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相关概念视频

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

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Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Drug Absorption Mechanism: Passive Membrane Transport01:23

Drug Absorption Mechanism: Passive Membrane Transport

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Passive transport is a method of drug absorption where small, lipid-soluble drugs can move across the cell membrane. This movement happens along the concentration gradient, which is a natural flow from higher to lower concentration areas. The speed at which the drug moves is directly related to its lipid–water partition coefficient. This means that the more a drug dissolves in lipids, the faster it diffuses or spreads throughout the body. It is important to note that most drugs are either...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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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...
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Pore Transport and Ion-Pair Transport01:17

Pore Transport and Ion-Pair Transport

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Pore transport and ion-pair formation are critical mechanisms for the absorption and distribution of drugs in the body.
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited  but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
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A Method for Determination and Simulation of Permeability and Diffusion in a 3D Tissue Model in a Membrane Insert System for Multi-well Plates
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通过皮肤吸收的溶解性-透性-矩阵相互作用的例子是西奥菲林.

Sophia Engel1, Jozef Al-Gousous1, Christiane Grünewald2

  • 1Department of Biopharmaceutics and Pharmaceutical Technology, Johannes Gutenberg University Mainz, 55128, Mainz, Germany.

AAPS PharmSciTech
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概括
此摘要是机器生成的。

阿米诺菲林在通过皮肤贴片的皮肤透率高于西奥菲林. 这是由于其作为悬浮剂的配方,增强其化学潜力,通过水性途径更好地传递药物.

关键词:
亚米诺菲林 (Aminophylline) 是一种氨基酸.透性 透性的角质层 (stratum corneum) 是一个层.泰奥菲林 (Theophylline) 是一种神奇的东西.通过皮肤贴的贴片.

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科学领域:

  • 制药科学 制药科学
  • 生物材料科学 生物材料科学
  • 药物运输 药物运输 药物运输

背景情况:

  • 角层是通过皮肤传递诸如阿米诺菲林之类的爱水和电离药物的主要障碍.
  • 了解药物溶解性,皮肤透性和补丁矩阵之间的相互作用对于有效的透皮配方至关重要.

研究的目的:

  • 为了研究氨基和理论在基甲基纤维素 (HPMC) 和基于的Bio-PSA透皮贴片中的溶解性-透性矩阵相互作用.
  • 评估不同透增强剂对这些模范药物通过皮肤传递的影响.

主要方法:

  • 用猪耳皮的弗朗兹扩散细胞进行体外皮肤透研究.
  • 使用透析膜进行了补充释放研究.
  • 评估透增强剂Geraniol和Transcutol P对药物透的影响.

主要成果:

  • 在HPMC和Bio-PSA矩阵中,相比于theophylline,阿米诺菲林表现出显著更高的皮肤间流量.
  • 悬浮氨基林的高热力学活性增强了化学潜能梯度,促进了通过水路的透.
  • 格拉尼奥尔通过破坏角层脂质有效地增加了皮肤透率,而Transcutol P由于有限的矩阵相互作用和释放,显示了适度的效果.

结论:

  • 药物溶解性和增强剂性质对于水友药物通过皮肤传递至关重要.
  • 优化矩阵参数,如厚度,水分和释放特征,对于最大限度地提高皮肤贴片中的溶解度-透度相互作用至关重要.