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Pharmacokineticsnoun explanation

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Pharmacokinetics

Simulation

仿真

仿真(英语:simulation)或译作模拟,泛指基于实验或训练为目的,将原本的真实或抽象的选定系统或流程,建立一个模型以表征其关键特性(key characteristics)或者行为、功能,予以系统化与公式化,以便进行可对关键特征做出仿真。模型表示系统自身,而仿真表示系统的时序行为。 电脑仿真常被用来研究仿真模型(simulation model)。仿真也被用于对自然系统或人造系统的科学建模以获取深入理解。仿真可以用来展示可选条件或动作过程的最终结果。仿真也会用在因为无法接近、也可能太过于危险或不可接受的后果、或者设计了但还未建造、或者根本就不存在等原因而不能在真实的系统中达成的。仿真的关键是获取相关选定的关键特性与行为的有效信息源,仿真时使用简化的近似或者假定,仿真结果的保真度(fidelity)与有效性。模型验证(verification)与有效性(validation)的过程、协议是学术学习、改进、研究、开发仿真技术的热点,特别是对计算机仿真。 仿真保真度(Simulation Fidelity)用于描述仿真精度,模拟真实对应物有多近似: 低保真:对系统的最小模拟,接受输入产生输出 中等保真:对刺激能自动响应,有限精度 高保真:接近不可辨识或者尽可能地接近真实系统

A simulation is an imitative representation of a process or system that could exist in the real world. In this broad sense, simulation can often be used interchangeably with model. Sometimes a clear distinction between the two terms is made, in which simulations require the use of models; the model represents the key characteristics or behaviors of the selected system or process, whereas the simulation represents the evolution of the model over time. Another way to distinguish between the terms is to define simulation as experimentation with the help of a model. This definition includes time-independent simulations. Often, computers are used to execute the simulation. Simulation is used in many contexts, such as simulation of technology for performance tuning or optimizing, safety engineering, testing, training, education, and video games.

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Pharmacokinetics

Residence time

停留时间

流体包裹的停留时间是流体包裹在控制体积(例如:化学反应器、湖泊、人体)内花费的总时间。一组宗地的停留时间根据该组中停留时间的频率分布(称为停留时间分布 (RTD))或以其平均值(称为平均停留时间)来量化。停留时间在化学尤其是环境科学和药理学中起着重要作用。交货时间或等待时间分别在供应链管理和排队理论中发挥着核心作用,其中流动的材料通常是离散的而不是连续的。

The residence time of a fluid parcel is the total time that the parcel has spent inside a control volume (e.g.: a chemical reactor, a lake, a human body). The residence time of a set of parcels is quantified in terms of the frequency distribution of the residence time in the set, which is known as residence time distribution (RTD), or in terms of its average, known as mean residence time. Residence time plays an important role in chemistry and especially in environmental science and pharmacology. Under the name lead time or waiting time it plays a central role respectively in supply chain management and queueing theory, where the material that flows is usually discrete instead of continuous.

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Pharmacokinetics

Steady state

穩態 (系統)

在系统理论中,如果定义系统或过程行为的变量(称为状态变量)不随时间变化,则系统或过程处于稳定状态。在连续时间内,这意味着对于系统的这些属性 p,相对于时间的偏导数为零并且保持不变:对于所有当前和未来 t ,∂ p ∂ t = 0。

In systems theory, a system or a process is in a steady state if the variables (called state variables) which define the behavior of the system or the process are unchanging in time. In continuous time, this means that for those properties p of the system, the partial derivative with respect to time is zero and remains so: ∂ p ∂ t = 0 for all present and future t .

