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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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...
Structure of Amines01:19

Structure of Amines

The hybridized nitrogen atom in amines possesses a lone pair of electrons and is bound to three substituents with a bond angle of around 108°, which is less than the tetrahedral angle of 109.5°. However, the C–N–H bond angle is slightly larger at 112°, with a carbon–nitrogen bond length of 147 pm. This carbon–nitrogen bond length of of amines is longer than the carbon–oxygen bond of alcohols (143 pm) but shorter than alkanes’ carbon–carbon bond (154 pm). These aspects are illustrated in Figure...
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
Polymer Classification: Crystallinity01:21

Polymer Classification: Crystallinity

Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
Ionic Crystal Structures02:42

Ionic Crystal Structures

Ionic crystals consist of two or more different kinds of ions that usually have different sizes. The packing of these ions into a crystal structure is more complex than the packing of metal atoms that are the same size.
Most monatomic ions behave as charged spheres, and their attraction for ions of opposite charge is the same in every direction. Consequently, stable structures for ionic compounds result (1) when ions of one charge are surrounded by as many ions as possible of the opposite...
Structures of Carboxylic Acid Derivatives01:28

Structures of Carboxylic Acid Derivatives

Structure of Carboxylic Acid Derivatives
Carboxylic acid derivatives contain an acyl group attached to a heteroatom such as chlorine, oxygen, or nitrogen. The carbonyl carbon and oxygen are both sp2-hybridized with an unhybridized p orbital.
The three sp2 orbitals of the carbonyl carbon form three σ bonds, one each with the carbonyl oxygen, the α carbon, and the heteroatom, whereas the other two sp2 orbitals of the carbonyl oxygen are occupied by the lone pairs. Further, the unhybridized p...

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Application and Methodology of the Non-destructive 19F Time-domain NMR Technique to Measure the Content in Fluorine-containing Drug Products
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Application and Methodology of the Non-destructive 19F Time-domain NMR Technique to Measure the Content in Fluorine-containing Drug Products

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フルフェナミク酸の非変形性と,構造が解けた多形化合物の新記録.

Vilmalí López-Mejías1, Jeff W Kampf, Adam J Matzger

  • 1Department of Chemistry and the Macromolecular Science and Engineering Program, University of Michigan-Ann Arbor, 930 North University Avenue, Ann Arbor, Michigan 48109-1055, USA.

Journal of the American Chemical Society
|June 14, 2012
PubMed
まとめ

非ステロイド性抗炎症薬 (NSAID) であるフルーフェナミク酸 (FFA) は,前例のない多形性を示しています. 研究者らは9つの異なる結晶形を合成し,FFAがオクトモルフであることを確認し,その相選択に影響を与える複雑な要因を強調しました.

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Neutron Crystallography Data Collection and Processing for Modelling Hydrogen Atoms in Protein Structures
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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode
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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode

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Application and Methodology of the Non-destructive 19F Time-domain NMR Technique to Measure the Content in Fluorine-containing Drug Products
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Published on: August 22, 2017

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科学分野:

  • マテリアルサイエンス 材料科学
  • クリスタログラフィーです.
  • 医薬品科学 医薬品科学とは

背景:

  • ポリモルフィズム,すなわち固体の物質が複数の結晶形に存在する能力は,薬物の特性に大きな影響を与えます.
  • 非ステロイド性抗炎症薬 (NSAID) であるフルーフェナミク酸 (FFA) は,以前は限られた結晶形であることが知られていた.
  • FFAのポリモルフィズムを理解することは,その医薬品開発と有効性にとって極めて重要です.

研究 の 目的:

  • フルーフェナミク酸 (FFA) の広範なポリモルフィズムを調査し,特徴づけること.
  • FFAの異なる結晶形へのアクセスと解明のための新しい方法を探求する.
  • FFAの結晶化と相選択を左右する運動要因を理解する.

主な方法:

  • 結晶化を誘導するために,ポリマー誘導ヘテロ核化 (PIHn) を利用しました.
  • 低温での固体-固体変換技術を使用した.
  • 先進的な分析技術を使用して,得られた結晶形の構造の解明を行いました.

主要な成果:

  • フルーフェナミク酸 (FFA) の9つの異なるポリモルフにアクセスしました.
  • FFAがオクトモルフィックであることが確認され,以前に知られている2つの形に加えて6つの新たに特徴づけられた形があります.
  • 単一のPIHn条件下での複数のポリモルフの同時発生を観察し,複雑な結晶化運動性を示した.

結論:

  • フルーフェナミク酸 (FFA) は,顕著で前例のない多形性を示しています.
  • ポリマー誘発異核化 (PIHn) は,多様なFFAポリモルフにアクセスするための効果的な戦略です.
  • FFAの相選択は,結晶化中の動的要因の複雑な相互作用によって支配されます.