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药代动力学二室模型药代动力学单室模型计算题导读：就爱阅读网友为您分享以下“药代动力学单室模型计算题”的资讯，希望对您有所帮助，感谢您对的支持!1. 计算题：一个病人用一种新药，以2mg/h的速度滴注，6小时即终止滴注，问终止后2小时体内血药浓度是多少？（已知k=0.01h－1，V＝10L）2. 计算题：已知某单室模型药物，单次口服剂量0.25g，F=1，K=0.07h－1，AUC=700μg/ml·h，求表观分布容积、清除率、生物半衰期（假定以一级过程消除）。
3. 某药静注剂量0.5g，4小时测得血药浓度为4.532μg/ml，12小时测得血药浓度为2.266μg/ml，求表观分布容积Vd为多少？4. 某人静注某药，静注2h、6h血药浓度分别为1.2μg/ml和0.3μg/ml（一级动力学），求该药消除速度常数？如果该药最小有效剂量为0.2μg/ml，问第二次静注时间最好不迟于第一次给药后几小时？5. 病人静注复方银花注射剂2m/ml后，立即测定血药浓度为1.2μg/ml，3h为0.3μg/ml，该药在体内呈单室一级速度模型，试求t1/2。
6. 某病人一次用四环素100mg，血药初浓度为10μg/ml，4h 后为7.5μg/ml，试求t1/2。
7. 静脉快速注射某药100mg，其血药浓度－时间曲线方程为：C=7.14e-0.173t，其中浓度C的单位是mg/L，时间t的单位是h。
请计算：（1）分布容积；（2）消除半衰期；（3）AUC。
8. 计算题：某药物具有单室模型特征，体内药物按一级速度过程清除。
其生物半衰期为2h，表观分布容积为20L。
现以静脉注射给药，每4小时一次，每次剂量为500mg。
求：该药的蓄积因子第2次静脉注射后第3小时时的血药浓度稳态最大血药浓度稳态最小血药浓度9. 给病人一次快速静注四环素100mg，立即测得血清药物浓度为10μg/ml，4小时后血清浓度为7.5μg/ml。
第一章一、单项选择题1．以下关于生物药剂学的描述，正确的是A．剂型因素是指片剂、胶囊剂、丸剂和溶液剂等药物的不同剂型B．药物产品所产生的疗效主要与药物本身的化学结构有关C．药物效应包括药物的疗效、副作用和毒性D．改善难溶性药物的溶出速率主要是药剂学的研究内容2．以下关于生物药剂学的描述，错误的是A．生物药剂学与药理学和生物化学有密切关系，但研究重点不同B．药物动力学为生物药剂学提供了理论基础和研究手段C．由于生物体液中药物浓度通常为微量或痕量，需要选择灵敏度高，专属性强、重现性好的分析手段和方法D．从药物生物利用度的高低就可判断药物制剂在体内是否有效二、多项选择题1．药物及剂型的体内过程是指A.吸收 B．渗透 C．分布 D．代谢 E．排泄2．药物转运是指A．吸收 B．渗透 C．分布 D．代谢 E．排泄3．药物处置是指A．吸收 B.渗透 C．分布 D．代谢 E．排泄4．药物消除是指A．吸收 B.渗透 C．分布 D.代谢 E．排泄三、名词解释1. 生物药剂学2. 剂型因素；3．生物因素；4．药物及剂型的体内过程四、问答题1.生物药剂学的研究工作主要涉及哪些内容？2.简述生物药剂学研究对于新药开发的作用。
第二章一、单项选择题1．对生物膜结构的性质描述错误的是A．流动性 B．不对称性C．饱和性 D．半透性E．不稳定性2．K+、单糖、氨基酸等生命必需物质通过生物膜的转运方式是A.被动扩散B.膜孔转运C．主动转运 D.促进扩散E．膜动转运3．红霉素的生物有效性可因下述哪种因素而明显增加A. 缓释片 B．肠溶衣C．薄膜包衣片 D．使用红霉素硬脂酸盐E．增加颗粒大小4．下列哪项不属于药物外排转运器A. P-糖蛋白 B．多药耐药相关蛋白C.乳腺癌耐药蛋白D.有机离子转运器E．ABC转运蛋白5．以下哪条不是主动转运的特点A．逆浓度梯度转运 B．无结构特异性和部位特异性C．消耗能量 D.需要载体参与E．饱和现象6．胞饮作用的特点是A.有部位特异性B.需要载体C. 不需要消耗机体能量D.逆浓度梯度转运E．以上都是7．下列哪种药物不是P-gp的底物A.环孢素A B．甲氨蝶呤C.地高辛D.诺氟沙星E.维拉帕米8．药物的主要吸收部位是A.胃B.小肠C.大肠D.直肠 E．均是9．关于影响胃空速率的生理因素不正确的是A.胃内容物的黏度和渗透压 B．精神因素C．食物的组成 D.药物的理化性质E．身体姿势10.在溶出力限速过程吸收中，溶解了的药物立即被吸收，即为( )状态A.漏槽 B．动态平衡C.饱和D.均是E.均不足11. 淋巴系统对（）的吸收起着重要作用A. 脂溶性药物B.解离型药物C. 水溶性药物D.小分子药物E. 未解离型药物12．有关派伊尔结(PP)描述错误的是A．回肠含量最多B．≤10μm的微粒可被PP内的巨噬细胞吞噬C．由绒毛上皮和M细胞（微褶细胞）构成D．与微粒吸收相关E．与药物的淋巴转运有关13．药物理化性质对于药物在胃肠道的吸收影响显着，下列叙述中错误的是A.药物的溶出快一般有利于吸收B.具有均质多晶型的药物，一般其亚稳定型有利于吸收C.药物具有一定脂溶性，但不可过大，有利于吸收D.酸性药物在胃酸条件下一定有利于吸收；碱性药物在小肠碱性的条件下一定有利于药物的吸收E．胆汁分泌常会影响难溶性药物的口服吸收14.影响片剂中药物吸收的剂型和制剂工艺因素不包括A．片重差异 B.片剂的崩解度C．药物颗粒的大小 D．药物的溶出与释放E．压片的压力15．下列叙述错误的是A．