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Related Concept Videos

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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Acids are classified by the number of protons per molecule that they can give up in a reaction. Acids such as HCl, HNO3, and HCN that contain one ionizable hydrogen atom in each molecule are called monoprotic acids. Their reactions with water are:
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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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Complexation Equilibria: Factors Influencing Stability of Complexes01:09

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In complexation reactions, metal cations are the electron pair acceptors, and the ligands are the electron pair donors. The stability of the metal complexes depends primarily on the complexing ability of the central metal ion and the nature of the ligands. Generally, the complexing ability of the metal ion depends on the size and charge of the ion. As the metal ion size increases, the stability of the metal complexes decreases, provided that the valency of the metal ion and the ligands remain...
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Crystal Growth: Principles of Crystallization01:25

Crystal Growth: Principles of Crystallization

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Crystallization is a phase transformation process in which crystals are precipitated from a supersaturated solution or formed from other sources. During crystallization, atoms or molecules arrange themselves into a well-defined, rigid crystal lattice to minimize energy.
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Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
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Novel Ascorbic Acid Co-Crystal Formulations for Improved Stability.

Hui Zhang1, Huahui Zeng2, Mengfei Li1,2

  • 1Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China.

Molecules (Basel, Switzerland)
|November 26, 2022
PubMed
Summary
This summary is machine-generated.

New ascorbic acid co-crystals exhibit enhanced stability against light, pH, and temperature variations. These findings offer potential for improved vitamin C formulations and applications.

Keywords:
ascorbic acidco-crystalshydrogen bondingimproved stability

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Area of Science:

  • Materials Science
  • Crystallography
  • Pharmaceutical Chemistry

Background:

  • Ascorbic acid (Vitamin C) is a vital nutrient with known instability issues.
  • Developing stable formulations is crucial for effective therapeutic and dietary applications.
  • Co-crystallization is a promising strategy to enhance the physicochemical properties of active pharmaceutical ingredients.

Purpose of the Study:

  • To synthesize and characterize novel ascorbic acid co-crystals.
  • To evaluate the enhanced stability of these co-crystals under various stress conditions.
  • To explore the molecular interactions governing the co-crystal formation and stability.

Main Methods:

  • Co-crystal synthesis via slow solvent evaporation and solvent-assisted grinding.
  • Characterization using single-crystal and powder X-ray diffraction, IR spectroscopy, DSC, and TGA.
  • Molecular dynamics simulations to analyze interaction energies and hydrogen bonding.

Main Results:

  • Successful formation of ascorbic acid co-crystals with five different co-crystal formers.
  • Demonstrated improved photostability, pH stability (especially at high pH), and thermal stability compared to free ascorbic acid.
  • MD simulations confirmed favorable interaction energies and predicted intermolecular hydrogen bonds.

Conclusions:

  • Co-crystallization effectively enhances the stability of ascorbic acid.
  • The developed co-crystals offer a promising approach for more stable vitamin C delivery systems.
  • Further research can optimize these co-crystals for specific pharmaceutical and nutraceutical applications.