转移稳定的多态生物是否总是生长得更快? 测量和比较托尔芬胺酸三种多态的生长动力学
Pietro Sacchi1,2, Petros Neoptolemou2, Roger J Davey2
1The Cambridge Crystallographic Data Centre 12 Union Road Cambridge CB2 1EZ UK psacchi@ccdc.cam.ac.uk.
Chemical science
|November 3, 2023
概括
这项研究测量了三种形式的托尔芬胺酸 (TFA) 的晶体生长率. 转移性TFA-II增长最快,TFA-IX在更高度下变得具有竞争力,两者都超过了稳定的TFA-I形式.
科学领域:
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
- 结晶科学 结晶科学
背景情况:
- 分子晶体多态性对于依赖结晶的制造业至关重要.
- 虽然多态的热力学预测是先进的,但由于实验数据稀缺,动力学预测仍然具有挑战性.
- 测量多态核和生长动力学是困难的,通常会产生不完整的数据.
研究的目的:
- 在异醇中实验测量和比较三种托尔芬胺酸 (TFA) 多态体 (I,II和IX) 的晶体生长动力学.
- 分析测量增长率与TFA多态的晶体结构之间的关系.
- 为了确定在不同的条件下,哪种多态生长速度更快.
主要方法:
- 在异醇溶液中实验测量三种TFA多态的晶体生长动力学.
- 分析与晶体结构相关的增长率.
- TFA晶体体体积的近似值,以比较相对增长率.
主要成果:
- 在所有溶液度中,转基因稳定的TFA-II多态体表现出最快的晶体生长.
- 转基因稳定的TFA-IX多态体显示,随着结晶的驱动力上升,其动力竞争力增加.
- 两种转移稳定的形式 (TFA-II和TFA-IX) 的生长速度都比稳定的TFA-I多态形式更快.
结论:
- 晶体生长动力学显著影响结晶过程中的多态化结果.
- 了解和测量多态生长率对于控制结晶至关重要.
- 这项研究为托尔芬胺酸的动态多态性研究提供了关键的实验数据.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
314
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
314
Three-Compartment Open Model
241
The three-compartment open model is a pharmacokinetic model used to describe the distribution and elimination of drugs following extravascular administration. It comprises a central compartment representing the plasma and two peripheral compartments. The highly perfused peripheral compartment represents organs and tissues with a rich blood supply, such as the liver, kidneys, and lungs. The scarcely perfused peripheral compartment represents tissues with lower blood supply, such as adipose...
241
Drug Distribution: Tissue Binding
2.7K
Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
For...
For...
2.7K
Nonlinear Pharmacokinetics: Causes of Nonlinearity
204
Nonlinearity in drug pharmacokinetics is caused by various factors influencing how a drug is absorbed, distributed, metabolized, and excreted. Understanding these nonlinear processes is crucial for predicting drug behavior in the body and optimizing drug dosing regimens.
Nonlinear drug absorption can occur when the process is rate-limited by solubility, carrier-mediated transport systems, or saturation of the presystemic gut wall or hepatic metabolism. For instance, high doses of riboflavin...
Nonlinear drug absorption can occur when the process is rate-limited by solubility, carrier-mediated transport systems, or saturation of the presystemic gut wall or hepatic metabolism. For instance, high doses of riboflavin...
204
Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance
163
The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
A study on guinea pigs examined the...
A study on guinea pigs examined the...
163
Time Course of Drug Effect
2.1K
The progression of a drug's impact can be analyzed by examining both the concentration-time course and the effect-time course. The concentration-time course is determined by the drug's half-life and is influenced by factors such as its pharmacokinetics, including absorption, distribution, metabolism, and elimination. The effect of the drug is often related to its concentration in the plasma and is calculated using the maximum drug effect and the plasma concentration that generates 50...
2.1K