细胞膜可以主动变形而将某些物质摄入细胞内或从细胞内释放到细胞外，称为胞饮B．大多数药物通过被动扩散方式透过生物膜C.被动扩散需要载体参与D.主动转运是借助载体或酶促系统从低浓度区域向高浓度区域转运的过程E.促进扩散一般比单纯扩散的速度快得多16．pH分配假说可用下面哪个方程描述A．Fick's方程 B. Noyes-Whitney方程C．Henderson-Hasselbalch方程 D. Stokes方程E．Michaelis-Menten方程17．漏槽条件下，药物的溶出速度方程为A. dC/dt=kSCs B. dC/dt=kCsC. dC/dt=k/SCs D. dC/dt=kS/CsE．dC/dt=k/S/Cs18．一般认为在口服剂型中药物吸收的大致顺序为A. 水溶液>混悬液>散剂>胶囊剂>片剂B. 水溶液>混悬液>胶囊剂> 散剂>片剂C. 水溶液>散剂>混悬液>胶囊剂>片剂D. 混悬液>水溶液>散剂>胶囊剂>片剂E. 水溶液>混悬液>片剂>散剂>胶囊剂19.关于药物间及药物与辅料间的相互作用描述错误的是A. 药物引起胃肠道pH的改变会明显妨碍药物的吸收B．药物在制剂中与辅料发生相互作用形成络合物可使药物在吸收部位的浓度减小C．华法林与氢氧化镁同时服用可提高华法林的血药浓度D．脂质类材料为载体制备固体分散体，可不同程度地延缓药物释放E．药物被包合后，使药物的吸收增大20.根据药物生物药剂学分类系统以下哪项为Ⅱ型药物A．高的溶解度，低的通透性 B. 低的溶解度，高的通透性C．高的溶解度，高的通透性 D. 低的溶解度，低的通透性E．以上都不是21.下列关于药物转运的描述正确的是A．浓度梯度是主动转运的动力B．易化扩散的速度一般比主动转运的快C．P-gp是药物内流转运器D．肽转运器只能转运多肽E．核苷转运器是外排转运器22.对低溶解度，高通透性的药物，提高其吸收的方法错误的是A. 制成可溶性盐类 B．制成无定型药物C. 加入适量表面活性剂D. 增加细胞膜的流动性E. 增加药物在胃肠道的滞留时间23.弱碱性药物的溶出速率大小与pH大小的关系是A.随pH增加而增加B.随pH减少而不变C.与pH无关D.随pH增加而降低E.随pH减少而减少24.根据Henderson-Hasselbalch方程式求出，酸性药物的pKa-pH=A. lg(Ci ×Cu) B. lg (Cu/Ci)C. Ig (Ci -Cu) D. lg( Ci+Cu)E. Ig (Ci /Cu)25.在溶剂化物中，药物的溶解度和溶解速度顺序为A.水合物<有机溶剂化物<无水物B.无水物<水合物<有机溶剂化物C.水合物<无水物<有机溶剂化物D.有机溶剂化物<无水物<水合物E.有机溶剂化物<水合物<无水物26.哪种方法可提高地高辛的药物吸收A.增大DnB.减小DoC.增大DoD.减小DnE.减小An 所需要的时间27．下列有关溶出度参数的描述错误的A．溶出参数td表示药物从制剂中累积溶出%所需要的时间B．Ritger-Peppas方程中释放参数n与制剂骨架等形状有关C. Higuchi方程描述的是累积溶出药量与时间的平方根成正比D．单指数模型中k越小表明药物从制剂中溶出的速度越快E．相似因子与变异因子可以定量地评价参比制剂与试验制剂溶出曲线之间的差别28．关于肠道灌流法描述正确的是A．小肠有效渗透系数（P）是决定药物在小肠吸收速度和程度的一个重要参eff数B．对受试动物的数量没有要求C．吸收研究过程中药物必须以溶液状态存在D. 与体内情况相关性较差E．能排除药物肠道代谢、肠壁吸附等因素所致的药物损失29．研究药物的吸收时，生理状态更接近自然给药情形的研究方法是A.小肠单向灌流法B.肠襻法C.外翻环法D.小肠循环灌流法模型30.寡肽转运体PEPT1的底物包括A.嘧啶类 B．心律失常药 C.头孢菌素类D.抗组胺药物 E．维生素类31．多肽类药物以( )作为口服的吸收部位A.结肠 B．盲肠 C.十二指肠D.直肠 E．空肠32.多晶型中以( )有利于制剂的制备，因为其溶解度、稳定性较适宜A.稳定型 B．不稳定型C.亚稳定型、B、C均是E．A、B、C均不是33.血流量可显着影响药物在( )的吸收速度A．直肠 B．结肠 c．小肠 D．胃 E．以上都是34．下列有关药物在胃肠道的吸收描述错误的是A．胃肠道分为三个主要部分：胃、小肠和大肠，而小肠是药物吸收的最主要部位B．胃肠道内的pH从胃到大肠逐渐上升，通常是：胃pH1～3（空腹偏低，约为～，进食后pH上升到3），十二指肠pH5～6，空肠pH6～7，大肠pH7～8C. pH影响被动扩散药物的吸收D.胃是弱碱性药物吸收的最佳环境E.主动转运很少受pH的影响35.下列可影响药物溶出速率的是A．粒子大小 B．溶剂化物C．多晶型 D. 溶解度E．均是36.下列各种因素中除( )外，均能加快胃的排空A.胃内容物渗透压降低 B．胃大部分切除C.胃内容物黏度降低D. 普萘洛尔E．吗啡37.关于胃肠道吸收的叙述错误的是A. 当食物中含有较多脂肪，有时对溶解度特别小的药物能增加吸收量B．一些通过主动转运吸收的物质，饱腹服用吸收量增加C．一般情况下，弱碱性药物在胃中容易吸收D. 当胃空速率增加时，多数药物吸收加快E．脂溶性，非离子型药物容易透过细胞膜38.膜孔转运有利于( )药物的吸收A. 脂溶性大分子B.水溶性小分子C．水溶性大分子 D.带正电荷的蛋白质E．带负电荷的药物39．影响被动扩散的主要因素是A. 药物的溶解度 B．药物的脂溶性C．药物的溶出速率 D. 药物的晶型E．药物的粒子大小40.各类食物中，( )胃排空最快A. 碳水化合物 B．