在研究体外药物穿透通过粘膜的近期进展
Juan Song1, Zizhao Xu2, Lingxiao Xie1
1Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, RI 02881, USA.
Pharmaceutics
|February 26, 2025
概括
试验室透测试 (IVPT) 通过评估药物释放和透来评估跨粘膜药物递送系统. 本次审查涵盖了粘膜壁垒,IVPT方法以及药物开发和生物等价性测试中的未来应用.
科学领域:
- 药理学和制药科学 药理学和制药科学
- 生物医学工程 生物医学工程
- 药物输送系统 药物输送系统
背景情况:
- 跨菌体的药物产品 (气溶,薄膜,半固体,假药,药片) 针对各种疾病.
- 粘膜药物吸收取决于组织结构和施用路径生理学 (鼻腔,直肠,阴道).
- 试验室透测试 (IVPT) 是一种具有成本效益的方法,用于评估药物释放和透的跨粘膜输送.
研究的目的:
- 审查不同跨粘膜路径的粘膜透障碍.
- 讨论关于开发体外透测试 (IVPT) 方法的考虑.
- 突出IVPT在跨粘膜药物产品的配方,质量控制和生物等价性方面的作用.
主要方法:
- 关于鼻腔,直肠和阴道通道的关键粘膜透障碍的概述.
- 已建立的IVPT方法的概述:垂直扩散单元,流通扩散单元,Ussing室和跨井系统.
- 讨论新兴技术,如用于体外药物透研究的光学方法.
主要成果:
- 识别关键的跨粘膜透障碍物.
- 各种IVPT方法的比较,以确定它们在药物输送研究中的适用性.
- 探索体外-体内相关的潜力 (IVIVC) 在跨粘膜药物开发.
结论:
- IVPT 是一种有价值的工具,用于配方开发和质量控制的跨粘膜药物递送系统.
- 未来的研究应该专注于先进的IVPT方法和建立强大的IVIVC.
- IVPT具有很大的潜力,可以在体外对局部作用的膜产品进行生物等价性评估.
相关概念视频
01:16Methods for Studying Drug Absorption: In vitro
195
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
195
01:09Methods for Studying Drug Absorption: In situ
195
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
195
01:23Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport
356
Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
356
01:17Passive Diffusion: Overview and Kinetics
360
Passive diffusion is a critical process that allows small lipophilic drugs to cross the cell membrane along a concentration gradient. This mechanism's efficiency depends on four primary factors: the membrane's surface area, the drug's lipid-water partition coefficient, the concentration gradient, and the membrane's thickness.
When administered orally, drugs establish a substantial concentration gradient between the gastrointestinal (GI) lumen and the bloodstream, expediting...
When administered orally, drugs establish a substantial concentration gradient between the gastrointestinal (GI) lumen and the bloodstream, expediting...
360
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
168
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
168
01:24Cellular Membranes and Drug Transport
251
Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
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