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Pharmacokinetics

Osmotic-controlled release oral delivery system

渗透控释口服给药系统

渗透控释口服给药系统(OROS)是一种先进的控释口服给药系统,其形式为刚性片剂,具有半透性外膜和一个或多个小激光钻孔。当片剂通过体内时,水通过渗透作用通过半透膜被吸收,产生的渗透压用于推动活性药物通过片剂中的激光钻孔并进入胃肠道。 OROS 是 ALZA Corporation 拥有的商标名称,该公司率先使用渗透泵进行口服药物输送。与其他控释机制相比,渗透释放系统具有许多主要优点。它们受 pH 值、食物摄入量、胃肠蠕动和不同肠道环境等因素的影响明显较小。

The osmotic-controlled release oral delivery system (OROS) is an advanced controlled release oral drug delivery system in the form of a rigid tablet with a semi-permeable outer membrane and one or more small laser drilled holes in it. As the tablet passes through the body, water is absorbed through the semipermeable membrane via osmosis, and the resulting osmotic pressure is used to push the active drug through the laser drilled opening(s) in the tablet and into the gastrointestinal tract. OROS is a trademarked name owned by ALZA Corporation, which pioneered the use of osmotic pumps for oral drug delivery. Osmotic release systems have a number of major advantages over other controlled-release mechanisms. They are significantly less affected by factors such as pH, food intake, GI motility, and differing intestinal environments.

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Pharmacokinetics

Parallel artificial membrane permeability assay

平行人工膜通透性测定

在药物化学中,平行人工膜渗透性测定 (PAMPA) 是一种测定物质从供体室通过注入脂质的人工膜进入受体室的渗透性的方法。供体使用多孔微量滴定板,顶部放置膜/受体室;整个组件通常被称为“三明治”。测试开始时,供体室中添加药物,受体室中无药物。经过可能包括搅拌的孵育期后,将夹层分离并测量每个隔室中的药物量。质量平衡允许计算保留在膜中的药物。

In medicinal chemistry, parallel artificial membrane permeability assay (PAMPA) is a method which determines the permeability of substances from a donor compartment, through a lipid-infused artificial membrane into an acceptor compartment. A multi-well microtitre plate is used for the donor and a membrane/acceptor compartment is placed on top; the whole assembly is commonly referred to as a “sandwich”. At the beginning of the test, the drug is added to the donor compartment, and the acceptor compartment is drug-free. After an incubation period which may include stirring, the sandwich is separated and the amount of drug is measured in each compartment. Mass balance allows calculation of drug that remains in the membrane.

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Pharmacokinetics

Polypharmacy

复方用药

多药治疗(polypragmasia)是一个总称,描述患者针对其病情同时使用多种药物。复方用药一词通常被定义为定期服用五种或更多药物,但没有标准定义,并且当一个人同时服用两种或多种药物时也使用该术语。多重用药可能是患有多种长期病症的结果,也称为多重病态。这两种情况在老年人中更为常见。多重用药可能会增加老年人群和/或患有许多慢性合并症的人发生不良事件的风险。在许多情况下,多重用药是不可避免的,但鼓励“适当的多重用药”做法以降低不良反应的风险。

Polypharmacy (polypragmasia) is an umbrella term to describe the simultaneous use of multiple medicines by a patient for their conditions. The term polypharmacy is often defined as regularly taking five or more medicines, but there is no standard definition, and the term has also been used when a person is prescribed 2 or more medications at the same time. Polypharmacy may be the consequence of having multiple long-term conditions, also known as multimorbidity. Both are more common in the elderly. Polypharmacy may increase the risk of an adverse event in elderly populations and/or those with many chronic comorbidities. In many cases, polypharmacy cannot be avoided, but 'appropriate polypharmacy' practices are encouraged to decrease the risk of adverse effects.

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Pharmacokinetics

PottersWheel

陶艺轮

PottersWheel 是一个 MATLAB 工具箱,用于对瞬态动态系统进行数学建模,可以表示为化学反应网络或常微分方程 (ODE)。它允许通过将模型拟合到实验测量来自动校准模型参数。 CPU 密集型函数是用 C 编写的,或者在模型相关函数的情况下动态生成。建模可以使用图形用户界面交互地完成,也可以使用 PottersWheel 函数库基于 MATLAB 脚本来完成。该软件旨在支持数学建模者的工作,因为真正的陶轮可以简化陶器的建模。 PottersWheel 的基本用途涵盖了从模型创建到新实验预测的七个阶段。

PottersWheel is a MATLAB toolbox for mathematical modeling of time-dependent dynamical systems that can be expressed as chemical reaction networks or ordinary differential equations (ODEs). It allows the automatic calibration of model parameters by fitting the model to experimental measurements. CPU-intensive functions are written or – in case of model dependent functions – dynamically generated in C. Modeling can be done interactively using graphical user interfaces or based on MATLAB scripts using the PottersWheel function library. The software is intended to support the work of a mathematical modeler as a real potter's wheel eases the modeling of pottery. The basic use of PottersWheel covers seven phases from model creation to the prediction of new experiments.

