In-Vivo Analysis and Model-Based Prediction of Tensides' Influence on Drug Absorption

Area of Science:

• Pharmacokinetics
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Surfactants (tensides) influence drug absorption, crucial for controlled-release dosage forms.
• In-vivo absorption rates are difficult to measure directly, often substituted by in-vitro dissolution.
• Pharmacokinetic models offer direct prediction of absorption rates and bioavailability.

Purpose of the Study:

• To present a novel approach for analyzing drug absorption rates.
• To demonstrate the superiority of this new method over traditional in-vivo techniques.
• To analyze the influence of a specific surfactant (monolaurin of sucrose) on drug (sulfathiazole) absorption in rats.

Main Methods:

• In-vivo pharmacokinetic analysis in rats.
• Development and validation of a parsimonious predictive pharmacokinetic model.
• Comparison of model-based predictions with in-vivo observations.

Main Results:

• A 0.001% surfactant solution increased sulfathiazole absorption rate by approximately 50%.
• A two-fold increase in absolute bioavailability was observed with surfactant use.
• The developed pharmacokinetic model accurately predicted in-vivo results, confirming its validity.

Conclusions:

• Pharmacokinetic modeling provides a superior method for analyzing drug absorption compared to traditional in-vivo measurements.
• Surfactants can significantly enhance drug absorption and bioavailability.
• The study validates a predictive model for surfactant-mediated drug absorption.