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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 pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

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.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...
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...
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,...
Drug Dissolution: Requirements and Profile Comparison01:14

Drug Dissolution: Requirements and Profile Comparison

The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...
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...

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Dissolution-permeation approach for biopharmaceutical evaluation: a feasibility study using naproxen.

Andrejs Sitovs1,2, Katarina Gurkina1, Liga Petersone1

  • 1Leading Research Group, Faculty of Pharmacy, Rīga Stradiņš University, Riga, Latvia.

Journal of Pharmacy & Pharmaceutical Sciences : a Publication of the Canadian Society for Pharmaceutical Sciences, Societe Canadienne Des Sciences Pharmaceutiques
|May 27, 2026
PubMed
Summary

A new dissolution-permeation system integrating an Ussing chamber allows simultaneous testing of drug dissolution and permeability. This method, using naproxen, provides insights into drug absorption for poorly soluble compounds.

Keywords:
BCSdissolutionnaproxenpermeabilitypermeation

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Published on: September 20, 2017

Area of Science:

  • Pharmaceutical Sciences
  • Biopharmaceutics
  • Drug Delivery

Background:

  • Dissolution profiles alone are insufficient for predicting in vivo absorption of poorly soluble drugs.
  • Permeation testing is crucial for biopharmaceutical assessment.
  • Existing dissolution-permeation systems have limitations, including lack of compendial dissolution, small acceptor volumes, and incompatibility with ex vivo membranes.

Purpose of the Study:

  • To develop and evaluate a novel dissolution-permeation system by integrating an Ussing chamber with a dissolution apparatus.
  • To address the limitations of current systems for biopharmaceutical assessment.
  • To enable simultaneous determination of drug dissolution and permeability.

Main Methods:

  • The study assembled a dissolution-permeation system incorporating an Ussing chamber.
  • The system evaluated the impact of soy L-α-phosphatidylcholine in dodecane (LiDo) concentrations (5% and 10%) and membrane material on naproxen apparent permeability.
  • Naproxen, a BCS II class drug, was used as the model compound.

Main Results:

  • Naproxen release from tablets reached ~100% within 30 minutes.
  • Apparent permeability coefficients (Papp) for naproxen were determined across PVDF and PC membranes with varying LiDo concentrations.
  • Papp values were approximately 100-fold lower than literature values, potentially due to differences in sink conditions and membrane composition.

Conclusions:

  • The proposed system enables simultaneous dissolution and permeability testing.
  • The use of a PC membrane resulted in higher apparent permeability compared to PVDF.
  • Further refinement of this methodology could facilitate ex vivo membrane dissolution-permeability testing.