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Pharmacokinetics

Rate of infusion

输注速度

在药代动力学中,输注速率(或给药速率)不仅指施用药物的速率,还指为达到已被证明具有治疗效果的固定剂量的稳态而应施用药物的所需速率。它可以计算为血浆中的稳态浓度乘以清除率: K i n = C s s ⋅ C L {\displaystyle \textstyle K_{in}=C_{ss}\cdot CL}

In pharmacokinetics, the rate of infusion (or dosing rate) refers not just to the rate at which a drug is administered, but the desired rate at which a drug should be administered to achieve a steady state of a fixed dose which has been demonstrated to be therapeutically effective. It can be calculated as the steady-state concentration in the plasma multiplied by the clearance: K i n = C s s ⋅ C L {\displaystyle \textstyle K_{in}=C_{ss}\cdot CL}

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Pharmacokinetics

Modified-release dosage

缓释剂量

缓释剂量是一种(与立即释放剂量相比)在给药后延迟(延迟释放剂量)或长时间(缓释[ER、XR、XL]剂量)或体内特定靶点(靶向释放剂量)递送药物的机制。缓释剂型是设计为以预定速率释放(释放)药物的剂型,以便在特定时间段内维持恒定的药物浓度,同时将副作用降至最低。这可以通过多种制剂来实现,包括脂质体和药物-聚合物缀合物(例如水凝胶)。持续释放的定义更类似于“控制释放”而不是“持续”。缓释剂量由缓释(SR)剂量或控释(CR)剂量组成。

Modified-release dosage is a mechanism that (in contrast to immediate-release dosage) delivers a drug with a delay after its administration (delayed-release dosage) or for a prolonged period of time (extended-release [ER, XR, XL] dosage) or to a specific target in the body (targeted-release dosage). Sustained-release dosage forms are dosage forms designed to release (liberate) a drug at a predetermined rate in order to maintain a constant drug concentration for a specific period of time with minimum side effects. This can be achieved through a variety of formulations, including liposomes and drug-polymer conjugates (an example being hydrogels). Sustained release's definition is more akin to a "controlled release" rather than "sustained". Extended-release dosage consists of either sustained-release (SR) or controlled-release (CR) dosage.

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Pharmacokinetics

Target-mediated drug disposition

靶点介导的药物处置

靶点介导的药物处置(TMDD)是药物以其高亲和力与其药理学靶点(例如受体)结合到影响其药代动力学特征的程度的过程。各种药物类别都可能表现出 TMDD,最常见的是大化合物(生物制剂,例如抗体、细胞因子或生长因子),但较小的化合物也可能表现出 TMDD(例如华法林和 CHK-336)。抗体的典型 TMDD 模式显示出非线性清除率,并且可以在通常定义为“中到低”的浓度范围内看到。在此浓度范围内,目标部分饱和。这篇与药理学相关的文章是一个小作品。您可以通过添加缺失的信息来帮助维基百科。

Target-mediated drug disposition (TMDD) is the process in which a drug binds with high affinity to its pharmacological target (for example, a receptor) to such an extent that affects its pharmacokinetic characteristics. Various drug classes can exhibit TMDD, most often these are large compounds (biologics such as antibodies, cytokines or growth factors) but also smaller compounds can exhibit TMDD (such as warfarin and CHK-336). A typical TMDD pattern of antibodies displays non-linear clearance and can be seen at concentration ranges that are usually defined as 'mid-to-low'. In this concentration range, the target is partly saturated. This pharmacology-related article is a stub. You can help Wikipedia by adding missing information.

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Pharmacokinetics

Targeted drug delivery

靶向药物输送

靶向药物输送,有时称为智能药物输送,是一种向患者输送药物的方法,其方式是增加身体某些部位相对于其他部位的药物浓度。这种递送方式主要建立在纳米医学的基础上,纳米医学计划采用纳米颗粒介导的药物递送来克服传统药物递送的缺陷。这些纳米粒子将装载药物并靶向身体仅存在患病组织的特定部位,从而避免与健康组织相互作用。靶向药物递送系统的目标是延长、定位、靶向并与病变组织产生受保护的药物相互作用。传统的药物递送系统是药物穿过生物膜的吸收,而靶向释放系统以剂型释放药物。

Targeted drug delivery, sometimes called smart drug delivery, is a method of delivering medication to a patient in a manner that increases the concentration of the medication in some parts of the body relative to others. This means of delivery is largely founded on nanomedicine, which plans to employ nanoparticle-mediated drug delivery in order to combat the downfalls of conventional drug delivery. These nanoparticles would be loaded with drugs and targeted to specific parts of the body where there is solely diseased tissue, thereby avoiding interaction with healthy tissue. The goal of a targeted drug delivery system is to prolong, localize, target and have a protected drug interaction with the diseased tissue. The conventional drug delivery system is the absorption of the drug across a biological membrane, whereas the targeted release system releases the drug in a dosage form.