蛋白质C. 脂肪D. 三者混合物E．均一样41.弱碱性药物奎宁的pK= ，在小肠中(pH=解离型和未解离型的比为aA．1 B. 25/1 C. 1/25 D. 14/1 E．无法计算42.某有机酸类药物在小肠中吸收良好，主要因为A.该药在肠道中的非解离型比例大B.药物的脂溶性增加C.小肠的有效面积大D.肠蠕动快E．该药在胃中不稳定43.以下关于氯霉素的叙述错误的是A. 棕榈氯霉素无效晶型经水浴加热(87～89℃)熔融处理后可转变为有效晶型 B．棕榈氯霉素混悬剂中，氯霉素为B晶型，故有治疗作用C．无定型为有效晶型D. 棕榈氯霉素有A、B、C三种晶型及无定型，其中A晶型是有效晶型 E．棕榈氯霉素有效晶型的血液浓度比其无效晶型的血液浓度高44.药物的溶出速率可用下列( )表示A. Higuchi方程B. Henderson-Hasselbalch方程C. Fick定律D. Noyes-Whitney方程E. Stokes方程45.细胞旁路通道的转运屏障是A.紧密连接B.绒毛C.刷状缘膜D.微绒毛E.基底膜46.消化液中的( )能增加难溶性药物的溶解度，从而影响药物的吸收A.黏蛋白 B．酶类C.胆酸盐 D．糖E．维生素47.胃肠道中影响高脂溶性药物透膜吸收的屏障是A.溶媒牵引效应B.不流动水层C．微绒毛 D.紧密连接E．刷状缘膜二、多项选择题1．生物药剂学分类系统中参数吸收数An与( )项有关A．药物的有效渗透率 B．药物溶解度C. 肠道半径 D．药物在肠道内滞留时间E．药物的溶出时问2．BCS中用来描述药物吸收特征的三个参数是A.吸收数 B．剂量数 C．分布数 D.溶解度 E．溶出数3．以下哪种药物不适于用微粉化的方法增加药物吸收A. 在消化道的吸收受溶出速度支配的药物B．弱碱性药物C．胃液中不稳定的药物D. 难溶于水的药物E．对胃肠道有刺激性的药物4．下列有关生物药剂学分类系统相关内容的描述正确的是A.生物药剂学分类系统根据溶解性与通透性的差异将药物分成四大类B. I型药物具有高通透性和高渗透性C．III型药物透过是吸收的限速过程，与溶出速率没有相关性D. 剂量数是描述水溶性药物的口服吸收参数，一般剂量数越大，越有利于药物的吸收E．溶出数是描述难溶性药物吸收的重要参数，受剂型因素的影响，并与吸收分数F密切相关5．以下可提高Ⅲ类药物吸收的方法有A.加入透膜吸收促进剂B.制成前体药物C．制成可溶性盐类 D.制成微粒给药系统E．增加药物在胃肠道的滞留时间6．Caco-2细胞限制药物吸收的因素有A．不流动水层 B．细胞间各种连接处C.细胞形态D.细胞膜E.单层完整性7.影响药物胃肠道吸收的剂型因素有A.药物在胃肠道中的稳定性B.粒子大小C.多晶型D.解离常数E.胃排空速率8．口服固体制剂申请生物学试验豁免需满足以下哪些条件 A.为速释型口服固体制剂B．主药具有低渗透性C．制剂中的主药必须在pH 1～范围内具有高溶解性D. 辅料的种类与用量符合FDA的规定E．主药具有较宽的治疗窗9．体外研究口服药物吸收作用的方法有A.组织流动室法 B．外翻肠囊法C．外翻环法 D.肠道灌流法E．肠襻法10.下列一般不利于药物吸收的因素有A. 不流动水层B. P-gp药泵作用C．胃排空速率增加 D.加适量的表面活性剂E．溶媒牵引效应11.影响药物吸收的剂型因素有A.药物油水分配系数 B．药物粒度大小C.药物晶型D. 药物溶出度E.药物制剂的处方组成12.被动扩散具以下哪些特征A. 不消耗能量B.有结构和部位专属性C．有饱和状态 D.借助载体进行转运E．由高浓度向低浓度转运13.影响胃排空速度的因素有A. 药物的多晶型B.食物的组成C．胃内容物的体积 D.胃内容物的黏度E．药物的脂溶性14. Caco-2细胞模型主要应用于A. 研究药物结构与吸收转运的关系 B．快速评价前体药物的口服吸收 C．研究口服药物的吸收转运机制 D.确定药物在肠腔吸收的最适pH E．研究辅料以及剂型对吸收的影响作用15.协同转运发生时需要的重要条件有A.浓度梯度B.结构特异性C.部位特异性D.载体亲和力的构象差E．能量16.影响药物吸收的理化因素有A.解离度 B．脂溶性 C.溶出速度 D.稳定性 E.晶型17.改善跨细胞膜途径吸收机制有A.改变黏液的流变学性质 B．提高膜的流动性C.膜成分的溶解作用D. 溶解拖动能力的增加E.与膜蛋白的相互作用三、名词解释1．细胞通道转运；2．被动转运；3．溶出速率；4．载体媒介转运；5．促进扩散；6．ATP驱动泵；7．多药耐药；8．生物药剂学分类系统；9．药物外排转运器；10.多晶型四、问答题1．简述促进扩散的特点，并与被动转运比较两者的异同。
血药浓度随时间变化的规律及药动学参数（The regularity and pharmacokinetic parameters of serum concentration with time）The regularity and pharmacokinetic parameters of serum concentration with time(I) drug time curveAfter administration of drug concentration in vivo by transfer or transformation that is changing with time, effect also changes along with concentration, such as curve representation, the former