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Related Concept Videos

Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

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 employed to...
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...
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...
Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model01:09

Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model

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 concentration...
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

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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Dispersion of Nanomaterials in Aqueous Media: Towards Protocol Optimization
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Factors affecting the formation of eutectic solid dispersions and their dissolution behavior.

Sudha R Vippagunta1, Zeren Wang, Stefanie Hornung

  • 1Pharmaceutical and Analytical Development, Novartis Pharmaceutical Corporation, East Hanover, NJ 07936, USA. sudha.vippagunta@novartis.com

Journal of Pharmaceutical Sciences
|October 20, 2006
PubMed
Summary

Understanding eutectic solid dispersions requires analyzing drug properties and carrier interactions. Key factors influencing formation and dissolution include melting point, heat of fusion, lipophilicity, and specific drug-polymer interactions.

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Area of Science:

  • Materials Science
  • Pharmaceutical Sciences
  • Physical Chemistry

Background:

  • Poorly water-soluble drugs often exhibit low bioavailability.
  • Solid dispersions, particularly eutectic systems, can enhance drug dissolution.
  • Predicting solid dispersion formation and performance requires understanding drug-carrier interactions.

Purpose of the Study:

  • To elucidate factors governing eutectic/monotectic solid dispersion formation.
  • To investigate the influence of drug physicochemical properties and carrier characteristics on solid dispersion behavior.
  • To evaluate the impact of these factors on the dissolution of drug-carrier systems.

Main Methods:

  • Application of a theoretical model to predict solid dispersion formation for five poorly water-soluble drugs and polyethylene glycol (PEG).
  • Experimental phase diagram construction and dissolution testing for selected drug-PEG systems.
  • Evaluation of drug properties (melting point, heat of fusion, lipophilicity, molar volume) and PEG molecular weight.

Main Results:

  • Theoretical model successfully predicted eutectic/monotectic formation for most drugs, except flurbiprofen, when specific interactions were ignored.
  • Melting point, heat of fusion, and lipophilicity significantly influenced eutectic system formation.
  • Specific drug-carrier interactions and polymer molecular weight impacted eutectic composition and dissolution behavior, particularly for flurbiprofen-PEG systems.

Conclusions:

  • Drug crystal energy (heat of fusion) and lipophilicity are critical for eutectic system formation.
  • Specific intermolecular interactions between drug and carrier play a significant role in determining eutectic composition and dissolution.
  • Rational selection of water-soluble carriers for eutectic solid dispersions can be guided by understanding these influencing factors.