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Related Concept Videos

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...
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...
In Vitro Drug Dissolution: Alternative Methods01:17

In Vitro Drug Dissolution: Alternative Methods

Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
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...

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Related Experiment Video

Updated: Jun 6, 2026

Coherent anti-Stokes Raman Scattering (CARS) Microscopy Visualizes Pharmaceutical Tablets During Dissolution
09:59

Coherent anti-Stokes Raman Scattering (CARS) Microscopy Visualizes Pharmaceutical Tablets During Dissolution

Published on: July 4, 2014

IVIVR in oral absorption for fenofibrate immediate release tablets using dissolution and dissolution permeation

P Buch1, P Holm, J Q Thomassen

  • 1Department of Pharmaceutical Technology and Biopharmaceutics', Johannes Gutenberg-University, Mainz, Germany.

Die Pharmazie
|November 26, 2010
PubMed
Summary

A dissolution/permeation (D/P) system effectively predicted in vivo fenofibrate exposure in rats. In humans, micellar entrapment by surfactants, not dissolution, explained Cmax differences, highlighting permeation

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Area of Science:

  • Pharmaceutical Sciences
  • Pharmacokinetics
  • Drug Delivery Systems

Background:

  • Previous studies showed a dissolution/permeation (D/P) system could differentiate fenofibrate formulations and correlate with rat in vivo exposure.
  • Immediate-release fenofibrate formulations require careful assessment for consistent in vivo performance.

Purpose of the Study:

  • To investigate human pharmacokinetic data for six fenofibrate tablet formulations.
  • To evaluate the role of dissolution and permeation in predicting in vivo fenofibrate performance, specifically Cmax.
  • To understand how formulation excipients, like surfactants, influence fenofibrate's bioavailability.

Main Methods:

  • Analysis of pharmacokinetic data (AUC, Cmax) from human in vivo studies of six fenofibrate tablet formulations.
  • Utilized a permeation system with dialysis membranes to assess the impact of micellar entrapment by surfactants.
  • Correlated in vitro dissolution profiles with in vivo pharmacokinetic parameters.

Main Results:

  • No significant differences in Area Under the Curve (AUC) were observed between fenofibrate formulations in humans.
  • Significant differences in Maximum Concentration (Cmax) were found but were not explained by dissolution alone.
  • Permeation studies demonstrated that surfactants caused micellar entrapment and reduced fenofibrate mobility, explaining Cmax variations.

Conclusions:

  • Permeation, in addition to dissolution, is crucial for establishing accurate in vitro-in vivo correlations (IVIVC) for fenofibrate.
  • Surfactant-mediated micellar entrapment significantly impacts the Cmax of fenofibrate, a factor not captured by dissolution testing alone.
  • The D/P system, incorporating a permeation step, offers a more robust prediction of in vivo drug performance compared to dissolution alone.