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Pharmacokinetics

Cmin

最小血药浓度

Cmin 是药代动力学中使用的一个术语,表示药物在给药间隔期间达到的最低血浆浓度,即两次给药之间的时间间隔。该定义与 Ctrough(下一次给药前的浓度)略有不同。 Cmin 与 Cmax 相反,即药物达到的最大浓度。 Cmin 必须高于某些阈值,例如最低抑菌浓度 (MIC),才能达到治疗效果。在大多数情况下,Cmin 是可以直接测量的。

Cmin is a term used in pharmacokinetics for the minimum blood plasma concentration reached by a drug during a dosing interval, which is the time interval between administration of two doses. This definition is slightly different from Ctrough, the concentration immediately prior to administration of the next dose. Cmin is the opposite of Cmax, the maximum concentration that the drug reaches. Cmin must be above certain thresholds, such as the minimum inhibitory concentration (MIC), to achieve a therapeutic effect. In most cases Cmin is directly measurable.

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Pharmacokinetics

Drug accumulation ratio

药物蓄积率

在药代动力学中,药物蓄积率(Rac)是指药物在稳态条件下(即重复给药后)与单剂量相比蓄积的比率。该值越高,药物在体内蓄积越多。 Rac 为 1 意味着没有累积。

In pharmacokinetics, the drug accumulation ratio (Rac) is the ratio of accumulation of a drug under steady state conditions (i.e., after repeated administration) as compared to a single dose. The higher the value, the more the drug accumulates in the body. An Rac of 1 means no accumulation.

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Pharmacokinetics

Absorption rate constant

吸收速率常数

吸收速率常数Ka是药代动力学中用于描述药物进入系统的速率的值。它以时间−1为单位表示。 Ka 与吸收半衰期 (t1/2a) 相关,计算公式如下:Ka = ln(2) / t1/2a。 Ka 值通常只能在研究文章中找到。这与生物利用度和消除半衰期等参数形成鲜明对比,这些参数通常可以在药物和药理学手册中找到。

The absorption rate constant Ka is a value used in pharmacokinetics to describe the rate at which a drug enters into the system. It is expressed in units of time−1. The Ka is related to the absorption half-life (t1/2a) per the following equation: Ka = ln(2) / t1/2a. Ka values can typically only be found in research articles. This is in contrast to parameters like bioavailability and elimination half-life, which can often be found in drug and pharmacology handbooks.

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Pharmacokinetics

Metabolite

代謝產物

在生物化学中,代谢物是新陈代谢的中间产物或最终产物。该术语通常用于小分子。代谢物具有多种功能,包括燃料、结构、信号传导、对酶的刺激和抑制作用、自身的催化活性(通常作为酶的辅因子)、防御以及与其他生物体的相互作用(例如色素、气味剂和信息素)。初级代谢物直接参与正常的“生长”、发育和繁殖。乙烯是工业微生物大规模生产的初级代谢物的例子。次级代谢产物不直接参与这些过程,但通常具有重要的生态功能。例子包括抗生素和颜料,例如树脂和萜烯等。

In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc.

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Pharmacokinetics

Cytochrome P450

细胞色素P450

细胞色素 P450(P450 或 CYP)是一个酶超家族,含有血红素作为辅助因子,主要但不限于单加氧酶。然而,它们并不是无所不在的;例如,在大肠杆菌中尚未发现它们。在哺乳动物中,这些酶氧化类固醇、脂肪酸、外源物质,并参与许多生物合成。通过羟基化,CYP450 酶将异生素转化为亲水性衍生物,更容易排出体外。一般来说,P450 是电子传递链中的末端氧化酶,大致分为含 P450 的系统。术语“P450”源自当酶处于还原状态并与一氧化碳络合时在酶的最大吸收波长(450nm)处的分光光度峰。

Cytochromes P450 (P450s or CYPs) are a superfamily of enzymes containing heme as a cofactor that mostly, but not exclusively, function as monooxygenases. However, they are not omnipresent; for example, they have not been found in Escherichia coli. In mammals, these enzymes oxidize steroids, fatty acids, xenobiotics, and participate in many biosyntheses. By hydroxylation, CYP450 enzymes convert xenobiotics into hydrophilic derivatives, which are more readily excreted. P450s are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometric peak at the wavelength of the absorption maximum of the enzyme (450 nm) when it is in the reduced state and complexed with carbon monoxide.

