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Theories of Dissolution: Diffusion Layer Model01:15

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Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
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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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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Various dissolution theories provide insight into the factors that influence the dissolution rate. Danckwerts' Model suggests that turbulence, rather than a stagnant layer, characterizes the dissolution medium at the solid-liquid interface. In this model, the agitated solvent contains macroscopic packets that move to the interface via eddy currents, facilitating the absorption and delivery of the drug to the bulk solution. The regular replenishment of solvent packets maintains the...
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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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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Characterization and Dissolution Study of Oxodipine from Solid Binary Systems.

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Thennomicroscopy and differential scanning calorimetry characterized oxodipine solid dispersions. Thermal analysis revealed drug-carrier interactions, enhancing oxodipine dissolution rates.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Oxodipine's dissolution rate is crucial for its therapeutic efficacy.
  • Solid dispersions are a promising strategy to enhance drug solubility and bioavailability.
  • Understanding drug-carrier interactions is key to optimizing solid dispersion formulations.

Purpose of the Study:

  • To characterize solid binary systems of oxodipine with PEG 6000, 2-hydroxypropyl-β-cyclodextrin, and mannitol.
  • To investigate the influence of carriers on oxodipine dissolution.
  • To elucidate the role of thermal analysis in differentiating physical mixtures and solid dispersions.

Main Methods:

  • Thennomicroscopy and differential scanning calorimetry (DSC) were used for thermal characterization.
  • Dissolution studies were conducted to assess drug release profiles.
  • Analysis focused on drug-carrier interactions and particle composition.

Main Results:

  • DSC curves could not differentiate physical mixtures from solid dispersions.
  • Thennomicroscopy effectively revealed drug-carrier interactions and particle composition in solid dispersions.
  • Physical mixtures showed improved dissolution due to carrier-induced desegregation and increased drug surface area.
  • Solid dispersions exhibited stronger drug-carrier interactions, significantly influencing oxodipine dissolution.

Conclusions:

  • Thennomicroscopy is a valuable tool for characterizing solid dispersions and understanding drug-carrier interactions.
  • Carrier type and proportion significantly impact oxodipine dissolution, particularly in solid dispersions.
  • Optimized solid dispersions can enhance oxodipine's dissolution profile through stronger drug-carrier interactions.