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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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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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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...
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Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
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相关实验视频

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在球磨加工过程中不同化物多形态形式的形态化:跟踪固体到固体相位转换.

Mengwei Wang1, Junbo Gong2, Thomas Rades3

  • 1Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.

International journal of pharmaceutics
|November 6, 2023
PubMed
概括

球磨转化制药水晶的形式. 化物形式I和III直接变为无形,而形式II在无形化之前转换为形式I,无形性质的变化明显.

关键词:
形态无形的形式.无形的放松是一种放松.球磨机 球磨机 球磨机二化物是一种二化物.玻璃过渡温度是玻璃过渡温度.多态的多态体.

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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
  • 固态化学 固态化学

背景情况:

  • 球磨加工改变了除了减少颗粒大小之外的制药粉的特性.
  • 了解固态转换对于药物配方和稳定性至关重要.

研究的目的:

  • 在球磨加工过程中研究三种化胺晶体形式 (I,II和III) 的固态变化.
  • 描述造引起的物理性质变化,包括无形含量和玻璃过渡温度.

主要方法:

  • 制备三种富洛塞米德晶体形式.
  • 用不同的时间进行化胺样品的球磨.
  • 使用粉末X射线衍射 (PXRD) 和调制差分扫描热量计 (mDSC) 进行表征.

主要成果:

  • 形式I和III直接转化为无形状态.
  • 形式II表现出多态过渡到形式I,随后是无形化.
  • 形式III的无形分数显示,随着磨时间的增加,玻璃过渡温度 (Tg) 增加,表明无形到无形的转变.
  • 与I型和II型相比,I型和II型的无形分数具有较高的分子流动性,与III型相比,在削过程中Tg不变.

结论:

  • 球磨引发了不同的固态转换和furosemide晶体形式的属性变化.
  • 形式III在削过程中经历了不寻常的无形到无形的转变.
  • 观察到的转变和属性变化凸显了制药中的磨诱导的固态修饰的复杂性.