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Pharmacokinetics

Pharmacogenomics

药物基因组学

药物基因组学,通常缩写为“PGx”,是研究基因组在药物反应中的作用的学科。它的名字(pharmaco-+基因组学)反映了它的药理学和基因组学的结合。药物基因组学分析患者的基因组成如何影响他们对药物的反应。它通过将 DNA 突变(包括点突变、拷贝数变异和结构变异)与药代动力学(药物吸收、分布、代谢和消除)、药效学(通过药物生物靶点介导的效应)和免疫原性终点相关联,研究获得性和遗传性遗传变异对药物反应的影响。药物基因组学旨在根据患者的基因型开发合理的方法来优化药物治疗,以实现最大的效率和最小的副作用。

Pharmacogenomics, often abbreviated "PGx", is the study of the role of the genome in drug response. Its name (pharmaco- + genomics) reflects its combining of pharmacology and genomics. Pharmacogenomics analyzes how the genetic makeup of a patient affects their response to drugs. It deals with the influence of acquired and inherited genetic variation on drug response, by correlating DNA mutations (including point mutations, copy number variations, and structural variations) with pharmacokinetic (drug absorption, distribution, metabolism, and elimination), pharmacodynamic (effects mediated through a drug's biological targets), and immunogenic endpoints. Pharmacogenomics aims to develop rational means to optimize drug therapy, with regard to the patients' genotype, to achieve maximum efficiency with minimal adverse effects.

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Pharmacokinetics

Prodrug

前体药物

前药是一种药理学上无活性的药物或化合物,在摄入后,其代谢(即在体内转化)为药理学活性药物。可以使用相应的前药来改善药物的吸收、分布、代谢和排泄(ADME),而不是直接给药。当药物本身从胃肠道吸收不良时,前药通常旨在提高生物利用度。前药可用于改善药物与非其预期靶标的细胞或过程相互作用的选择性。这可以减少药物的不良或意外影响,这在化疗等治疗中尤其重要,因为化疗可能会产生严重的意外和不良副作用。

A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.

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Pharmacokinetics

Drug interaction

药物相互作用

在制药科学中,当药物的作用机制受到同时服用的食物、饮料或其他药物等物质的影响时,就会发生药物相互作用。药物与食物相互作用的一个流行例子是葡萄柚对药物代谢的影响。相互作用可以通过直接或间接同时靶向受体而发生。例如,唑吡坦和酒精都会影响 GABAA 受体,同时服用它们会导致受体过度刺激,从而导致意识丧失。当两种药物相互影响时,称为药物相互作用(DDI)。 DDI 的风险随着所用药物数量的增加而增加。很大一部分老年人经常使用五种或更多药物或补充剂,药物间相互作用产生副作用的风险很大。

In pharmaceutical sciences, drug interactions occur when a drug's mechanism of action is affected by the concomitant administration of substances such as foods, beverages, or other drugs. A popular example of drug–food interaction is the effect of grapefruit on the metabolism of drugs. Interactions may occur by simultaneous targeting of receptors, directly or indirectly. For example, both Zolpidem and alcohol affect GABAA receptors, and their simultaneous consumption results in the overstimulation of the receptor, which can lead to loss of consciousness. When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions.

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Pharmacokinetics

Enzyme inhibitor

酶抑制剂

酶抑制剂是一种与酶结合并阻断其活性的分子。酶是加速生命必需的化学反应的蛋白质,其中底物分子转化为产物。酶通过将底物与其活性位点结合来促进特定的化学反应,活性位点是酶上的一个特殊区域,可加速反应中最困难的步骤。酶抑制剂通过与酶的活性位点结合(从而防止底物本身结合)或通过与酶上的另一个位点结合来阻止(“抑制”)该过程,从而阻止酶对反应的催化。酶抑制剂可以可逆或不可逆地结合。不可逆抑制剂与酶形成化学键,从而抑制酶直至化学键断裂。

An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken.