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Pharmacokinetics

Therapeutic drug monitoring

治疗药物监测

治疗药物监测(TDM)是临床化学和临床药理学的一个分支,专门用于测量血液中的药物水平。其主要关注点是治疗范围较窄的药物,即很容易剂量不足或过量的药物。 TDM 旨在通过单独调整药物剂量来改善患者护理,临床经验或临床试验表明它可以改善一般或特殊人群的治疗结果。它可以基于先验的药物遗传学、人口统计和临床信息,和/或基于药物血液浓度的事后测量(药代动力学监测)或生物替代或效应终点标记(药效监测)。

Therapeutic drug monitoring (TDM) is a branch of clinical chemistry and clinical pharmacology that specializes in the measurement of medication levels in blood. Its main focus is on drugs with a narrow therapeutic range, i.e. drugs that can easily be under- or overdosed. TDM aimed at improving patient care by individually adjusting the dose of drugs for which clinical experience or clinical trials have shown it improved outcome in the general or special populations. It can be based on an a priori pharmacogenetic, demographic and clinical information, and/or on the a posteriori measurement of blood concentrations of drugs (pharmacokinetic monitoring) or biological surrogate or end-point markers of effect (pharmacodynamic monitoring).

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Pharmacokinetics

Dissociation constant

解离常数

在化学、生物化学及药理学中,解离常数(英语:dissociation constant, K d {\displaystyle K_{d}} )是一种特定类型的平衡常数,用于衡量一较大物体与另一较小组分分开(解离)的倾向,也可以描述配合物解体成组分分子或盐分裂为其组分离子。解离常数是缔合常数的倒数。对于一些特定的盐,解离常数亦可被称为电离常数。

In chemistry, biochemistry, and pharmacology, a dissociation constant (KD) is a specific type of equilibrium constant that measures the propensity of a larger object to separate (dissociate) reversibly into smaller components, as when a complex falls apart into its component molecules, or when a salt splits up into its component ions. The dissociation constant is the inverse of the association constant. In the special case of salts, the dissociation constant can also be called an ionization constant.

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Pharmacokinetics

Michaelis–Menten kinetics

米-门二氏动力学

米-门二氏动力学(英语:Michaelis-Menten kinetics),又称米氏动力学,以德国生物化学家莱昂诺尔·米夏埃利斯和加拿大医师莫德·门滕的名字命名,是酶动力学中一个极为重要的方程,可以描述多种非变异构酶动力学现象,其表示式为: V 0 = V m a x [ S ] K M + [ S ] {\displaystyle V_{0}=V_{max}{\frac {[S]}{K_{M}+[S]}}}

In biochemistry, Michaelis–Menten kinetics, named after Leonor Michaelis and Maud Menten, is the simplest case of enzyme kinetics, applied to enzyme-catalysed reactions involving the transformation of one substrate into one product. In 1913, Michaelis and Menten expanded on Victor Henri's fundamental equation of enzyme kinetics, which was established in 1902. It takes the form of a differential equation describing the reaction rate v {\displaystyle v} (rate of formation of product P, with concentration p {\displaystyle p} ) as a function of a {\displaystyle a} , the concentration of the substrate A (using the symbols recommended by the IUBMB).

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Pharmacokinetics

Enzyme

酶

酶(英语:enzyme,/ˈɛnzaɪm/),又称酵素,是一类大分子生物催化剂。酶能加快化学反应的速度(即具有催化作用)。由酶催化的反应中,反应物称为底物,生成的物质称为产物。几乎所有细胞内的代谢过程都离不开酶。酶能大大加快这些过程中各化学反应进行的速率,使代谢产生的物质和能量能满足生物体的需求。细胞中酶的类型对可在该细胞中发生的代谢途径的类型起决定作用。对酶进行研究的学科称为酶学(enzymology)。 目前已知酶可以催化超过5000种生化反应。大部分酶是蛋白质,有少部分酶是具有催化活性的核糖核酸(RNA)分子,这些酶被称为核酶。酶的特异性是由其独特的三级结构决定的。 和所有的催化剂一样,酶通过降低反应激活能来加快化学反应速率。一些酶可以将底物转化为产物的速率提高数百万倍。一个比较极端的例子是乳清苷-5'-磷酸脱羧酶。该酶可以使在无催化剂条件下需要进行数百万年的化学反应在几毫秒内完成。从化学原理上讲,酶和其它所有催化剂一样,反应不会使其物质量发生变化。酶亦不能改变化学平衡,这一点和其它催化剂也是一样的。酶和其它催化剂的不同之处在于,它们的专一性要强得多。一些分子可以影响酶的活性。如酶抑制剂能降低酶的活性,酶激活剂能提高酶的活性。许多药物及毒物是酶的抑制剂。当超出或小于适宜的温度和pH值后,酶的活性会显著下降。 酶在工业和人们的日常生活中的应用也非常广泛。例如,药厂用特定的合成酶来合成抗生素;洗衣粉中添加酶能加速附着在衣物上的蛋白质、淀粉或脂肪渍的分解;嫩肉粉中加入木瓜蛋白酶能将蛋白质分解为稍小的分子,使肉的口感更嫩滑。

An enzyme is a biological macromolecule, usually a protein, that acts as a biological catalyst, accelerating chemical reactions without being consumed in the process. The molecules on which enzymes act are called substrates, which are converted into products. Nearly all metabolic processes within a cell depend on enzyme catalysis to occur at biologically relevant rates. A metabolic pathway is typically composed of a series of enzyme-catalyzed steps. The study of enzymes is known as enzymology, and a related field focuses on pseudoenzymes—proteins that have lost catalytic activity but may retain regulatory or scaffolding functions, often indicated by alterations in their amino acid sequences or unusual 'pseudocatalytic' behavior. Enzymes are known to catalyze over 5,000 types of biochemical reactions. Other biological catalysts include catalytic RNA molecules, or ribozymes, which are sometimes classified as enzymes despite being composed of RNA rather than protein.

