the drug to be added as a dry powder electrostatically at this stage.Most drugs,however,are incorporated into the tablets during manufacturing.药物装载是将药物掺入到剂型中。一些RDT制成空白，药物被后加载，或在空白制成后添加。通常，药物在溶液中并加入到片剂中，之后溶剂蒸发。在该阶段静电地加入药物作为干粉也是可能的。然而，大多数药物在制造期间并入片剂中.

Taste masking poses numerous challenges for RDTs.Since the drug product dissolves in the mou th,any taste of the drug must be covered,either by a flavoring technique or by microencapsulati on or nanoencapsulation.The product also should not be gritty,which necessitates very small pa rticle sizes if micraencapsulation is used.味道掩蔽对RDT提出了许多挑战。由于药物产品溶解在口中，所以必须通过调味技术或通过微胶囊化或纳米包封来覆盖药物的任何味道。该产品也不应该是砂砾的，如果使用微胶囊化，这就需要非常小的颗粒尺寸。

Friability is an inherent problem in RDTs.For a product to dissolve instantly.it may be quite friabl e.Making it more firm and less friable may increase dissolution time.A balance generally must b e achieved between friability and speed of dissolution.易碎性是RDT中的固有问题。对于产品立即溶解。它可能是相当易碎。使其更坚固和更不易碎可增加溶解时间。通常必须在脆性和溶解速度之间实现平衡。

Lyophilized Foam

The first entry into the RDT field was the Zydis delivery system.The tablets are prepared by foaming a mixture of gelatin.sugar or sugars,drug,and any other components and pouring th e foam into a mold.The mold also serves as the unit dose dispensing package.The foam is lyophil ized,and the tablets in the mold are packaged.This system is the fastest disintegrating on the ma rket,as the tablets will dissolve on the tongue in a matter of a few seconds.One disadvantage of this method is that taste masking can be a problem.since the drug is incorporated during the for mation of the tablet itself.Another difficulty is that these tablets are sometimes difficult to remo ve from the packaging,since they are soft and one should not press on the dosage unit to remov e it but should peel off the material,exposing the tablet in its mold.进入RDT字段的第一个条目是Zydis传递系统。片剂通过发泡明胶的混合物制备。糖或糖，药物和任何其它组分，并将泡沫倒入模具中。模具还用作单位剂量分配包装。将泡沫冻干，并且包装模具中的片剂。该系统是市场上最快的崩解剂，因为片剂将在几秒钟内溶解在舌头上。该方法的一个缺点是味道掩蔽可能是一个问题。因为药物在片剂本身的形成过程中掺入。另一个困难是这些

片剂有时难以从包装中取出，因为它们是软的，并且不应当压在剂量单元上以除去它，而是应该从材料上剥离，使片剂在其模具中暴露

Claritin(loratadine)rapidly disintegrating tablets(Reditabs,Schering Corporation)contain l 0mg of micronized loratadine in a base containing citric acid.gelatin,mannitol,and mint flavor f ormed with the Zydis technology.It disintegrates within seconds after being placed on the tongu e,with or without water.Claritin Reditabs have been shown to provide at least equivalent pharm acokinetic parameters to those of traditional tablets in some cases the Reditabs provided greater maximum concentration(C max)and area under the curve(AUC)values.Claritin Reditabs are blis ter packaged tablets that should be stored in a dry place at2℃to25℃.They should be used wit hin6months of opening the protective laminated foil pouch cantaining the blister cards:each fo il pouch contains one blister card containing l0individually sealed tablers(1).Other commercial products using this technology include the Maxah-MLT(Merck).Zofran ODT(GlaxoS mithKlinc).and Zyprexa Zydis(Eli Lilly)tablets.开瑞坦（氯雷他定）快速崩解片（Reditabs，先灵葆雅公司）在含有柠檬酸的碱中含有10mg的微粉化氯雷他定。明胶，甘露醇和用Zydis 技术形成的薄荷香料。它在放置在舌头上后，在有或没有水的情况下在几秒钟内崩解。已经显示开瑞坦Reditab提供与传统片剂至少相当的药代动力学参数，在一些情况下，Reditabs 提供更大的最大浓度（C max）和曲线下面积（AUC）值。开瑞坦Reditabs是泡罩包装片，应储存在2℃至25℃的干燥处。他们应该在6个月内使用保护层压箔袋保持吸塑卡：每个铝箔袋包含一个吸塑卡包含10个单独密封的片剂（1）。使用这种技术的其他商业产品包括Maxah-MLT（Merck）。Zofran ODT（GlaxoSmithKlinc）。和Zyprexa Zydis（Eli Lilly）片剂。