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Pharmacokinetics

Plasma protein binding

血浆蛋白结合

血浆蛋白结合是指药物与血浆中的血液蛋白结合的程度。药物的功效可能会受到其结合程度的影响。药物的结合越少,它穿过或扩散穿过细胞膜的效率就越高。药物结合的常见血液蛋白有人血清白蛋白、脂蛋白、糖蛋白以及 α、β、γ 球蛋白。

Plasma protein binding refers to the degree to which medications attach to blood proteins within the blood plasma. A drug's efficacy may be affected by the degree to which it binds. The less bound a drug is, the more efficiently it can traverse or diffuse through cell membranes. Common blood proteins that drugs bind to are human serum albumin, lipoprotein, glycoprotein, and α, β‚ and γ globulins.

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Pharmacokinetics

Active metabolite

活性代謝產物

活性代谢物或药理活性代谢物是外源物质(例如药物或环境化学品)的生物活性代谢物。活性代谢物可能产生治疗作用,也可能产生有害作用。

An active metabolite, or pharmacologically active metabolite, is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects.

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Pharmacokinetics

Enzyme inducer

酵素誘導物

酶诱导剂是一类通过与酶结合并激活它,或通过增加酶编码基因的表达来增加酶的代谢活性的药物。酶诱导剂的例子之一是细胞色素 P450 酶,它将有助于药物在生物体内更快地代谢。酶诱导剂在制药领域对于了解药物相互作用非常重要。研究表明某些药物会增加诱导剂的活性,例如抗生素。它与酶抑制剂相反。有一些特定类型的酶诱导剂可以产生细胞保护途径,在预防和治疗癌症和其他疾病(包括心血管疾病和神经退行性疾病)中发挥作用。酶诱导剂可以是天然存在的或合成的。

An enzyme inducer is a type of drug that increases the metabolic activity of an enzyme, either by binding to the enzyme and activating it, or by increasing the expression of the gene coding for the enzyme. One of the examples of enzyme inducers can be Cytochrome P450 enzymes, which will help to metabolize the drugs faster in the organism. Enzyme inducers are important in the pharmaceutical field to learn drug interactions. Studies show that certain drugs will increase the activity of the inducer, examples could be antibiotics. It is the opposite of an enzyme repressor. There are specific types of enzyme inducers that create cytoprotective pathways that play a role in prevention and treatment of cancer and other diseases including cardiovascular disease and neurodegenerative diseases. Enzyme inducers can be either naturally occurring or synthetically made.

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Pharmacokinetics

Accuracy and precision

测量精度

准确度和精密度是观测误差的衡量标准;准确度是指给定的一组测量值与真实值的接近程度,精度是指测量值彼此之间的接近程度。国际标准化组织(ISO)定义了一个相关的衡量标准:真实度,“大量测试结果的算术平均值与真实或可接受的参考值之间的一致程度”。虽然精度是对随机误差的描述(统计变异性的度量),但精度有两种不同的定义:更常见的是对系统误差的描述(给定集中趋势度量的统计偏差的度量,例如平均值)。在“准确性”的定义中,该概念独立于“精度”,因此一组特定的数据可以说是准确的、精确的、两者都是准确的、或者两者都不是。这个概念符合ISO的真实性。

Accuracy and precision are measures of observational error; accuracy is how close a given set of measurements is to the true value and precision is how close the measurements are to each other. The International Organization for Standardization (ISO) defines a related measure: trueness, "the closeness of agreement between the arithmetic mean of a large number of test results and the true or accepted reference value." While precision is a description of random errors (a measure of statistical variability), accuracy has two different definitions: More commonly, a description of systematic errors (a measure of statistical bias of a given measure of central tendency, such as the mean). In this definition of "accuracy", the concept is independent of "precision", so a particular set of data can be said to be accurate, precise, both, or neither. This concept corresponds to ISO's trueness.