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Pharmacokinetics

Catalysis

催化

催化(catalysis)或催化作用,是利用催化剂参与,改变化学反应速率而不影响化学平衡的作用。广泛发生于无机物反应、有机物反应、生物体内反应。 许多化学工业要利用催化作用来获得需要的反应速率。催化也是一种化工单元过程,催化剂本身在反应中不会被消耗,但催化剂会改变反应速率,一催化剂亦可能参与复数的催化反应。正催化剂可加速反应;负催化剂或抑制剂则会与反应物反应进而降低化学反应。可提高催化剂活性的物质称为促进剂;降低催化剂活性者则称为催化毒。 相较于未催化的反应,同温度的催化反应拥有较低的活化能。催化剂可以借由结合反应物达到极化的效果,如酸催化剂之于羰基化合物的合成;催化剂也可产生非自然的反应中间物,如以四氧化锇催化烯烃的双羟基化中产生的锇酸盐酯;催化剂亦可造成反应物的裂解,如制氢时产生的单原子氢。 很多物质都可以做催化剂,在无机物反应中,通常利用酸、碱、金属或金属化合物作为催化剂,在有机物反应中多用有性的蛋白质分子——酶作为催化剂,生物体内许多化学反应都依赖酶来进行的。 催化反应可以发生在均相催化和多相催化中,也可以发生在复相催化中:

Catalysis (, kə-TAL-iss-iss) is the increase in rate of a chemical reaction due to an added substance known as a catalyst ( KAT-əl-ist). Catalysts are not consumed by the reaction and remain unchanged after the reaction. If the reaction is rapid and the catalyst is recycled quickly, a very small amount of catalyst often suffices; mixing, surface area, and temperature are important factors in reaction rate. Catalysts generally react with one or more reactants to form intermediates that subsequently give the final reaction product, in the process of regenerating the catalyst. The rate increase occurs because the catalyst allows the reaction to occur by an alternative mechanism which may be much faster than the noncatalyzed mechanism. However the noncatalyzed mechanism does remain possible, so that the total rate (catalyzed plus noncatalyzed) can only increase in the presence of the catalyst and never decrease.

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Pharmacokinetics

Reaction rate constant

速率常数

在化学动力学中,反应速率常数,又称速率常数 k或 λ是化学反应速率的量化表示方式。 对于反应物A和反应物B反应成生成物C的化学反应,反应速率可表示成此式: d [ C ] d t = k ( T ) [ A ] m [ B ] n {\displaystyle {\frac {d[C]}{dt}}=k(T)[A]^{m}[B]^{n}} k(T)是反应速率常数,会随温度改变。假设反应发生在固定容积内,[A]和[B]代表两种反应物的莫耳浓度。 指数m和n称为反应级数,取决于反应机理,可由实验测定。将m和n相加,可得到反应的总级数。

In chemical kinetics, a reaction rate constant or reaction rate coefficient (⁠ k {\displaystyle k} ⁠) is a proportionality constant which quantifies the rate and direction of a chemical reaction by relating it with the concentration of reactants.

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Pharmacokinetics

Arrhenius equation

阿伦尼乌斯方程

阿瑞尼斯方程(英语:Arrhenius equation)是化学反应的速率常数与温度之间的关系式,适用于基元反应和非基元反应,甚至某些非均相反应。其不定积分形式为: k = A e − E a / R T {\displaystyle \ k=Ae^{{-E_{a}}/{RT}}} 或 ln ⁡ k = − E a R T + ln ⁡ A {\displaystyle \ \ln k=-{\frac {E_{a}}{RT}}+\ln A} 其中: k {\displaystyle \ k} 为反应的速率常数; A {\displaystyle \ A} 称为指前因子/阿伦尼乌斯常数,单位与 k…

In physical chemistry, the Arrhenius equation is a formula for the temperature dependence of reaction rates. In 1889 while working with Wilhelm Ostwald at Leipzig University, Svante Arrhenius proposed the equation on the basis of the work of Dutch chemist Jacobus Henricus van 't Hoff, who had noted in 1884 that the Van 't Hoff equation for the temperature dependence of equilibrium constants suggests such a formula for the rates of both forward and reverse reactions. This equation has a vast and important application in determining the rate of chemical reactions and for calculation of energy of activation. Arrhenius provided a physical justification and interpretation for the formula. Currently, it is best seen as an empirical relationship. It can be used to model the temperature variation of diffusion coefficients, population of crystal vacancies, creep rates, and many other thermally induced processes and reactions. The Eyring equation, developed in 1935, also expresses the relationship between rate and energy.