Compression

Another method of preparation is using standard tableting technology with a composition that enhance fluid uptake and tablet disintegration and dissolution.For example,super-disintegrant s incorporated with a small quantity of effervescent material will lead to intermediately fast disin tegration.The tablets are compressed a little thinner than standard tablets to allow for a larger s urface area exposed to the saliva in the mouth.Upon placement in the mouth,the disintegrant st arts wicking water into the tablet.The effervescent materials start dissolving and aid in the break up.This continues until the tablet has disintegrated.另一种制备方法是使用具有增强流体吸收和片剂崩解和溶解的组合物的标准压片技术。例如，与少量泡腾材料结合的超级崩解剂将导致中间快速崩解。将片剂压缩得比标准片剂薄一些，以允许暴露于口腔中的唾液的较大表面积。在放入口中时，崩解剂开始将水吸入片剂中。泡腾材料开始溶解并帮助分解。这继续直到片剂崩解。

An example product is the Dimetapp ND Orally Disintegrating Tablet(Non-Drowsy Allergy Tab lets).These tablets contain loratadine10mg in a vehicle of artificial and natural flavor,aspartam e,citric acid,colloidal silicon dioxide,corn syrup solids,crospovidone,magnesium stearate.man nitol.microcrystalline cellulose,modified food starch,and sodium bicarbonate.一个示例产品是Dimetapp ND口腔崩解片剂（非嗜睡过敏片剂）。这些片剂在人工和天然香料，阿斯巴甜，柠檬酸，胶态二氧化硅，玉米糖浆固体，交聚维酮，硬脂酸镁的载体中含有氯雷他定10mg。甘露醇。微晶纤维素，改性食品淀粉和碳酸氢钠。

One product using the DuraSolv and OraSolv technologies by Cima Labs is Tempra Quicklets cont aining acetaminophen80mg.These tablets also contain aspartame,citric acid,DC Red No.27La ke,FDC Blue No.1Lake,flavor,magnesium stearate,mannitol,potassium carbonate,silicon dioxi de.and sodium.bicarbonate.They are somewhat slower than the Zydis tablet,taking about30t

o45seconds,unless some tongue pressure is used.These tablets come in a firm molded plastic p ackage to prevent breakage(3).Orher commercial products using the same technology include t he Alavert(Wyeth Consumer Healthcare),NuLev(Schwarz Pharma),Remeron SoITabs(Organon Teknika),Triaminic Softchews(Novartis PharmaceuticaJ),and the Zomig Rapidmeh(Zeneca Phar maceuticaFs).使用Cima Labs的DuraSolv和OraSolv技术的一种产品是包含对乙酰氨基酚

80mg的Tempra Quicklets。这些片剂还含有阿斯巴甜，柠檬酸，DC Red No27Lake，FDC Blue No.1Lake，香料，硬脂酸镁，甘露醇，碳酸钾，二氧化硅。和碳酸氢钠。他们比Zydis平板稍慢，大约30到45秒，除非使用舌头压力。这些片剂有一个坚固的塑料包装，以防止破损（3）。使用相同技术的Orher商业产品包括Alavert（Wyeth Consumer Healthcare），NuLev（Schwarz Pharma），Remeron SoITabs（Organon Teknika），Triaminic Softchews（Novartis PharmaceuticaJ）和Zomig Rapidmeh（Zeneca PharmaceuticaFs）

The Flashtab technology by Ethypharm is used in Excednn QuickTabs and an example of the W owtab technology by Yamanouchi Pharma is the Benadryl FastmeIt.

Ethpharm的Flashtab技术用于Excedrin QuickTabs，Yamanouchi Pharma的Wowtab技术的一个例子是Benadryl FastmeLt。

Extended-Release Tablets

Extended-release tablets(sometimes called controlled release CR tablets)are designed to releas e their medication in a predetermined manner over an extended period.They are discussed in Ch apter9.延长释放片剂（有时称为控释CR片剂）被设计为在预定的时间内释放其药物。他们在第9章中讨论

Vaginal Tablets

Vaginal tablets,also called vaginal inserts,are uncoated bullet-shaped or ovoid tablets inserted i nto the vagina for local effects,They are prepared by compression and shaped to fit snugly on pl astic inserter devices that accompany the product.They contain antibacterials for the treatment of vaginalis caused by Haemophilus vaginalis or antifungals for the treatment of vulvovaginitis ca ndidiasis caused by Candida阴道片剂，也称为阴道插入物，是未插入的子弹形状或卵形片插入阴道中用于局部效果。它们通过压缩制备并成形为贴合地贴合在伴随产品的塑料插入装置上。它们由阴道嗜血杆菌或抗真菌药物用于治疗阴道炎白念感染引起滴虫的治疗药物念珠菌引起的