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Pharmacokinetics

Reproducibility

复现性

再现性与可重复性和可重复性密切相关,是支撑科学方法的主要原则。研究结果的可重复性意味着,当研究被重复时,通过实验或观察性研究或数据集统计分析获得的结果应该再次获得高度的可靠性。复制有不同类型,但复制研究通常涉及使用相同方法的不同研究人员。只有在一次或多次成功复制之后,结果才能被视为科学知识。

Reproducibility, closely related to replicability and repeatability, is a major principle underpinning the scientific method. For the findings of a study to be reproducible means that results obtained by an experiment or an observational study or in a statistical analysis of a data set should be achieved again with a high degree of reliability when the study is replicated. There are different kinds of replication but typically replication studies involve different researchers using the same methodology. Only after one or several such successful replications should a result be recognized as scientific knowledge.

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Pharmacokinetics

Binding potential

结合潜力

在药代动力学和受体-配体动力学中,结合电位 (BP) 是“可用”神经受体密度和药物与该神经受体亲和力的综合衡量标准。

In pharmacokinetics and receptor–ligand kinetics the binding potential (BP) is a combined measure of the density of "available" neuroreceptors and the affinity of a drug to that neuroreceptor.

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Pharmacokinetics

Absorption (pharmacology)

吸收(药理学)

吸收是药物从给药部位到作用部位的旅程。药物通过某种给药途径(口服、局部皮肤等)以选定的剂型(例如片剂、胶囊或溶液)传播。其他一些途径的吸收,例如静脉治疗、肌内注射、肠内营养,甚至更直接,吸收的变异性较小,生物利用度通常接近 100%。血管内给药不涉及吸收,无药物损失。最快的吸收途径是吸入。吸收是药物开发和药物化学的主要关注点,因为药物必须被吸收才能产生任何药效。此外,通过调整影响吸收的因素,可以轻松且显着地改变药物的药代动力学特征。

Absorption is the journey of a drug travelling from the site of administration to the site of action. The drug travels by some route of administration (oral, topical-dermal, etc.) in a chosen dosage form (e.g., tablets, capsules, or in solution). Absorption by some other routes, such as intravenous therapy, intramuscular injection, enteral nutrition, is even more straightforward and there is less variability in absorption and bioavailability is often near 100%. Intravascular administration does not involve absorption, and there is no loss of drug. The fastest route of absorption is inhalation. Absorption is a primary focus in drug development and medicinal chemistry, since a drug must be absorbed before any medicinal effects can occur. Moreover, the drug's pharmacokinetic profile can be easily and significantly changed by adjusting factors that affect absorption.

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Pharmacokinetics

Area under the curve (pharmacokinetics)

曲线下面积 (药物代谢动力学)

在药代动力学领域,曲线下面积 (AUC) 是血浆中药物浓度随时间变化的定积分(这可以使用液相色谱-质谱法完成)。在实践中,在某些离散的时间点测量药物浓度,并使用梯形规则来估计 AUC。在药理学中,药物血浆浓度与给药后时间关系图下的面积(称为“曲线下面积”或 AUC)可以深入了解药物的暴露程度及其从体内的清除率。

In the field of pharmacokinetics, the area under the curve (AUC) is the definite integral of the concentration of a drug in blood plasma as a function of time (this can be done using liquid chromatography–mass spectrometry). In practice, the drug concentration is measured at certain discrete points in time and the trapezoidal rule is used to estimate AUC. In pharmacology, the area under the plot of plasma concentration of a drug versus time after dosage (called "area under the curve" or AUC) gives insight into the extent of exposure to a drug and its clearance rate from the body.

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Pharmacokinetics

Bioanalysis

生物分析

生物分析是分析化学的一个子学科,涵盖生物系统中外源物质(药物及其代谢物、非自然位置或浓度的生物分子)和生物物质(大分子、蛋白质、DNA、大分子药物、代谢物)的定量测量。

Bioanalysis is a sub-discipline of analytical chemistry covering the quantitative measurement of xenobiotics (drugs and their metabolites, and biological molecules in unnatural locations or concentrations) and biotics (macromolecules, proteins, DNA, large molecule drugs, metabolites) in biological systems.

