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. 2024 Sep 29;29(19):4629.
doi: 10.3390/molecules29194629.

Development and Evaluation of a Cost-Effective, Carbon-Based, Extended-Release Febuxostat Tablet

Israa Hamid Al-Ani  1 , Mohammad Hailat  2 , Dina J Mohammed  1 , Sina Mahmoud Matalqah  1 , Alaa Azeez Abu Dayah  1 , Bashar J M Majeed  1   3 , Riad Awad  4 , Lorena Filip  5 , Wael Abu Dayyih  6
Affiliations

Development and Evaluation of a Cost-Effective, Carbon-Based, Extended-Release Febuxostat Tablet

Israa Hamid Al-Ani et al. Molecules. .

Abstract

This study outlines the development of a cost-effective, extended-release febuxostat (FEB) tablet using activated charcoal as an adsorbent to enhance drug release. FEB, a BCS Class II drug, presents formulation challenges due to low solubility and high lipophilicity. We evaluated eight formulations with varying FEB-to-charcoal ratios using FTIR and DSC for physical interactions and followed USP standards for overall assessment. The optimal 1:0.25 FEB-to-charcoal ratio demonstrated a consistent 12 h zero-order release pattern. In vivo studies indicated a significantly extended plasma profile compared to immediate-release tablets. The optimal tablets demonstrated acceptable hardness and disintegration times. This innovative approach enhances patient compliance, improves bioavailability, and reduces production costs, offering a promising solution for controlled FEB delivery.

Keywords: FEB; bioavailability; charcoal; extended release; tablet.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Chemical structure of FEB [3].
Figure 2
Figure 2
A chromatogram of FEB shows a retention time (RT) of 3.7 min.
Figure 3
Figure 3
The calibration curve and linearity data of FEB show an R2 of 0.9993 and a linearity equation.
Figure 4
Figure 4
FTIR spectrum of (A): FEB, (B): CHR, and (C): FEB-CHR adsorbate powder showing the absence of the major peaks of the drug in the powder mixture prepared by the trituration method.
Figure 5
Figure 5
Thermogram of FEB (A) showing its melting point at 240 °C. With CHR (B), no peak is observed due to the high melting point, and FEB-CHR (C) adsorbate powder shows a wide broad peak indicative of a physical interaction.
Figure 6
Figure 6
The particle size distribution measurement of FEB-CHR powder shows a single peak with an average particle size of 830 ± 254 nm.
Figure 7
Figure 7
Release profile of the prepared formulations at pH 6.8 using dissolution apparatus II, 50 rpm, and 37 °C. Results show the highest percent of release from F8, which contained FEB:CHR in a ratio of 1:0.25.
Figure 8
Figure 8
Chromatogram of FEB in rat plasma (from linearity test). RT was equal to 1 min.
Figure 9
Figure 9
Plasma level–time profile of FEB in rat plasma of F8 and the reference formula. (A) regular scale and (B) semilog scale.
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