Solutions

In physicochemical terms,solutions may be prepared from any combination of solid,liquid,and gas,the three states of matter.For example,a solid solute may be dissolved in another solid,a liquid,or a gas,and the same being true for a liquid solute and for a gas,nine types of homogeneous mixtures are possible.In pharmacy,however,interest in solutions is for the most part limited to preparations of a solid,a liquid,and less frequently a gas solute in a liquid solvent.在物理化学术语中，可以从固体，液体和气体的任何组合制备三种物质状态的溶液。例如，固体溶质可以溶解在另一种固体，液体或气体中，并且是真实的对于液体溶质和气体，九种类型的均匀混合物是可能的。然而，在药学中，对溶液的兴趣主要局限于固体，液体的制备，并且较不常见地是液体溶剂中的气体溶质。

In pharmaceutical terms,solutions are”liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents”.Because of a particular pharmaceutical solution’s use,it may be classified as oral,otic,ophthalmic,or topical.Still other solutions,because of their composition or use,may be classified as other dosage forms.For

example,aqueous solutions containing a sugar are classified as syrups;sweetened hydroalcoholic (combinations of water and ethanol)solutions are termed elixirs;solutions of aromatic materials are termed spirits if the solvent is alcoholic or aromatic waters if the solvent is aqueous.Solutions prepared by extracting active constituents from crude drugs are termed tinctures or fluidextracts,depending on their method of preparation and concentration.Tinctures may also be solutions of chemical substances dissolved in alcohol or in a hydroalcoholic solvent.Certain solutions prepared to be sterile and pyrogen free and intended for parenteral administration are classified as injections.Although other examples could be cited,it is apparent that a solution,as a distinct type of pharmaceutical preparation,is much further defined than the physicochemical definition of the term solution.在药物术语中，溶液是“含有一种或多种化学物质溶解在合适的溶剂或相互混溶的溶剂的混合物中的液体制剂”。由于特定的药物溶液的用途，它可以分为口服，耳用，眼用或局部由于其组成或用途，其它溶液可以分类为其它剂型。例如，含有糖的水溶液被分类为糖浆;增甜的水醇（水和乙醇的组合）溶液被称为酏剂;芳香剂的溶液如果溶剂是水性的，则如果溶剂是醇或芳香族水，则材料被称为烈酒。根据它们的制备方法和浓度，从生药中提取活性成分制备的溶液称为酊剂或氟化物提取物。化合物也可以是化学物质溶解在醇中或在水醇溶剂中。一些制备为无菌和无热原且旨在用于胃肠外给药的溶液被分类为注射剂。虽然可以列举其它实例，但显然作为不同类型的药物制剂的溶液，比术语溶液的物理化学定义进一步定义。

Oral solutions,syrups,elixirs,spirits,and tinctures are prepared and used for the specific effects of the medicinal agents they carry.In these preparations,the medicinal agents are intended to provide systemic effects.The fact that they are administered in solution form usually means that they are soluble in aqueous systems and that their absorption from the gastrointestinal tract into the systemic circulation may be expected to occur more rapidly than from suspension or solid dosage forms of the same medicinal agent.口服溶液，糖浆，酏剂，酒和酊剂被制备并用于它们携带的药剂的具体作用。在这些制剂中，药剂旨在提供全身效应。事实上，它们以溶液形式给药，通常意味着它们可溶于水性系统中，并且它们从胃肠道到体循环中的吸收可以预期比相同药剂的悬浮液或固体剂型更快地发生。

Solutes other than the medicinal agent are usually present in orally administered solutions.Th ese additional agents usually are included lo provide color,flavor,sweetness,or stability.In form ulating or compounding a pharmaceutical solution,the pharmacist must use information on the solubility and stability of each salute with regard to the solvent or solvent https://www.wendangku.net/doc/fb1423183.html,binations of medicinal or pharmaceutic agents that will result in chemical or physical interactions affecting the therapeutic quality or pharmaceutic stability of the product must be avoided.除了药物之外的溶质通常存在于口服给药的溶液中。通常包括这些另外的试剂以提供颜色，风味，甜味或稳定性。在配制或配制药物溶液时，药剂师必须使用关于溶剂或溶剂系统的每个凉味剂的溶解度和稳定性的信息。必须避免将导致影响产品的治疗质量或药物稳定性的化学或物理相互作用的药物或药物试剂的组合。

For single.solute solutions and especially for multiple-solute solutio ns,the pharmacist must be aware of the solubility characteristics of the solutes and the features of the common pharmaceutical solvents. Each chemical agent has its own solubility in a given solvent.For many medicinal agents,their solubilities in the usual solvents are stated in the United States Pharmacopeia-National Formulary(USP-NF) as well as in other reference books.对于单一绝对溶液，特别是对于多溶质溶

液，药剂师必须知道溶质的溶解度特性和常用药物溶剂的特征。每种化学试剂在给定溶剂中具有其自身的溶解度。对于许多药剂，它们在通常溶剂中的溶解度在美国药典-国家处方集（USP-NF）以及其它参考书中有所说明。.