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Pharmacokinetics

Chemical potential

化学势

在热力学中,某种物质的化学势指的是,在化学反应或者相变中,此物质的粒子数发生改变时所吸收或放出的能量。在混合物中的某种物质的化学势定义为此热力学系统的吉布斯自由能对此物质粒子数的变化率,即偏导数(其他物质的粒子数及其他系统参数保持不变)。当温度和压强固定时,化学势也被称作偏摩尔吉布斯自由能,或者摩尔化学势。在化学平衡或相平衡状态下,自由能处于极小值,各种物质的化学势与化学计量系数乘积之和为零。 在半导体物理中,零温电子系统的化学势被称为费米能。

In thermodynamics, the chemical potential of a species is the energy that can be absorbed or released due to a change of the particle number of the given species, e.g. in a chemical reaction or phase transition. The chemical potential of a species in a mixture is defined as the rate of change of free energy of a thermodynamic system with respect to the change in the number of atoms or molecules of the species that are added to the system. Thus, it is the partial derivative of the free energy with respect to the amount of the species, all other species' concentrations in the mixture remaining constant. When both temperature and pressure are held constant, and the number of particles is expressed in moles, the chemical potential is the partial molar Gibbs free energy. At chemical equilibrium or in phase equilibrium, the total sum of the product of chemical potentials and stoichiometric coefficients is zero, as the free energy is at a minimum. In a system in diffusion equilibrium, the chemical potential of any chemical species is uniformly the same everywhere throughout the system.

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Pharmacokinetics

Thermodynamics

热力学

热力学(英语:thermodynamics) 是物理学的一个分支,研究热现象中能量的转换规律,特别是研究热、功和温度,以及它们与能量和熵的关系。热力学应用于许多科学和工程领域,特别是物理化学、生物化学、化学工程和机械工程,以及气象学等领域。 热力学发端于18世纪对气体和蒸汽机的研究。在19世纪,随着对热机效率和功与热量之间能量转换的研究。开始建立起热力学定律,标志着热力学理论的成熟。随着研究的深化,热力学研究被拓展到很多方面,比如相变化、化学反应、输运现象甚至是黑洞。 热力学的研究对象是由大量微观粒子组成的热力学系统。热力学系统温度、压强和内能等由宏观物理量描述,这些物理量的行为受到四个热力学定律的约束。热力学定律是从实验中总结出来的,但也可以通过统计力学从微观角度来解释。

Thermodynamics is a branch of physics that deals with heat, work, and temperature, and their relation to energy, entropy, and the physical properties of matter and radiation. The behavior of these quantities is governed by the four laws of thermodynamics, which convey a quantitative description using measurable macroscopic physical quantities but may be explained in terms of microscopic constituents by statistical mechanics. Thermodynamics applies to various topics in science and engineering, especially physical chemistry, biochemistry, chemical engineering, and mechanical engineering, as well as other complex fields such as meteorology. Historically, thermodynamics developed out of a desire to increase the efficiency of early steam engines, particularly through the work of French physicist Sadi Carnot (1824).

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Pharmacokinetics

Biochemistry

生物化学

生物化学或生物化学(与化学生物学不同)是对生物体内部和与之相关的化学过程的研究。生物化学是化学和生物学的子学科,可分为三个领域:结构生物学、酶学和新陈代谢。在 20 世纪的最后几十年中,生物化学通过这三个学科成功地解释了生命过程。生命科学的几乎所有领域都是通过生化方法和研究来发现和发展的。生物化学侧重于了解生物分子在活细胞内和细胞间发生的过程的化学基础,进而与对组织和器官以及生物体结构和功能的理解密切相关。

Biochemistry, or biological chemistry (distinct from chemical biology), is the study of chemical processes within and relating to living organisms. A sub-discipline of both chemistry and biology, biochemistry may be divided into three fields: structural biology, enzymology, and metabolism. Over the last decades of the 20th century, biochemistry has become successful at explaining living processes through these three disciplines. Almost all areas of the life sciences are being uncovered and developed through biochemical methodology and research. Biochemistry focuses on understanding the chemical basis that allows biological molecules to give rise to the processes that occur within living cells and between cells, in turn relating greatly to the understanding of tissues and organs as well as organism structure and function.

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Pharmacokinetics

Molecular biology

分子生物学

分子生物学是生物学的一个分支,旨在了解作为细胞内和细胞间生物活性基础的分子结构和化学过程。它主要集中于核酸(例如 DNA 和 RNA)和蛋白质的研究。它检查这些大分子的结构、功能和相互作用,因为它们协调复制、转录、翻译、蛋白质合成和复杂的生物分子相互作用等过程。分子生物学领域是多学科的,依赖于遗传学、生物化学、物理学、数学以及最近的计算机科学(生物信息学)的原理。

Molecular biology is a branch of biology that seeks to understand the molecular structures and chemical processes that are the basis of biological activity within and between cells. It is centered largely on the study of nucleic acids (such as DNA and RNA) and proteins. It examines the structure, function, and interactions of these macromolecules as they orchestrate processes such as replication, transcription, translation, protein synthesis, and complex biomolecular interactions. The field of molecular biology is multi-disciplinary, relying on principles from genetics, biochemistry, physics, mathematics, and more recently computer science (bioinformatics).

