Formulation of a extended release tablet containing dexibuprofen

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Pharmacokinetics

Background:

• Dexibuprofen, the active S(+)-enantiomer of ibuprofen, presents formulation challenges due to its low melting point.
• Amorphous solid dispersions can enhance the properties of low-melting-point drugs.
• Developing novel drug delivery systems for dexibuprofen is crucial for optimizing therapeutic outcomes.

Purpose of the Study:

• To prepare an amorphous form of dexibuprofen with an improved melting point using fused solid dispersion.
• To formulate and characterize immediate release, extended release, and dual release tablets of dexibuprofen.
• To evaluate the dissolution profiles and pharmacokinetic properties of the developed dexibuprofen formulations.

Main Methods:

• Fused solid dispersion method was employed to create amorphous dexibuprofen.
• Immediate, extended, and dual release tablets were compressed using varying amounts of release modulators (PEO 5,000,000).
• Dissolution profiles were analyzed, and pharmacokinetic evaluation was conducted in healthy volunteers comparing dual release tablets (DRT-1) to conventional immediate release tablets (Daxfen).

Main Results:

• The release profiles of extended release and dual release tablets were dependent on the concentration of PEO 5,000,000.
• Release kinetics for extended release tablets and the extended release component of dual release tablets followed a zero-order release model (correlation coefficient 0.982–0.995).
• Pharmacokinetic studies showed that the dual release tablet (300 mg) was bioequivalent to two doses of conventional immediate release tablets (300 mg each) taken 6 hours apart, within a 12-hour period.

Conclusions:

• Amorphous dexibuprofen prepared via fused solid dispersion is suitable for developing modified-release formulations.
• Dual release tablets offer a bioequivalent alternative to multiple doses of immediate-release dexibuprofen, potentially improving patient compliance.
• The release rate of dexibuprofen can be effectively modulated by incorporating release modifiers like PEO 5,000,000.