Solubility

Attractive forces between atoms lead to the formation of molecules and ions.The intermolecular forces,which are developed between like molecules,are responsible for the physical state(solid, liquid,or gas)of the substance under given conditions,such as temperature

and pressure.Under ordinary conditions,most organic compounds,and thus most drug form mol ecular solids.原子之间的吸引力导致分子和离子的形成。在类似分子之间形成的分子间力负责物质在给定条件（例如温度和压力）下的物理状态（固体，液体或气体）。在普通条件下，大多数有机化合物，因此大多数药物形成分子固体。

When molecules interact,attractive and repulsive forces are in effect.The attractive forces cause the molecules to cohere,whereas the repulsive forces prevent molecular interpenetration and d estruction.When the attractive and repulsive forces are equal,the potential energy between tw o molecules is minimum and the system is most stable.当分子相互作用时，吸引力和排斥力是有效的。吸引力使分子粘合，而排斥力防止分子的相互渗透和破坏。当吸引力和排斥力相等时，两个分子之间的势能最小，系统最稳定

Dipolar molecules frequently tend to align themselves with other dipolar molecules so th at the negative pole of one molecule points toward the positive pole of the https://www.wendangku.net/doc/fb1423183.html,rge groups of molecules may be associated through these weak attractions,known as dipole-dipole or van der Waals forces.Other attractions also occur between polar and nonpolar molecules and ions. These include ion-dipole forces and hydrogen bonding.The latter is of particular interest.Becaus e of small size and large electrostatic field,the hydrogen atom can move in close to an electrone gative atom,forming an electrostatic type of association,a hydrogen bond or hydrogen bridge.H ydrogen bonding involves strongly electronegative atoms such as oxygen,nitrogen,and fluorine. Such a bond exists in water,represented by the dotted lines:双极分子通常倾向于使其自身与其它偶极分子对准，使得一个分子的负极指向另一个的正极。大组的分子可以通过这些弱的吸引力相关联，称为偶极-偶极或范德华力。其他吸引力也发生在极性和非极性分子和离子之间。这些包括离子-偶极力和氢键。后者是特别感兴趣的。由于小尺寸和大静电场，氢原子可以移动靠近电负性原子，形成静电类型的缔合，氢键或氢桥。氢键涉及强电负性原子，例如氧，氮和氟。这种键存在于水中，由虚线表示：

Hydrogen bonds also exist between some alcohol molecules,esters,carboxylic acids,aldehydes, and polypeptides.一些醇分子，酯，羧酸，醛和多肽之间也存在氢键

When a solute dissolves,the substance's intermolecular forces of attraction must be overcome b y forces of attraction between the solute and solvent molecules.This entails breaking the solute-solute forces and the solvent-solvent forces to achieve the solute-solvent attraction.当溶质溶解时，物质的分子间吸引力必须通过溶质和溶剂分子之间的吸引力克服。这需要破坏溶质-溶质力和溶剂-溶剂力以实现溶质-溶剂吸引。

The solubility of an agent in a particular solvent indicates the maximum concentration to wh ich a solution may be prepared with that agent and that solvent.When a solvent at a given temp erature has dissolved all of the solute it can,it is said to be saturated.To emphasize the possible variation in solubility between two chemical agents and therefore in the amounts of each require d to prepare a saturated solution,two official aqueous saturated solutions are cited as examples, Calcium Hydroxide Topical https://www.wendangku.net/doc/fb1423183.html,P,and Potassium.Iodide Oral Solution,USP.The first solu

tion.prepared by agitating an excess amount of calcium hydroxide with purified water:contains only about140mg of dissolved solute per l00mL of solution at21C,whereas potassium iodide so lution contains about100g of solute per l00mL of solution,more than700rimes as much solute as in the calcium hydroxide topical solution.Thus the maximum possible concentration to which a pharmacist may prepare a solution varies greatly and depends in part on the chemical constitut ion of the solute.Through selection of a different solubilizing agent or a different chemical salt fo rm of the medicinal