is called curve relationship (Time-concentration Relationship Curve), the latter for the aging curve(Time-response Relationship Curve).Taking the non intravenous administration for example, the dose duration relationship and the time dependence of the drug pass through the following three stages: incubation period, duration, and residual period.Incubation period: the time after which medication starts to function, reflecting the absorption and distribution of drugs;Duration: the time at which an effective concentration of the drug is maintained;Residual period: the concentration of the drug has been reduced to below the minimum effective concentration, but has not yet been completely eliminated from the body.(three) elimination kinetics of drugs: the dynamic process ofcontinuous attenuation of serum concentration.Elimination of drugs: the process of biotransformation and excretion of drugs that results in the disappearance of pharmacological activity. There are two kinds of the kinetics of the elimination of drugs:1, first-order elimination kinetics: the elimination of drugs at a constant rate per unit time.That is, the rate of elimination of drugs in the blood is directly proportional to the concentration of drugs in the blood, the blood concentration of the body is high, the amount of drugs is eliminated in unit time, and the elimination rate decreases with the decrease of serum concentration. After the decrease in serum concentration, the elimination of the drug is still eliminated at a rate. Therefore, it is also called the constant ratio elimination of drugs. Most drugs are eliminated this way.Such as the elimination of 1/2 per hour.2. Zero elimination kinetics: the elimination of a constant amount of drugs per unit time. That is, regardless of the level of plasma drug concentration, the amount of drugs removed per unit time. It is also known as the quantity of drug elimination. Often too much, more than the maximum elimination capacity caused by the body.Such as the elimination of 100mg/h per hour.