Formulation and evaluation of sustained release paracetamol tablets

Area of Science:

• Pharmaceutical Sciences
• Pharmacokinetics
• Drug Delivery Systems

Background:

• Conventional paracetamol formulations offer rapid but short-lived pain relief.
• Developing sustained-release formulations requires robust methods to predict in vivo performance.
• Non-invasive monitoring of drug levels, such as in saliva, can simplify pharmacokinetic assessments.

Purpose of the Study:

• To develop and evaluate slow-releasing paracetamol tablet formulations.
• To establish a correlation between in vitro dissolution and in vivo drug absorption.
• To validate saliva paracetamol levels as a predictor of plasma concentrations and pharmacokinetic parameters.

Main Methods:

• Production of compression-coated, slow-release paracetamol tablets.
• In vitro dissolution testing of the novel formulations.
• In vivo pharmacokinetic studies comparing new formulations with a conventional product.
• Analysis of paracetamol concentrations in both saliva and plasma.
• Correlation analysis between in vitro dissolution data, saliva levels, and plasma pharmacokinetic parameters.

Main Results:

• Slow-releasing paracetamol tablets successfully maintained therapeutic drug levels for up to 5 hours.
• A significant correlation was confirmed between paracetamol concentrations in saliva and plasma.
• In vitro dissolution data effectively predicted in vivo pharmacokinetic parameters.
• The dissolution test proved useful in the predictive development of the slow-release formulation.

Conclusions:

• Slow-releasing paracetamol formulations can provide prolonged therapeutic effects.
• Saliva analysis offers a viable, non-invasive method for estimating pharmacokinetic parameters.
• In vitro dissolution testing is a valuable predictive tool for developing optimized drug delivery systems.
• The developed compression-coated formulation demonstrates potential for extended pain management.