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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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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).
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Polymers: Molecular Weight Distribution01:10

Polymers: Molecular Weight Distribution

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For any given polymer, the weight average molecular weight (Mw) is higher than, if not equal to, the number average molecular weight (Mn). The only situation in which the weight average molecular weight and the number average molecular weight are equal is when a polymer consists only of chains with equal molecular weight. However, this never happens in a synthetic polymer, since it is difficult to control the polymerization process up to a molecular level with accuracy to a hundred percent.
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Children at play often make suspensions such as mixtures of mud and water, flour and water, or a suspension of solid pigments in water known as tempera paint. These suspensions are heterogeneous mixtures composed of relatively large particles visible to the naked eye or seen with a magnifying glass. They are cloudy, and the suspended particles settle out after mixing. The suspended particles in a suspension settle out after some time of mixing. The separation of particles from a suspension is...
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Children at play often make suspensions such as mixtures of mud and water, flour and water, or a suspension of solid pigments in water known as tempera paint. These suspensions are heterogeneous mixtures composed of relatively large particles that are visible to the naked eye or can be seen with a magnifying glass. They are cloudy, and the suspended particles settle out after mixing. On the other hand, a solution is a homogeneous mixture in which no settling occurs and in which the dissolved...
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There is no one solvent that can dissolve every type of solute. Some substances that readily dissolve in a certain solvent might be insoluble in a different solvent. A simple way to predict which substances dissolve in which solvent is the phrase "like dissolves like". This means that polar substances, such as salt and sugar, dissolve in a polar substance like water. In contrast, non-polar substances are more soluble in non-polar solvents such as carbon tetrachloride.
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The high insolubility of some precipitates can result in an unfavorable relative supersaturation. This can lead to colloidal particles with a large surface-to-mass ratio, where adsorption is promoted. For instance, in the precipitation of silver chloride, silver ions are adsorbed on the surface of the colloidal particles, forming a primary layer. This layer attracts ions of opposite charge (such as nitrate ions), forming a diffuse secondary layer of adsorbed ions. This electric double layer...
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Dispersion of Nanomaterials in Aqueous Media: Towards Protocol Optimization
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在固体分散中的多态性.

Karina Sanabria Ortiz1,2, José R Hernández Espinell1,2, Desire Ortiz Torres1,2

  • 1Department of Chemistry, University of Puerto Rico, Río Piedras Campus, San Juan, Puerto Rico 00931, United States.

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概括

制备方法显著影响固体分散的多态形式. 融合方法产生混合多态,而基于溶剂的方法产生单晶形式,这对于准确的相位图和药物质量至关重要.

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科学领域:

  • 制药科学 制药科学
  • 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.

背景情况:

  • 固体分散通过在聚合物载体中嵌入活性药物成分 (API) 来提高药物的溶解性.
  • 常见的制备技术包括溶剂蒸发,溶剂融合和融合方法.
  • 这些技术经常用于相位图的确定,但它们对API多态性的影响还未得到充分研究.

研究的目的:

  • 研究不同制备方法对晶体固体分散 (CSD) 的多态形式的影响.
  • 分析制备技术对流胺酸 (FFA) 和聚乙烯糖醇 (PEG) 系统相图测定的影响.

主要方法:

  • 使用溶剂蒸发,溶剂融合和融合方法制备晶体固体分散剂 (CSD).
  • 使用粉末X射线衍射 (PXRD),红外光谱 (IR) 和差分扫描热量计 (DSC) 进行物理混合物和CSD的表征.

主要成果:

  • 融合方法导致CSD中同时存在的芬胺酸多态 (FFA I和FFA III).
  • 溶剂蒸发和溶剂融合方法主要产生了FFA III多态.
  • 准备方法显著影响了相位图的确定,平均相对偏差小于或等于8%.

结论:

  • 准备方法的选择极大地影响了固体分散的多态结果.
  • 精确的相位图的确定,对于工艺设计和质量控制至关重要,取决于选择适当的制备技术.
  • 了解制备方法对多态性的影响,可以确保制药配方的关键质量属性.