(three) elimination kinetics of drugs: the dynamic process of continuous attenuation of serum concentration.Elimination of drugs: the process of biotransformation and excretion of drugs that results in the disappearance of pharmacological activity. There are two kinds of the kinetics of the elimination of drugs:1, first-order elimination kinetics: the elimination of drugs at a constant rate per unit time.That is, the rate of elimination of drugs in the blood is directly proportional to the concentration of drugs in the blood, the blood concentration of the body is high, the amount of drugs is eliminated in unit time, and the elimination rate decreases with the decrease of serum concentration. After the decrease in serum concentration, the elimination of the drug is still eliminated at a rate. Therefore, it is also called the constant ratio elimination of drugs. Most drugs are eliminated this way.Such as the elimination of 1/2 per hour.2. Zero elimination kinetics: the elimination of a constant amount of drugs per unit time. That is, regardless of the level of plasma drug concentration, the amount of drugs removed per unit time. It is also known as the quantity of drug elimination. Often too much, more than the maximum elimination capacity caused by the body.Such as the elimination of 100mg/h per hour.Four 、 pharmacokinetic parameters of commonly used drugs(a) bioavailability (Bioavailability):.The speed and extent of absorption of drugs into the body circulation.Notation: F= (A/D) * 100% (oral: <100%; vein: 100%)Divided into: absolute bioavailability: F= (PO equal amount of drugs, AUC/iv equal amount of drugs AUC) * 100%The relative bioavailability of F= (equivalent to the reagent AUC/ with standard drug AUC * 100%)(two) apparent volume of distributionThe volume of fluid required for the distribution of plasma drug levels in vivo after the distribution of plasma and tissue is balanced. Vd=A/C0, theoretical capacity)Significance:1, the distribution volume of a given drug is measured to produce the desired dosage of the drug concentration: D = C, Vd2. Predict the distribution of drugs:Vd small drugs are mainly distributed in organs with large bloodflow;Vd large, low blood concentration and wide distribution of drugs;(three) half-life: generally refers to the half-life of plasma (T1/2), that is, the time required for the plasma concentration to fall by half. Since most drugs are eliminated in afirst-order kinetic manner, their half-life is a constant, T1/2=0.693/ke.Significance: reflects the rate of drug elimination. T1/2 long to eliminate slow and maintain long time(1) drug classification