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Pharmacokinetics

Physiologically based pharmacokinetic modelling

生理药代动力学建模

基于生理学的药代动力学 (PBPK) 建模是一种数学建模技术,用于预测人类和其他动物物种中合成或天然化学物质的吸收、分布、代谢和排泄 (ADME)。 PBPK 建模用于药物研究和药物开发,以及化妆品或一般化学品的健康风险评估。 PBPK 模型力求通过数学方式转录复杂 ADME 过程中所涉及现象的解剖学、生理学、物理和化学描述来实现机械化。这些模型中仍然存在很大程度的残余简化和经验主义,但与经典的、基于经验函数的药代动力学模型相比,它们具有扩展的适用范围。

Physiologically based pharmacokinetic (PBPK) modeling is a mathematical modeling technique for predicting the absorption, distribution, metabolism and excretion (ADME) of synthetic or natural chemical substances in humans and other animal species. PBPK modeling is used in pharmaceutical research and drug development, and in health risk assessment for cosmetics or general chemicals. PBPK models strive to be mechanistic by mathematically transcribing anatomical, physiological, physical, and chemical descriptions of the phenomena involved in the complex ADME processes. A large degree of residual simplification and empiricism is still present in those models, but they have an extended domain of applicability compared to that of classical, empirical function based, pharmacokinetic models.

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Pharmacokinetics

Polymersome

聚合物囊泡

在生物技术中,聚合物囊泡是一类人造囊泡,是包围溶液的微小空心球体。聚合物囊泡是使用两亲性合成嵌段共聚物形成囊泡膜制成的,半径范围为 50 nm 至 5 μm 或更大。大多数报道的聚合物囊泡在其核心中含有水溶液,可用于封装和保护敏感分子,例如药物、酶、其他蛋白质和肽以及 DNA 和 RNA 片段。聚合物囊泡膜提供了物理屏障,将封装材料与外部材料(例如生物系统中发现的材料)隔离开来。合成体是被设计为含有通道(跨膜蛋白)的聚合物囊泡,这些通道允许某些化学物质穿过膜,进入或离开囊泡。这允许收集或酶促修饰这些物质。

In biotechnology, polymersomes are a class of artificial vesicles, tiny hollow spheres that enclose a solution. Polymersomes are made using amphiphilic synthetic block copolymers to form the vesicle membrane, and have radii ranging from 50 nm to 5 μm or more. Most reported polymersomes contain an aqueous solution in their core and are useful for encapsulating and protecting sensitive molecules, such as drugs, enzymes, other proteins and peptides, and DNA and RNA fragments. The polymersome membrane provides a physical barrier that isolates the encapsulated material from external materials, such as those found in biological systems. Synthosomes are polymersomes engineered to contain channels (transmembrane proteins) that allow certain chemicals to pass through the membrane, into or out of the vesicle. This allows for the collection or enzymatic modification of these substances.

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Pharmacokinetics

Patlak plot

帕特拉克图

Patlak 图(有时称为 Gjedde–Patlak 图、Patlak–Rutland 图或 Patlak 分析)是一种基于房室模型的图形分析技术,它使用线性回归来识别和分析涉及不可逆摄取的示踪剂的药代动力学,例如脱氧葡萄糖的情况。它用于注射不透射线或放射性示踪剂后评估核医学成像数据。该方法是模型无关的,因为它不依赖于示踪剂的任何特定隔室模型配置,并且最小的假设是示踪剂的行为可以通过两个隔室来近似——一个与血浆快速平衡的“中央”(或可逆)隔室,以及一个“外围”(或不可逆)隔室,其中示踪剂在测量期间进入而不离开。

A Patlak plot (sometimes called Gjedde–Patlak plot, Patlak–Rutland plot, or Patlak analysis) is a graphical analysis technique based on the compartment model that uses linear regression to identify and analyze pharmacokinetics of tracers involving irreversible uptake, such as in the case of deoxyglucose. It is used for the evaluation of nuclear medicine imaging data after the injection of a radioopaque or radioactive tracer. The method is model-independent because it does not depend on any specific compartmental model configuration for the tracer, and the minimal assumption is that the behavior of the tracer can be approximated by two compartments – a "central" (or reversible) compartment that is in rapid equilibrium with plasma, and a "peripheral" (or irreversible) compartment, where tracer enters without ever leaving during the time of the measurements.

