Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Dexibuprofen, a poorly water-soluble non-steroidal anti-inflammatory drug (NSAID), exhibits limited bioavailability.
• Improving the solubility and dissolution rate of dexibuprofen is crucial for enhancing its therapeutic efficacy.
• Current formulations may not provide optimal pharmacokinetic profiles for rapid pain relief and sustained action.

Purpose of the Study:

• To develop a novel controlled-release (CR) dexibuprofen formulation with improved solubility and bioavailability.
• To create a dual-release system combining immediate-release (IR) and sustained-release (SR) components.
• To evaluate the pharmacokinetic profile of the developed CR formulation compared to conventional dexibuprofen powder.

Main Methods:

• Spray-drying technique was employed to create a dexibuprofen-loaded solid dispersion for the IR component.
• The IR formulation utilized dexibuprofen/poloxamer 407/hydroxypropyl methylcellulose (HPMC) 2910 (50 cps)/sodium lauryl sulfate (SLS).
• The SR formulation consisted of dexibuprofen/ethylcellulose/HPMC 2910 (4000 cps)/magnesium stearate, and both were encapsulated into hard gelatin capsules to form the CR product.

Main Results:

• The IR solid dispersion significantly increased dexibuprofen's solubility and dissolution rate.
• The IR formulation demonstrated higher initial plasma concentration, area under the curve (AUC), and maximum concentration (Cmax) compared to dexibuprofen powder.
• The developed CR formulation exhibited a 5.5-fold increase in AUC and a 3.5-fold increase in Cmax versus dexibuprofen powder.

Conclusions:

• The spray-dried solid dispersion effectively enhanced the solubility and dissolution of dexibuprofen.
• The developed CR formulation provides a promising approach for achieving both rapid onset and prolonged therapeutic effects.
• This novel CR dexibuprofen formulation may serve as an improved oral dosage form for managing pain effectively.