Development and Evaluation of a Cost-Effective, Carbon-Based, Extended-Release Febuxostat Tablet
Israa Hamid Al-Ani1, Mohammad Hailat2, Dina J Mohammed1
1Faculty of Pharmacy, PDRC, Al-Ahliyya Amman University, Amman 19328, Jordan.
Molecules (Basel, Switzerland)
|October 16, 2024
Summary
This study developed extended-release febuxostat (FEB) tablets using activated charcoal, improving drug release and patient compliance. The new formulation offers a cost-effective, controlled delivery solution with enhanced bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Febuxostat (FEB), a BCS Class II drug, exhibits poor solubility and high lipophilicity, complicating oral formulation development.
- Existing formulations may not provide optimal therapeutic profiles or patient compliance due to rapid drug release.
- Controlled-release drug delivery aims to improve efficacy and reduce dosing frequency.
Purpose of the Study:
- To develop a cost-effective extended-release febuxostat tablet formulation.
- To utilize activated charcoal as an adsorbent to modify febuxostat release characteristics.
- To evaluate the physical, in vitro, and in vivo performance of the developed formulation.
Main Methods:
- Formulation of eight different febuxostat-to-charcoal ratios.
- Characterization using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC).
- In vitro drug release studies adhering to United States Pharmacopeia (USP) standards.
- In vivo pharmacokinetic studies comparing extended-release and immediate-release tablets.
Main Results:
- The optimal formulation (1:0.25 FEB-to-charcoal ratio) achieved a consistent 12-hour zero-order drug release profile.
- Physical interaction studies (FTIR, DSC) confirmed compatibility.
- In vivo studies demonstrated a significantly extended plasma concentration-time profile for febuxostat.
- The optimized tablets met USP standards for hardness and disintegration.
Conclusions:
- Activated charcoal effectively enhances controlled release of febuxostat.
- The developed extended-release febuxostat tablets offer improved bioavailability and patient compliance.
- This formulation presents a cost-effective and promising approach for febuxostat delivery.
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