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Pharmacokinetics

Protein folding

蛋白质折叠

蛋白质折叠(英语:Protein folding)是蛋白质获得其功能性结构和构象的物理过程。通过这一物理过程,蛋白质从无规则卷曲折叠成特定的功能性三维结构。在从mRNA序列翻译成线性的氨基酸链时,蛋白质都是以去折叠多肽或无规则卷曲的形式存在。 蛋白质的基本单位为氨基酸,而蛋白质的一级结构指的就是其氨基酸序列。蛋白质会由所含氨基酸残基的亲水性、疏水性、带正电、带负电等特性通过残基间的相互作用而折叠成一立体的三级结构。 根据克里斯琴·B·安芬森(1972年的诺贝尔化学奖得主)的研究,蛋白质可由加热或置于某些化学环境而变性,三级结构解体;而当环境回复到原本的状态时,蛋白质可于不到一秒的时间折叠至原先的立体结构,不论试验几次,蛋白质都仅此一种立体结构,于是安芬森提出一个结论:蛋白质分子的一级结构决定其立体结构(安芬森法则)。 安芬森的研究结果非常重要,因为蛋白质的功能取决于其立体结构,而目前根据已知某基因序列可翻译获得对应蛋白质的氨基酸序列,即蛋白质的一级结构;如果从蛋白质的一级结构就能知道立体结构,那么即可直接从基因推测其编码蛋白质所对应的生物学功能。虽然蛋白质可在短时间中从一级结构折叠至立体结构,研究者却无法在短时间中从氨基酸序列计算出蛋白质结构,甚至无法得到准确的三维结构。因此,研究蛋白质折叠的过程,可以说是破译折叠密码的过程。 目前蛋白质的再折叠依然遵从先使用胍或脲变性,然后逐渐降低胍或者脲的浓度,也就是逐渐降低对蛋白质天然“回缩”能力的干扰。使其自然回到天然的最低能量状态。只是这个过程无法很好的控制肽链与肽链之间和肽链内部形成错误折叠的干扰。

Protein folding is the physical process by which a protein, after synthesis by a ribosome as a linear chain of amino acids, changes from an unstable random coil into a more ordered three-dimensional structure. This structure permits the protein to become biologically functional or active. The folding of many proteins begins even during the translation of the polypeptide chain. The amino acids interact with each other to produce a well-defined three-dimensional structure, known as the protein's native state. This structure is determined by the amino-acid sequence or primary structure. The correct three-dimensional structure is essential to function, although some parts of functional proteins may remain unfolded, indicating that protein dynamics are important.

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Pharmacokinetics

Protein primary structure

蛋白質一級結構

蛋白质一级结构(protein primary structure)是肽或蛋白质中氨基酸的线性序列,即氨基酸序列(amino acid sequence)。按照惯例,蛋白质的一级结构被报道从氨基末端(N)端到羧基末端(C)端。蛋白质生物合成最通常由细胞中的核糖体进行。肽也可以在实验室中合成。蛋白质一级结构可以直接进行蛋白质测序,或从DNA序列推断。 在生物化学里,生物分子的一级结构是其分子组成和分子间化学键结的精确模样。对于一典型的无分支、无交叉的生物聚合物(如DNA、RNA或典型的细胞内蛋白质等分子),其第一结构等同于描述其单体单位的序列,即如DNA序列和肽序列。“一级结构”这一名词在Linderstrom-Lang于1951年的Lane Medical Lectures上首次被提到。一级结构和一级序列有一点相似,即使在二级或三级结构中并没有平行的概念。

Protein primary structure is the linear sequence of amino acids in a peptide or protein. By convention, the primary structure of a protein is reported starting from the amino-terminal (N) end to the carboxyl-terminal (C) end. Protein biosynthesis is most commonly performed by ribosomes in cells. Peptides can also be synthesized in the laboratory. Protein primary structures can be directly sequenced, or inferred from DNA sequences.

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Pharmacokinetics

Ligand (biochemistry)

配體 (生物化學)

在生物化学和药理学中,配体(英语:ligand)是指一种能与受体结合以产生某种生理效果的物质。在蛋白质—配体复合物中,配体通常是与靶蛋白特定结合位点相连的信号触发分子。而在DNA—配体复合物中,与DNA双链相连的配体在一般情况下可以是任何的小分子或离子甚至是蛋白质。值得注意的是,生物化学中的配体和化学中定义的配体(比如铜氨络离子中,氨是铜离子的配体)并无实际联系,配体未必要结合在金属原子上。 配体与受体的连接由诸如离子键的化学键或氢键、范德华力等分子间作用力维系。它们的连接过程通常是可逆的,配体与受体之间形成的真正难以断开的共价键在生物界是相当罕见的。 配体在与受体结合后,可以改变它们的立体构型,而立体构型又常常决定了蛋白质的功能。配体包括底物、酶抑制剂、酶激活剂、以及神经递质。配体与受体结合的难易度与结合后的强度叫做亲和力。两者越容易结合,结合后结合的强度越大,则亲和力越强,反之亦然。亲和力不仅由配体和受体间的直接的相互作用决定,还由溶剂效应决定,后者间接主导溶液中的非共价性结合。 用放射性同位素标记的放射性配体已被用作正电子发射计算机断层扫描(PET)中的放射性示踪剂。此外,这种物质还被用于在体外进行的配体—受体结合研究。

In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ligare, which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems.