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Pharmacokinetics

Pharmacometrics

药理学

药物计量学是疾病和药理学测量模型的方法论和应用的研究领域。它使用生物学、药理学、疾病和生理学的数学模型来描述和量化异生素与患者(人类和非人类)之间的相互作用,包括有益影响和不利影响。它通常用于量化药物、疾病和试验信息,以帮助有效的药物开发、监管决策和患者的合理药物治疗。药理学使用基于药理学、生理学和疾病的模型来定量分析药物与患者之间的相互作用。这涉及系统药理学、药代动力学、药效学和疾病进展,重点关注群体和变异性。

Pharmacometrics is a field of study of the methodology and application of models for disease and pharmacological measurement. It uses mathematical models of biology, pharmacology, disease, and physiology to describe and quantify interactions between xenobiotics and patients (human and non-human), including beneficial effects and adverse effects. It is typically used to quantify drug, disease, and trial information to aid efficient drug development, regulatory decisions, and rational drug treatment in patients. Pharmacometrics uses models based on pharmacology, physiology, and disease for quantitative analysis of interactions between drugs and patients. This involves Systems pharmacology, pharmacokinetics, pharmacodynamics and disease progression with a focus on populations and variability.

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Pharmacokinetics

PEGylation

聚乙二醇化

聚乙二醇化(或聚乙二醇化)是聚乙二醇(PEG,在药学中称为聚乙二醇)聚合物链与分子和宏观结构(例如药物、治疗性蛋白质或囊泡)共价和非共价连接或合并的过程,然后将其描述为聚乙二醇化。聚乙二醇化会影响所得衍生物或聚集体的相互作用,这通常会减慢它们的聚结和降解以及体内消除。聚乙二醇化通常通过将 PEG 的反应性衍生物与靶分子一起孵育来实现。 PEG 与药物或治疗蛋白的共价连接可以“掩盖”宿主免疫系统的药剂(降低免疫原性和抗原性),并增加其流体动力学尺寸(溶液中的尺寸),从而通过减少肾脏清除率来延长其循环时间。

PEGylation (or pegylation) is the process of both covalent and non-covalent attachment or amalgamation of polyethylene glycol (PEG, in pharmacy called macrogol) polymer chains to molecules and macrostructures, such as a drug, therapeutic protein or vesicle, which is then described as PEGylated. PEGylation affects the resulting derivatives or aggregates interactions, which typically slows down their coalescence and degradation as well as elimination in vivo. PEGylation is routinely achieved by the incubation of a reactive derivative of PEG with the target molecule. The covalent attachment of PEG to a drug or therapeutic protein can "mask" the agent from the host's immune system (reducing immunogenicity and antigenicity), and increase its hydrodynamic size (size in solution), which prolongs its circulatory time by reducing renal clearance.

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Pharmacokinetics

Pegol

佩戈尔

Pegol 是药物通用名称中使用的一个术语,表示存在聚乙二醇连接(聚乙二醇化)。该术语用于单克隆抗体和工程蛋白以及小分子。聚乙二醇化的目的是延长药物的半衰期。示例包括: Alacizumab 聚乙二醇 Calaspargase 聚乙二醇 Certolizumab 聚乙二醇 依替立康聚乙二醇 Lulizumab 聚乙二醇