according to: short effect, medium effect, long effect;(2) determine the interval between dosing(3) the steady-state concentration time was predicted: 4-5 t1/2;(4) predict the basic elimination time of drugs: 4-5 t1/2 after the last dose(four) the steady blood concentration (CSS/ / Ping Ping concentration value): continuous constant drug dosages, gradually accumulated, through 5 half-life, blood concentration reached a stable level. The serum concentration at this time is called steady-state serum concentration, CSS. At this point the amount of drugs removed and the amount of drugsentering the body is equal, drugs are no longer accumulated in the body.Significance: (1) the plateau concentration is directly proportional to the total quantity of the day.(2) the fluctuation range of plateau concentration, high limit and low limit is proportional to each dose.(five) clearance rate:The rate of clearance of the drug is how many liters of blood can be removed per unit time. Each drug has its own fixed CL.CL=ke/Vd.Four 、 the change of serum concentration and the regimen of administrationIn clinical, most drugs need to be repeatedly given in order to achieve the desired level of serum concentration. Therefore, the time curve of the administration is zigzag.(1) continuous constant dose, total dose increases, CSS increases; administration of the same amount, change the number of drug CSS invariant. A total of conventional drugs in children, the same day the total number of drug, the more each use less, smaller fluctuations in safety range of small, multiple service, Ping concentration maintained at the minimum effective dose and minimum dose.(2) dose volume maintenance method: doubling the first dose, then rapidly reaching CSS in a half life, and then using maintenance dose. This method is suitable for emergency treatment, and requires rapid treatment.(3) intermittent administration: according to the needs of clinical treatment, the medication regimen with interval of more than half time can be used to reduce the incidence of adverse reactions. Such as glucocorticoids.(4) the regimen should be individualized, such as liver and kidney dysfunction, the half-life is longer than normal, and the time to CSS is longer. Therefore, the dosage should be reduced and the interval between doses should be extended.。