agent.alteration of the pH of a solution.or substitution in pan or in whole of the solvent a phar macist can in certain instances dissolve greater quantities of a solute than would otherwise be p ossible.For example.iodine granules are soluble in water only to the extent of I g in about3000 mL Using only these two agents,the maximum concentration possible would be approximately0. 03of iodine.However,through the use of an aqueous solution of potassium iodide or sodium io dide as the solvent_much larges amounts of iodine may be dissolved as the result of the formati on of a water-soluble complex with the iodide salt.This reaction is taken advantage of,for exam ple,in Iodine Topical Solution,USP,prepared to contain about2%iodine and2.4%sodium iodide.试剂在特定溶剂中的溶解度表示可以用该试剂和该溶剂制备溶液的最大浓度。当在给定温度下的溶剂已经溶解了其所有的溶质时，据说它是饱和的。为了强调两种化学试剂之间的溶解度的可能变化，因此，为了制备饱和溶液所需的量，可以使用两种官能的饱和水溶液作为实例，即氢氧化钙局部溶液。USP和钾。碘化物口服溶液，USP。第一个解决方案。通过用纯化水搅拌过量的氢氧化钙制备：在21℃下每100mL溶液仅含有约140mg溶解的溶质，而碘化钾溶液每100mL溶液含有约100g溶质，超过700次大量的溶质，如在氢氧化钙局部溶液中。因此，药剂师可以制备溶液的最大可能浓度变化很大，并且部分地取决于溶质的化学组成。通过选择不同的增溶剂或不同的化学盐形式的药物

代理。改变溶液的pH。或在锅中或在整个溶剂中的替代，药剂师在某些情况下可溶解比其它可能的更大量的溶质。例如。碘颗粒仅在约3000mL中溶于水的程度。仅使用这两种试剂，最大可能浓度为约0.03的碘。然而，通过使用碘化钾或碘化钠的水溶液作为溶剂，由于与碘化物盐形成水溶性络合物，可以溶解大量的碘。该反应利用例如制备成含有约2％碘和2.4％碘化钠的碘局部溶液USP。

Temperature is an important factor in determining the solubility of a drug and in preparing its sol ution_Most chemicals absorb heat when they are dissolved and are said to have a positive heat of solution,resulting in increased solubility with an increase in temperature.A few chemicals have

a negative heat of solution and exhibit a decrease in solubility with a rise in temperature.Other f actors in addition to temperature affect solubility.These include the various chemical and other physical properties of both the-solute and the solvent,pressure,the pH of the solution,the ate o f subdivision of the salute,and the physical agitation applied to the solution as it dissolves.The s olubility of a pure chemical substance at a given temperature and pressure is constant;however. its rate of solution,that is,the speed at which it dissolves,depends on the particle size of the su

b stance and the extent of agitation.The finer the powder,the greater the surface area that comes in contact with the solvent and the more rapid the dissolving process.Also,tile greater the agitat ion,the more unsaturated solvent passes over tile drug,and the faster the formation of the solut ion.温度是确定药物溶解度和制备其溶液的重要因素。大多数化学物质在溶解时吸收热量，并且据说具有溶液的正热，导致随温度升高溶解度增加。几种化学物质溶解的负热并且随着温度的升高表现出溶解度的降低。除了温度以外的其他因素影响溶解度。这些包括溶质和溶

剂的各种化学和其他物理性质，压力，溶液的pH，盐溶物的细分，以及当溶液溶解时施加到溶液的物理搅拌。纯化学物质在给定温度和压力下的溶解度是恒定的;但是。其溶解速率，即其溶解速度取决于物质的粒径和搅拌的程度。粉末越细，与溶剂接触的表面积越大，溶解过程越快。此外，搅拌越大，不饱和溶剂越过瓦片药物越多，溶液的形成越快。

The solubility of a substance in a given solvent may be determined by preparing a saturat ed solution of it at a specific temperature and determining by chemical analysis the amount of ch emical dissolved in a given weight of solution.The amount of solvent required to dissolve the am ount of salute can be deter mined by simple calculation.The solubility may then be expressed as grams of solute dissolving in milliliters of solvent for example,"lg of sodium chloride dissolves in 2.8mL of water."When the exact solubility has not been determined.general expressions of rela tive solubility may be used.These terms are defined in the USP and presented in Table13.1.物质在给定溶剂中的溶解度可以通过在特定温度下制备其饱和溶液并通过化学分析确定溶解在给定重量溶液中的化学物质的量来确定。溶解所需的溶剂量所需的溶剂量可以通过简单的计算来确定。然后可以将溶解度表示为溶解在毫升溶剂中的溶质克数，例如“1g氯化钠溶解在2.8mL水中。当确切的溶解度尚未确定。可以使用相对溶解度的一般表示。这些术语在USP中定义并在表13.1中给出。

