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Related Concept Videos

X-ray Diffraction of Biological Samples01:10

X-ray Diffraction of Biological Samples

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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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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

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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,...
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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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X-ray Crystallography02:18

X-ray Crystallography

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The size of the unit cell and the arrangement of atoms in a crystal may be determined from measurements of the diffraction of X-rays by the crystal, termed X-ray crystallography.
Diffraction
Diffraction is the change in the direction of travel experienced by an electromagnetic wave when it encounters a physical barrier whose dimensions are comparable to those of the wavelength of the light. X-rays are electromagnetic radiation with wavelengths about as long as the distance between neighboring...
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Using X-ray Diffraction Techniques for Biomimetic Drug Development, Formulation, and Polymorphic Characterization.

Israel Rodríguez1, Ritika Gautam2, Arthur D Tinoco1

  • 1Department of Chemistry, University of Puerto Rico Río Piedras, San Juan, PR 00925, USA.

Biomimetics (Basel, Switzerland)
|January 5, 2021
PubMed
Summary
This summary is machine-generated.

X-ray diffraction techniques, including SCXRD, PXRD, and PDF analysis, offer crucial structural insights for drug development. These methods enhance drug formulation, stability, and efficacy, accelerating the approval process.

Keywords:
X-ray crystallographyactive pharmaceutical ingredientamorphous solid dispersionsdrug productsexcipientspair distribution function

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Area of Science:

  • Materials Science
  • Pharmaceutical Sciences
  • Structural Biology

Background:

  • Drug development is a lengthy and costly process, often constrained by traditional approaches.
  • Optimizing drug targets and formulations is key to improving biocompatibility and efficacy.
  • X-ray structural characterization has become indispensable in drug discovery and design.

Purpose of the Study:

  • To review the application of X-ray structural techniques in drug development.
  • To highlight how these methods provide insights into drug formulation, stability, and efficacy.
  • To showcase the utility of pair distribution function (PDF) analysis for amorphous materials.

Main Methods:

  • Single Crystal X-ray Diffraction (SCXRD) for detailed structural and interaction analysis.
  • Powder X-ray Diffraction (PXRD) for assessing phase, purity, and stability of crystalline compounds.
  • Pair Distribution Function (PDF) analysis, particularly with synchrotron sources, for characterizing amorphous solids and amorphous solid dispersions (ASDs).

Main Results:

  • SCXRD elucidates structural details critical for disease understanding and therapeutic effects.
  • PXRD enables the determination of crystallinity, purity, and stability of drug compounds.
  • PDF analysis provides atomic-level insights into amorphous materials, vital for ASD formulation.

Conclusions:

  • X-ray structural techniques offer deep insights essential for effective drug formulation and development.
  • These analytical methods contribute to optimizing drug stability, administration, and overall efficacy.
  • Advancements in X-ray sources and techniques expand the study of diverse drug materials, including amorphous forms.