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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

346
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...
346
Solvents01:12

Solvents

64.8K
A solvent is a substance, most often a liquid, that can dissolve other substances. Here, the substance being dissolved is called a solute. When a solvent and a solute combine, they form a solution - a homogenous mixture of both the solvent and the solute. Water is a universal biological solvent. Its polar structure allows it to dissolve many other polar compounds. The ability of water to dissolve is governed by a balance between water molecules binding to each other and binding to the solute.
A...
64.8K
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

157
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
157
Drug Delivery: Overview01:16

Drug Delivery: Overview

327
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
327
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

590
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...
590
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

235
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...
235

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Updated: Jul 25, 2025

Preparation of Binary and Ternary Deep Eutectic Systems
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Preparation of Binary and Ternary Deep Eutectic Systems

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协同形态与深层阳性溶剂的配方,用于通过皮肤给药.

Yannick Guinet1, Laurent Paccou1, Alain Hédoux1

  • 1UMR 8207-UMET-Unité Matériaux et Transformations, Université de Lille, CNRS, INRAE, Centrale Lille, F-59000 Lille, France.

Pharmaceutics
|June 28, 2023
PubMed
概括

在局部配方中稳定无形布洛芬是有效药物输送的关键. 这项研究发现,特定的深溶解溶剂和共同形态混合物可以防止布洛芬再结晶,增强皮肤透.

科学领域:

  • 制药科学 制药科学
  • 材料科学 材料科学 材料科学
  • 物理化学 物理化学

背景情况:

  • 通过皮肤递送药物提供了口服药物的替代方案,最大限度地减少副作用.
  • 优化局部配方需要增强药物透和物理稳定性.
  • 像布洛芬这样的无形药物容易重新结晶,从而对疗效产生负面影响.

研究的目的:

  • 在新型局部配方中研究无形布洛芬的物理稳定性.
  • 探索使用深度环氧溶剂 (DES) 和共同形态混合物的稳定策略.
  • 了解依据布洛芬再结晶抑制的机制.

主要方法:

  • 使用低频拉曼光谱分析ibuprofen:L-menthol相图.
  • 在甲基醇:薄荷醇DES中研究无形布洛芬的稳定性.
  • 通过化和冷研磨来制备和表征氨酸-氨酸共形混合物.
  • 确定玻璃过渡温度 (Tg) 和分析结相互作用 (拉曼光谱).

主要成果:

  • 在不同度的ibuprofen:L-menthol混合物中观察到ibuprofen的再结晶.
  • 无形布洛芬在提摩尔:孟托尔DES中配制时表现出增强的稳定性.
关键词:
同形态的同形态.结冷磨的方法深性溶剂的溶剂.气结合是一种气结合.低频拉曼光谱法 低频拉曼光谱法

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  • 化处理的氨酸-氨酸混合物稳定了无形氨酸,而冷磨粉版本显示了再结晶.
  • 重结晶抑制与异分子键的优先形成有关,防止了不论Tg的IBUPROFEN二分化.
  • 结论:

    • 甲醇:醇DES和化处理的氨酸 - 布洛芬混合物有效地稳定无形布洛芬.
    • 异分子结合在防止局部配方中的布洛芬再结晶方面发挥着至关重要的作用.
    • 结果为设计稳定的无形药物配方提供了洞察力,用于通过皮肤递送.