Pegol is a term used in generic names for pharmaceutical drugs to indicate the presence of a polyethylene glycol attachment (pegylation). The term is used for monoclonal antibodies and engineered proteins as well as for small molecules. The purpose of the pegylation is to extend the half-life of the drug. Examples include: Alacizumab pegol Calaspargase pegol Certolizumab pegol Etirinotecan pegol Lulizumab pegol

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Pharmacokinetics

Plateau principle

高原原理

平台原理是最初为解释药物作用时间过程(药代动力学)而开发的数学模型或科学定律。该原理在药理学、生理学、营养学、生物化学和系统动力学方面具有广泛的适用性。它适用于以相对恒定的速率输注或摄入药物或营养素以及在每个时间间隔内消除恒定分数的情况。在这些条件下,输注速率的任何变化都会导致指数增加或减少,直到达到新的水平。这种行为也称为稳定状态的方法,因为当输注或生产速率与损失速率平衡时,不会导致无限增加或减少,而是实现自然平衡。

The plateau principle is a mathematical model or scientific law originally developed to explain the time course of drug action (pharmacokinetics). The principle has wide applicability in pharmacology, physiology, nutrition, biochemistry, and system dynamics. It applies whenever a drug or nutrient is infused or ingested at a relatively constant rate and when a constant fraction is eliminated during each time interval. Under these conditions, any change in the rate of infusion leads to an exponential increase or decrease until a new level is achieved. This behavior is also called an approach to steady state because rather than causing an indefinite increase or decrease, a natural balance is achieved when the rate of infusion or production is balanced by the rate of loss.

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Pharmacokinetics

PKPD model

PKPD模型

PKPD建模(药代动力学药效建模)(也可缩写为PK/PD或PK-PD建模)是一种结合了药代动力学和药效学两个经典药理学学科的技术。它将药代动力学和药效学模型组件集成到一组数学表达式中,从而可以描述响应药物剂量施用的效应强度的时间过程。 PKPD 建模与药理学领域相关。 PKPD 模型的核心是浓度效应或暴露反应关系。存在多种 PKPD 建模方法来描述暴露-反应关系。 PKPD关系可以通过简单的方程来描述,例如线性模型、Emax模型或Sigmoid Emax模型。

PKPD modeling (pharmacokinetic pharmacodynamic modeling) (alternatively abbreviated as PK/PD or PK-PD modeling) is a technique that combines the two classical pharmacologic disciplines of pharmacokinetics and pharmacodynamics. It integrates a pharmacokinetic and a pharmacodynamic model component into one set of mathematical expressions that allows the description of the time course of effect intensity in response to administration of a drug dose. PKPD modeling is related to the field of pharmacometrics. Central to PKPD models is the concentration-effect or exposure-response relationship. A variety of PKPD modeling approaches exist to describe exposure-response relationships. PKPD relationships can be described by simple equations such as linear model, Emax model or sigmoid Emax model.

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Pharmacokinetics

Physical pharmacy

物理药学

物理药学是药学的一个分支,专注于物理和化学在药学研究中的应用。换句话说,它是通过解决分子水平的问题来研究剂型对其环境的影响。它强调药物输送系统在给予患者之前的物理特征和作用。它构成了药品设计、制造和分销的基础,也是稳定和正确使用医疗药品的基础。它涵盖了溶解度、药代动力学和药物输送等领域。物理药学是指导药物开发的原则。它还可以作为了解药物治疗过程中发生的药物吸收、分布、代谢和消除的基础。

Physical pharmacy is the branch of pharmacy that concentrates on the applications of physics and chemistry to the study of pharmacy. In other words, it is the study of the effects that dosage forms have on their environment by addressing issues at the molecular level. It emphasis on the physical characteristics and actions of the drug delivery system before the same is given to the patient. It forms the basis for design, manufacture, and distribution of drug products and serves as the foundation for the stable and proper use of medical drugs. It covers areas such as solubility, pharmacokinetics and drug delivery. Physical pharmacy serves as principles that guide the pharmaceutical developments. It also serves as a basis for the understanding of drug absorptions, distributions, metabolism, and eliminations that happen during the course of drug treatment.

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