A great many of the important organic medicinal agents are either weak acids or weak bases, and their solubility depends to a large measure on the pH of the solvent.These drugs react either with strong acids or strong bases to form water-soluble salts;For instance,the weak bases,inclu ding many of the alkaloids(atropine.codeine,and morphine),antihistamines(diphenhydramine and tripelennamine),local anesthetics(cocaine.procaine,and tetracaine),and other important dr ugs are not very water soluble.but they are soluble in dilute solutions of acids.Pharmaceutical m anufacturers have prepared many acid salts of these organic bases to enable the preparation of a queous solutions.However,if the pH of the aqueous solution of these salts is changed by the addi tion of alkali,the free base may separate from solution unless it has adequate solubilitv in water. Organic medicinals that are weak acids include the barbiturate drugs(e.g,phenobarbital)and the sulfonamides(e.g.,sulfadiazine and sulfacetamide.These and other

weak acids form water-soluble salts in basic solution and may separate from the pH.Table13.2 presents the comparative solubilities of some typical examples of weak acids and weak bases an d their salts.许多重要的有机药剂是弱酸或弱碱，它们的溶解度在很大程度上取决于溶剂的pH值。这些药物与强酸或强碱反应形成水溶性盐;例如，弱碱，包括许多生物碱（阿托品，可待因和吗啡），抗组胺剂（苯海拉明和苄吡二胺），局部麻醉剂（可卡因，普鲁卡因和丁卡因）和其他重要的药物不是很溶于水。但它们可溶于酸的稀溶液中。药物制造商已经制备了这些有机碱的许多酸盐，以能够制备水溶液。然而，如果通过加入碱改变这些盐的水溶液的pH，则游离碱可以与溶液分离，除非其具有足够的作为弱酸的有机药物包括巴比妥酸盐药物（例如苯巴比妥）和磺胺类药物（例如磺胺嘧啶和磺胺醋酰胺）。这些和其它弱酸在碱性溶液中形成水溶性盐，并且可以与pH分离。图13.2给出了弱酸和弱碱及其盐的一些典型实例的比较溶解度

Disperse Systems

This chapter includes the main types of liquid preparations containing undissolved or immiscible drugs distributed throughout a vehicle.In these preparations,the substance distributed is referred to as the dispersed phase,and the vehicle is termed the dispersing phase or dispersion medium.Together,alley produce a dispersed system.本章包括分布在整个介质中的含有不溶解

或不混溶药物的主要类型的液体制剂。在这些制剂中，所分配的物质被称为分散相，并且该载体被称为分散相或分散介质。分散系统。

The particles of the dispersed phase are usually solid materials that are insoluble in the disper sion medium.In the case of emulsions,the dispersed phase is a liquid that is neither soluble nor miscible with the liquid of the dispersing phase.Emulsification results in the dispersion of liquid drug as fine droplets throughout the dispersing phase.In the case of an aerosol,the dispersed p hase may be small air bubbles throughout a solution or an emulsion.Dispersions also consist of droplets of a liquid(solution or suspension)in air.分散相的颗粒通常是不溶于分散介质的固体材料。在乳液的情况下，分散相是既不溶解也不与分散相的液体混溶的液体。乳化导致液体药物作为细小液滴在整个分散相中的分散。在气溶胶的情况下，分散相可以是遍及溶液或乳液的小气泡。分散体也由液体（溶液或悬浮液）在空气中的液滴组成。

The particles of the dispersed phase vary widely in size,from large particles visible to the nake d eye down to particles of colloidal dimension,falling between I.O nm and0.5um.Dispersions co ntaining coarse particles,usually l0to50um,are referred to as coarse dispersions;they include t he suspensions and emulsions.Dispersions containing particles of smaller size are termed fine dis persions(0.5-10um),and if the particles are in the colloidal range,colloidal dispersions.Magmas and gels are fine dispersions.分散相的颗粒在尺寸上广泛变化，从肉眼可见的大颗粒到胶体尺寸的颗粒，落在1.0nm和0.5μm之间。含有粗颗粒，通常为10至50um的分散体被称为粗分散体;它们包括悬浮液和乳液。含有较小尺寸颗粒的分散体称为细分散体（0.5-10μm），并且如果颗粒在胶体范围内，则为胶体分散体。岩浆和凝胶都很好分散

