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相关概念视频

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).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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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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X-ray Diffraction of Biological Samples01:10

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X-ray diffraction or XRD is an analytical tool that utilizes X-rays to study ordered structures such as crystalline organic and inorganic samples, polycrystalline materials, proteins, carbohydrates, and drugs.
According to Bragg's law, when X-rays strike the sample positioned on a stage, the rays are  scattered by the electron clouds around the sample atoms. The  X-ray diffraction or scattering is caused by constructive interference of the X-ray waves that reflect off the internal...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

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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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Racemic Mixtures and the Resolution of Enantiomers02:30

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A racemic mixture, or racemate, is an equimolar mixture of enantiomers of a molecule that can be separated using their unique interaction with chiral molecules or media. Racemic mixtures are denoted by the (±)- prefix. This ‘optical rotation descriptor’ applies to the whole solution of a racemic mixture rather than a specific stereoisomer. Enantiomers typically have the same physical and chemical properties. Hence, they are not easily separable. However, enantiomers can exhibit...
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Recrystallization is a purification technique used to separate impurities from solid compounds. In this technique, no chemical reactions occur. Instead, it exploits physical properties only, specifically, the solubility differences between the desired compound and impurities, either at a single temperature or at different temperatures, and under other selected conditions. The solid-solution equilibrium (solubility equilibrium) of each component in the solution represents a binary phase...
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A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
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同时的XRD-DSC识别了正确的药物-聚合物溶解性和混合性,用于反转变型固体形式.

Mustafa Bookwala1, Jiawanjun Shi2, Ira S Buckner1

  • 1School of Pharmacy and Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Ave, Pittsburgh, PA 15282, USA.

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概括

同时的X射线衍射 (XRD) 和差异扫描热度计 (DSC) 准确地确定了胺固体形式的热力学特性. 这种结合技术避免了经常仅用DSC看到的误解,这对于无形固体分散稳定性至关重要.

关键词:
无形固体分散的分散.溶解终点是溶解的终点.异能热的固体形成了固体形式.物理稳定性 物理稳定性多态依赖性溶解度的多态依赖性多态转换的多态转换.同时进行XRD-DSCC.

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科学领域:

  • 固态化学 固态化学
  • 材料科学是一种材料科学.
  • 制药科学 制药科学

背景情况:

  • 无形固体分散 (ASDs) 提高了药物的溶解性和生物可用性.
  • 自闭症的物理稳定性与药物聚合物的热力学特性如可溶性和可混合性密切相关.
  • 公胺呈现复杂的固体形式,需要精确的表征以获得稳定的ASD配方.

研究的目的:

  • 描述烯胺复杂固体形式的热力学特性.
  • 评估同时使用X射线衍射 (XRD) -差分扫描热度计 (DSC) 评估药物-聚合物相互作用的实用性.
  • 为了比较结合的XRD-DSC与单独的DSC的准确性,以确定固体形式的转换和可混合性.

主要方法:

  • 同时进行XRD-DSC测量,对胺和其混合物与聚烯酸乙烯酸乙烯酸随机共聚物 (PVPVA) 进行测量.
  • 最稳定的烯胺固体形式的结晶和结构溶液.
  • 使用XRD-DSC. 确定各种药物聚合物组合物的溶解终点 (Tend).
  • 从联合XRD-DSC与单独的DSC获得的热力学数据的比较分析.

主要成果:

  • 同时的XRD-DSC成功地确定了在加热过程中对应不同胺固体形式的独特衍射模式.
  • 对溶解终点 (Tend) 的准确测量可以在广泛的胺-PVPVA化合物中实现.
  • 结合XRD-DSC提供了可靠的数据来估计药物聚合物溶解性和可混合性,这对于ASD物理稳定性至关重要.
  • 分析显示,单靠DSC数据就可能导致关于固体形式及其转换的模两可或不正确的结论.

结论:

  • 同时XRD-DSC是一种强大而准确的技术,用于表征复杂的固体形式及其热力学特性.
  • 这种结合方法增强了对药物聚合物可变性和可溶性的理解,这对于开发稳定的无形固体分散来说至关重要.
  • 该研究强调了仅在复杂系统中使用DSC的局限性,并强调了需要使用像XRD这样的补充技术来进行可靠的固态分析.