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Pharmacokinetics

G protein-coupled receptor

G蛋白偶联受体

G蛋白偶联受体(GPCR),也称为七次跨膜结构域受体、7TM受体、七螺旋受体、蛇形受体和G蛋白连接受体(GPLR),形成一大类进化相关的蛋白质,它们是细胞表面受体,可检测细胞外的分子并激活细胞反应。它们与 G 蛋白结合。它们以氨基酸残基的六个环(三个与配体分子相互作用的胞外环、三个与G蛋白相互作用的胞内环、一个N端胞外区和一个C端胞内区)的形式穿过细胞膜七次,这就是为什么它们有时被称为七次跨膜受体。

G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. They are coupled with G proteins. They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminal extracellular region and a C-terminal intracellular region) of amino acid residues, which is why they are sometimes referred to as seven-transmembrane receptors.

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Pharmacokinetics

Affinity chromatography

亲和色谱法

亲和色谱法(英语:Affinity chromatography,又称为亲和层析)是一种利用固定相的结合特性来分离分子的色谱方法。亲和色谱在凝胶过滤色谱柱上连接与待分离的物质有一定结合能力的分子,并且它们的结合是可逆的,在改变流动相条件时二者还能相互分离。亲和色谱可以用来从混合物中纯化或浓缩某一分子,也可以用来去除或减少混合物中某一分子的含量。

Affinity chromatography is a method of separating a biomolecule from a mixture, based on a highly specific macromolecular binding interaction between the biomolecule and another substance. The specific type of binding interaction depends on the biomolecule of interest; antigen and antibody, enzyme and substrate, receptor and ligand, or protein and nucleic acid binding interactions are frequently exploited for isolation of various biomolecules. Affinity chromatography is useful for its high selectivity and resolution of separation, compared to other chromatographic methods.

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Pharmacokinetics

Fluorescence

荧光

荧光(英语:fluorescence)是光致冷发光现象,可以在气体、液体或固体化学体系中发生。当某种常温物质分子在单重基态吸收某种波长的入射光(通常是紫外线或X光)后被激发至单重激发态而产生的。当电子从激发态返回到基态时(几乎立即(大约在 10^-8 秒内),是由于材料中的原子受到激发后会释放出一个能量较低、波长较长的光子,其能量低于之前吸收的光子(通常波长比入射光的波长,在可见光波段)而且由于再发射过程非常迅速,一旦激发源被移除,荧光便会立即停止,而不像磷光那样会持续发光一段时间。(其与磷光不同,是因为电子的自旋方向仍然与基态电子保持配对。)有这性质的出射光就称为荧光。一般以持续发光时间来分辨荧光或磷光,持续发光时间短于10−8秒的称为荧光,长于10−8秒的称为磷光(原因详见磷光),严谨的定义基于发光的物理机制,而非持续时间。在日常生活,人们通常把各种微弱的光都一律称为荧光。

Fluorescence is one of two kinds of photoluminescence, the emission of light by a substance that has absorbed light or other electromagnetic radiation. When exposed to ultraviolet radiation, many substances will glow (fluoresce) with colored visible light. The color of the light emitted depends on the chemical composition of the substance. Fluorescent materials generally cease to glow nearly immediately when the radiation source stops. This distinguishes them from the other type of light emission, phosphorescence. Phosphorescent materials continue to emit light for some time after the radiation stops. This difference in duration is a result of quantum spin effects. Fluorescence occurs when a photon from incoming radiation is absorbed by a molecule, exciting it to a higher energy level, followed by the emission of light as the molecule returns to a lower energy state. The emitted light may have a longer wavelength and, therefore, a lower photon energy than the absorbed radiation.

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Pharmacokinetics

Fluorescence anisotropy

荧光各向异性

荧光各向异性或荧光偏振是荧光团发射的光沿不同偏振轴具有不相等强度的现象。该领域的早期先驱包括 Aleksander Jablonski、Gregorio Weber 和 Andreas Albrecht。 Lakowicz 的书中介绍了荧光偏振的原理以及该方法的一些应用。

Fluorescence anisotropy or fluorescence polarization is the phenomenon where the light emitted by a fluorophore has unequal intensities along different axes of polarization. Early pioneers in the field include Aleksander Jablonski, Gregorio Weber, and Andreas Albrecht. The principles of fluorescence polarization and some applications of the method are presented in Lakowicz's book.

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Pharmacokinetics

Flow cytometry

流式细胞术

流式细胞术 (FC) 是一种用于检测和测量细胞或颗粒群的物理和化学特性的技术。在此过程中,含有细胞或颗粒的样品悬浮在液体中并注入流式细胞仪仪器中。样品被聚焦,理想情况下一次让一个细胞流过激光束,其中散射的光是细胞及其成分的特征。细胞通常用荧光标记进行标记,因此光被吸收,然后以一定波长带发射。可以快速检查数以万计的细胞,并由计算机处理收集的数据。流式细胞术常用于基础研究、临床实践和临床试验。流式细胞仪的用途包括:

Flow cytometry (FC) is a technique used to detect and measure the physical and chemical characteristics of a population of cells or particles. In this process, a sample containing cells or particles is suspended in a fluid and injected into the flow cytometer instrument. The sample is focused to ideally flow one cell at a time through a laser beam, where the light scattered is characteristic to the cells and their components. Cells are often labeled with fluorescent markers so light is absorbed and then emitted in a band of wavelengths. Tens of thousands of cells can be quickly examined and the data gathered are processed by a computer. Flow cytometry is routinely used in basic research, clinical practice, and clinical trials. Uses for flow cytometry include:

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Pharmacokinetics

Proteomics

蛋白质组学

蛋白质组学是对蛋白质的大规模研究。蛋白质组是由生物体或系统产生或修饰的整套蛋白质。蛋白质组学是一个跨学科领域,涵盖从蛋白质组成、结构和活性的整体水平对蛋白质组的探索。虽然蛋白质组的规模和复杂性非常巨大,但最近的技术进步大大扩展了蛋白质组分析的灵敏度和范围。蛋白质组学通常指蛋白质和蛋白质组的大规模实验分析,但通常特指蛋白质纯化和质谱分析。事实上,无论是在由数百万个细胞组成的大样本中,还是在单个细胞中,质谱分析都是分析蛋白质组的最强大的方法。

Proteomics is the large-scale study of proteins. The proteome is the entire set of proteins produced or modified by an organism or system. Proteomics is an interdisciplinary field that covers the exploration of proteomes from the overall level of protein composition, structure, and activity. While the scale and complexity of the proteome is formidable, recent technological progress has substantially expanded the sensitivity and scope of proteome analysis. Proteomics generally denotes the large-scale experimental analysis of proteins and proteomes, but often refers specifically to protein purification and mass spectrometry. Indeed, mass spectrometry is the most powerful method for analysis of proteomes, both in large samples composed of millions of cells, and in single cells.

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Wikipedia contributors · Retrieved2026-10-04 · CC BY-SA 4.0. Introductions were extracted as plain text and shortened. Language versions may emphasize different aspects.For concept reference; consult the original standards for authoritative requirements. The Chinese definition is a machine-assisted translation of the cited English introduction; check technical terminology against the original.

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Pharmacokinetics

Genomics

基因組學

基因组学是分子生物学的一个跨学科领域,专注于基因组的结构、功能、进化、作图和编辑。基因组是生物体的完整 DNA 集,包括其所有基因及其分层的三维结构配置。遗传学是指研究个体基因及其在遗传中的作用,与此相反,基因组学旨在对生物体的所有基因、它们的相互关系以及对生物体的影响进行集体表征和量化。基因可以在酶和信使分子的帮助下指导蛋白质的产生。反过来,蛋白质构成器官和组织等身体结构,并控制化学反应并在细胞之间传递信号。

Genomics is an interdisciplinary field of molecular biology focusing on the structure, function, evolution, mapping, and editing of genomes. A genome is an organism's complete set of DNA, including all of its genes as well as its hierarchical, three-dimensional structural configuration. In contrast to genetics, which refers to the study of individual genes and their roles in inheritance, genomics aims at the collective characterization and quantification of all of an organism's genes, their interrelations and influence on the organism. Genes may direct the production of proteins with the assistance of enzymes and messenger molecules. In turn, proteins make up body structures such as organs and tissues as well as control chemical reactions and carry signals between cells.

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Wikipedia contributors · Retrieved2026-10-04 · CC BY-SA 4.0. Introductions were extracted as plain text and shortened. Language versions may emphasize different aspects.For concept reference; consult the original standards for authoritative requirements. The Chinese definition is a machine-assisted translation of the cited English introduction; check technical terminology against the original.

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Pharmacokinetics

Metabolomics

代谢物组学

代谢组学是对涉及代谢物、小分子底物、中间体和细胞代谢产物的化学过程的科学研究。具体来说,代谢组学是“对特定细胞过程留下的独特化学指纹的系统研究”,即对其小分子代谢物谱的研究。代谢组代表生物细胞、组织、器官或生物体中完整的代谢物集,它们是细胞过程的最终产物。信使 RNA (mRNA)、基因表达数据和蛋白质组分析揭示了细胞中产生的一组基因产物,这些数据代表了细胞功能的一个方面。相反,代谢分析可以提供该细胞生理学的即时快照,因此,代谢组学提供了生物体的直接“生理状态的功能读数”。

Metabolomics is the scientific study of chemical processes involving metabolites, the small molecule substrates, intermediates, and products of cell metabolism. Specifically, metabolomics is the "systematic study of the unique chemical fingerprints that specific cellular processes leave behind", the study of their small-molecule metabolite profiles. The metabolome represents the complete set of metabolites in a biological cell, tissue, organ, or organism, which are the end products of cellular processes. Messenger RNA (mRNA), gene expression data, and proteomic analyses reveal the set of gene products being produced in the cell, data that represents one aspect of cellular function. Conversely, metabolic profiling can give an instantaneous snapshot of the physiology of that cell, and thus, metabolomics provides a direct "functional readout of the physiological state" of an organism.

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Wikipedia contributors · Retrieved2026-10-04 · CC BY-SA 4.0. Introductions were extracted as plain text and shortened. Language versions may emphasize different aspects.For concept reference; consult the original standards for authoritative requirements. The Chinese definition is a machine-assisted translation of the cited English introduction; check technical terminology against the original.

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