Largely because of their greater size,particles in a coarse dispersion have a greater tende ncy to separate from the dispersion medium than do the particles of a fine dispersion.Most soli ds in dispersion tend to settle to the bottom of the container because of their greater density tha n the dispersion medium,whereas most emulsified liquids for oral use are oils.which generally h ave less density than the aqueous medium in which they are dispersed,so that they tend to rise t oward the top of the https://www.wendangku.net/doc/fb1423183.html,plete and uniform redistribution of the dispersed phase is essential to the accurate administration of uniform doses.For a properly prepared dispersion,thi s should be accomplished by moderate agitation of the container.主要由于它们的较大尺寸，粗分散体中的颗粒与细分散体的颗粒相比具有更大的从分散介质中分离的倾向。分散体中的大多数固体倾向于沉降到容器的底部，因为它们的密度大于分散介质的密度，而用于口服使用的大多数乳化液体是油。其通常具有比其中它们分散于其中的水性介质更低的密度，使得它们倾向于朝向制剂的顶部上升。分散相的完全和均匀的再分布对于准确施用均匀剂量是必要的。对于适当制备的分散体，这应当通过适度搅拌容器来实现。

The focus of this chapter is on dispersions of drugs administered orally or topically.The same b asic pharmaceutical characteristics apply to dispersion systems administered by other routes.Inc luded among these are ophthalmic and otic suspensions and stensions and sterile suspensions for injection,covered in Chapters17and15,respectively.本章的重点是口服或局部给药的药物分散体。相同的基本药物特性适用于通过其它途径施用的分散体系。其中包括眼用和耳用悬浮液和注射用的无菌悬浮液，分别在第17章和第15章中讨论。

Suspensions

Suspensions may be defined as preparations containing finely divided drug particles the s uspensoid)distributed somewhat uniformly throughout a vehicle in which the drug exhibits a mi nimum degree of solubility.Some suspensions are available in ready-to-use form,that is,already distributed through a liquid vehicle with or without stabilizers and other add available。Other

preparations are available as dry powders intended for suspension in liquid vehicles.this type

of product generally is a powder mixture containing the drug and suitable suspending and disper sing agents to be diluted and agitated with a specified quantity of vehicle,generally purified wate r.Figure14.2demonstrates preparation of this type of product.Drugs that are unstable if mainta ined for extended periods in the presence of an aqueous vehicle(for example,many antibiotic dr ugs)are most frequently supplied as dry powder mixtures for reconstitution at the time of dispensing.This type of preparation is designated in the USP by a title of the form"for Oral Suspe nsion.’Prepared suspensions not requiring reconstitution at the time of dispensing are simply designated as‘Oral Suspension.’悬浮液可以定义为含有微细药物颗粒悬浮液的制剂）在整个载体中稍微均匀地分布，其中药物显示出最小的溶解度。一些悬浮液可以以即用形式获得，即已经通过具有或不具有稳定剂和其他添加剂的液体载体分配。其它制剂可作为用于悬浮在液体载体中的干粉提供。这种类型的产品通常是含有药物和合适的悬浮剂和分散剂的粉末混合物，用特定量的载体（通常是纯化水）稀释和搅拌。图14.2显示了这种类型产品的制备。如果在水性载体（例如，许多抗生素药物）存在下长时间维持，则不稳定的药物最常作为用于在分配时重构的干粉混合物提供。这种类型的制剂在USP中被称为“用于口服悬浮液”的标题。在分配时不需要重构的制备悬浮液简称为“口服悬浮液”。

Reasons for Suspensions

There are several reasons for preparing suspensions.For one thing,certain drugs are chemically unstable in solution but stable when suspended.In instances such as this,the suspen sion ensures chemical stability while permitting liquid therapy.For many patients,the liquid form is preferred to the solid form of the same drug because of the ease of swallowing liquids and the flexibility in administration of a range of doses.This is particularly advantageous for infants,child ren,and the elderly.The disadvantage of a disagreeable taste of certain drugs in solution form is overcome when the drug is administered as undissolved particles of an oral suspension.In fact,c hemical forms of certain poor-tasting drugs have been specifically developed for their insolubility in a desired vehicle for the sole purpose of preparing a palatable liquid dosage form.For exampl e,chloramphenicol palmitate,the water insoluble ester farm of chloramphenicol,was developed to prepare a palatable liquid dosage form of chloramphenicol,the result being the development of chloramphenicol palmitate Oral Suspension,https://www.wendangku.net/doc/fb1423183.html,e of insoluble forms of drugs in suspensio ns greatly reduces the difficult taste-masking problems of developmental phannacists,and select ion of the flavorants to be used in a given suspension may be based on taste preference rather th an on a particular flavorant's ability to mask an unpleasant taste.For the most part,oral suspensi ons are aqueous preparations with the vehicle flavored and sweetened to suit the anticipated tas te preferences of the intended patient.制备悬浮液有几个原因。一方面，某些药物在溶液中是化学不稳定的，但是当悬浮时是稳定的。在这种情况下，悬浮液确保化学稳定性，同时允许液体治疗。对于许多患者，液体形式优于相同药物的固体形式，因为容易吞咽液体和施用一定剂量范围的灵活性。这对婴儿，儿童和老年人特别有利。当药物作为口服悬浮液的未溶解颗粒给药时，克服了溶液形式的某些药物的令人不快的味道的缺点。事实上，某些不良药物的化学形式已经被特别开发，因为它们在所需载体中的不溶性仅用于制备可口的液体剂型。例如，开发氯霉素棕榈酸酯（氯霉素的水不溶性酯农场）以制备适口的氯霉素的液体剂型，结果是氯霉素棕榈酸酯口服悬浮液（USP）的发展。在悬浮液中使用不溶性形式的药物大大减少了发展性药剂师困难的掩味问题，并且在给定的悬浮液中使用的调味剂的选择可以基于口味偏好，而不是基于特定调味剂掩盖不愉快味道的能力。大多数情况下，口服悬浮液是水性制剂，赋形剂和甜味剂以适合预期患者的预期味道偏好。

