Aim The current research aimed on the preparation of floating beads, which were then transformed into floating tablets to enhance gastric residence time. Methodology The beads (B1 to B5) were synthesized via the solvent evaporation method and subsequently characterized for Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC), flow properties, entrapment efficiency, percent yield, percent drug loading, floating behaviors, scanning electron microscopy (SEM), The optimized B5 (based on floating behaviors) was directly compressed into floating tablets, which were characterized for their physical and chemical properties, floating behaviors, and drug release mechanisms and compared with marketed products. Adult male rabbits were given B5 and a reference preparation to evaluate floating behaviors and pharmacokinetic parameters. Results The microbeads demonstrated free-flowing properties, and the findings adhered to USP standards. The particle size varied from 10 ± 0.16 to 10 ± 0.21 µm. The entrapment efficiency ranged from 72.42 ± 0.08 to 85.22 ± 0.12%. The percent yield was measured at 61.19 ± 0.02 to 67.52 ± 0.72%. The percent drug loading varied between 30.26 ± 0.25 and 38.29 ± 0.09%. The floating lag time ranged from 0.4 ± 0.22 to 1.0 ± 0.29 min, whereas the total floating time was recorded as 10.0 ± 0.16 to 12.5 ± 0.14 h. The surface morphology displayed roughness and irregularity. FTIR and DSC analyses validated that the drug and ingredients were not interacting with each other. The tablets' physical characteristics were found to comply with USP limits. B5 exhibited prolonged drug release rates for 20 h in 0.1 N HCl, achieving complete release in phosphate buffer at pH 6.8. The drug was released via pseudo-zero-order kinetics, characterized by swelling or erosion and non-Fickian mechanisms. The in vivo buoyancy of B5 was quantified at 20 ± 0.07 h. The pharmacokinetic parameters for B5 are as follows: tmax 5.03 ± 1.5 h, Cmax 186 ± 0.59 µg/mL, T1/2 10.0 ± 0.52 h, AUCo 4832.1 ± 1.34 µg·h/mL, AUCo-inf 6438 ± 0.42 µg·h/mL, MRTo-24 14.65 h, and Cl 0.023 mL/min. The pharmacokinetic parameters for the reference tablets are detailed below: Tmax was 1.3 ± 0.06 h, Cmax was 185 ± 0.24 µg/mL, T1/2 was 5.65 ± 1.94 h, AUCo was 38,581 ± 1.15 µg.h/mL, AUCo-inf was 4347 ± 1.24 µg.h/mL, MRT o-24 was 8.83 h, and Cl was 0.021 mL/min. Conclusion This study concludes that floating tablets can improve therapeutic effects by extending gastric residence time.

Fabrication and In-Vitro and In-Vivo Assessment of Levofloxacin Beads Loaded Floating Tablets to improve Gastric Residence Time

期刊论文
发表日期：

2026年2月27日

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Muhammad Israr,
Kamran Ahmad Khan,
Ashfaq Ahmad,
Kifayat Ullah Shah,
Naveed Ullah,
Naheed Akhtar

摘要

Aim

The current research aimed on the preparation of floating beads, which were then transformed into floating tablets to enhance gastric residence time.

Methodology

The beads (B1 to B5) were synthesized via the solvent evaporation method and subsequently characterized for Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC), flow properties, entrapment efficiency, percent yield, percent drug loading, floating behaviors, scanning electron microscopy (SEM), The optimized B5 (based on floating behaviors) was directly compressed into floating tablets, which were characterized for their physical and chemical properties, floating behaviors, and drug release mechanisms and compared with marketed products. Adult male rabbits were given B5 and a reference preparation to evaluate floating behaviors and pharmacokinetic parameters.

Results

The microbeads demonstrated free-flowing properties, and the findings adhered to USP standards. The particle size varied from 10 ± 0.16 to 10 ± 0.21 µm. The entrapment efficiency ranged from 72.42 ± 0.08 to 85.22 ± 0.12%. The percent yield was measured at 61.19 ± 0.02 to 67.52 ± 0.72%. The percent drug loading varied between 30.26 ± 0.25 and 38.29 ± 0.09%. The floating lag time ranged from 0.4 ± 0.22 to 1.0 ± 0.29 min, whereas the total floating time was recorded as 10.0 ± 0.16 to 12.5 ± 0.14 h. The surface morphology displayed roughness and irregularity. FTIR and DSC analyses validated that the drug and ingredients were not interacting with each other. The tablets' physical characteristics were found to comply with USP limits. B5 exhibited prolonged drug release rates for 20 h in 0.1 N HCl, achieving complete release in phosphate buffer at pH 6.8. The drug was released via pseudo-zero-order kinetics, characterized by swelling or erosion and non-Fickian mechanisms. The in vivo buoyancy of B5 was quantified at 20 ± 0.07 h. The pharmacokinetic parameters for B5 are as follows: t_max 5.03 ± 1.5 h, C_max 186 ± 0.59 µg/mL, T_1/2 10.0 ± 0.52 h, AUC_o 4832.1 ± 1.34 µg·h/mL, AUC_o-inf 6438 ± 0.42 µg·h/mL, MRT_o-24 14.65 h, and Cl 0.023 mL/min. The pharmacokinetic parameters for the reference tablets are detailed below: Tmax was 1.3 ± 0.06 h, C_max was 185 ± 0.24 µg/mL, T_1/2 was 5.65 ± 1.94 h, AUC_o was 38,581 ± 1.15 µg.h/mL, AUC_o-inf was 4347 ± 1.24 µg.h/mL, MRT _o-24 was 8.83 h, and Cl was 0.021 mL/min.

Conclusion

This study concludes that floating tablets can improve therapeutic effects by extending gastric residence time.