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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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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization 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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Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
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Improving Nefiracetam Dissolution and Solubility Behavior Using a Cocrystallization Approach.

Xavier Buol1, Koen Robeyns1, Camila Caro Garrido1

  • 1Institute of Condensed Matter and Nanosciences, UCLouvain, 1 Place Louis Pasteur, B-1348 Louvain-la-Neuve, Belgium.

Pharmaceutics
|July 15, 2020
PubMed
Summary
This summary is machine-generated.

Researchers identified thirteen novel cocrystals of Nefiracetam, a poorly water-soluble nootropic. Three cocrystals formed with biocompatible agents showed improved solubility and dissolution rates compared to the original active pharmaceutical ingredient (API).

Keywords:
cocrystalsdissolution rateformulationnefiracetamsolid statesolubilitystability

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Area of Science:

  • Pharmaceutical Science
  • Materials Science
  • Medicinal Chemistry

Background:

  • Nefiracetam is a nootropic compound known for its poor water solubility, limiting its bioavailability.
  • Cocrystallization is a strategy to enhance the physicochemical properties of poorly soluble active pharmaceutical ingredients (APIs).

Purpose of the Study:

  • To identify and characterize novel cocrystals of Nefiracetam.
  • To evaluate the potential of biocompatible cocrystals to improve Nefiracetam's solubility, dissolution rate, and stability.

Main Methods:

  • Cocrystal screening and synthesis were performed.
  • Structural and physical characterization utilized techniques such as X-ray diffraction and differential scanning calorimetry.
  • Solubility, dissolution rate, and stability studies were conducted and compared to the Nefiracetam API.

Main Results:

  • Thirteen novel cocrystals of Nefiracetam were successfully identified.
  • Three cocrystals were formed using biocompatible agents: citric acid, oxalic acid, and zinc chloride.
  • These selected cocrystals exhibited enhanced solubility, dissolution rate, and stability compared to the parent Nefiracetam API.

Conclusions:

  • The study presents the first identification of Nefiracetam cocrystals.
  • Cocrystals utilizing citric acid, oxalic acid, and zinc chloride offer a promising approach to improve Nefiracetam's pharmaceutical properties.
  • These findings could lead to improved formulations and therapeutic efficacy of Nefiracetam.