Features Desired in a Pharmaceutical Suspension

There are many considerations in the development and preparation of a pharmaceutically elegant suspension.In addition to therapeutic efficacy,chemical stability of Ihe components of t he formulation.permanency of the preparation,and esthetic appeal of the preparation-desirable qualities in all pharmaceutical preparations

a few other features apply more specifically to the pharmaceutical suspension:在开发和制备药学上优雅的悬浮液中有许多考虑。除了治疗功效，制剂的组分的化学稳定性。制剂的持久性和制剂的美学吸引力-所有药物制剂中期望的性质，一些其它特征更具体地应用于药物悬浮液：

1.A properly prepared pharmaceutical suspension should settle slowly and should be readily redispersed upon gentle shaking of the contai ner.适当制备的药物悬浮液应缓慢沉降，并且在容器轻轻摇动时应易于分散。

2.The particle size of the suspensoid should remain fairly constant throughout long periods of undisturbed standing.悬浮体的粒度在长期不受干扰的站立时应保持相当恒定

3.The suspension should pour readily and evenly from its container. These main features of a suspension,which depend on the nature of the dispersed phase,the dispersion medium,and pharmaceutical adjunc ts,will be discussed briefly3.悬浮液应容易且均匀地从其容器中倒出。将暂时讨论悬浮液的这些主要特征（其取决于分散相，分散介质和药物添加剂的性质）Emulsions

An emulsion is a dispersion in which the dispersed phase is composed of small globules of a liquid distributed throughout a vehicle in which it is immiscible.In emulsion terminology.the d ispersed phase is the internal phase.and the dispersion medium is the external or continuous ph ase.Emulsions with an oleaginous internal phase and an aqueous external phase are oil-in-water (o/w)emulsions.Conversely.emulsions having an aqueous internal phase and an oleaginous ext ernal phase are termed water-in-oil(w/o)emulsions.Because the external phase of an emulsion i s continuous,an ow emulsion may be diluted or extended with water or an aqueous preparation and a w/o emulsion,with an oleaginous or oilmiscible liquid.Generally,to prepare a stable emulsion,a third phase,an emulsifying agent,is necessary.Depending on their constituents,the viscosity of emulsions can vary greatly,and pharmaceutical emulsions may be prepared as liquids or semisolids.Based on the constituents and the intended application,liquid emulsions may be employed orally,topically,or parenterally;semisolid emulsions.topically.Many pharmaceutical preparations that are actually emulsions are not classified as such because they fit some other ph armaceutical category more appropriately.For instance,emulsions include certain lotions.linime nts.creams.ointments,and commercial vitamin drops that are discussed in this book under thes e various designations.乳液是一种分散体，其中分散相由分布在整个载体中的液体的小球组成，其中它是不混溶的。乳液术语。分散相是内相。并且分散介质是外部或连续相。含油内相和含水外相的乳液是水包油（o/w）乳液。相反。具有含水内相和含油外相的乳液称为油包水（w/o）乳液。由于乳液的外相是连续的，因此乳液可用水或含水制剂稀释或延长，和w/o乳液，与油性或油混溶性液体。通常，为了制备稳定的乳液，需要第三相，乳化剂。根据它们的成分，乳液的粘度可以变化很大，并且药物乳液可以制备为液体或半固体。基于组分和预期应用，液体乳剂可以口服，局部或胃肠外使用;半固体乳液。实际上是乳剂的许