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Background <p>This study developed and evaluated fast-release tablets of Linezolid to achieve rapid disintegration, enhanced dissolution, and improved therapeutic outcomes. Linezolid, an oxazolidinone antibiotic prescribed for multidrug-resistant Gram-positive bacterial infections, exhibits a slow onset of action in conventional dosage forms.</p> Methods <p>Fast-release tablets were prepared using wet granulation with superdisintegrants Kyron T-314 and Kyron T-316 in varying ratios (KP1–KP8). They evaluated tablet weight variation, hardness, friability, thickness, wetting time, disintegration time, drug content, and in vitro drug release studies.</p> Results and Discussion <p>FTIR (Fourier Transform Infrared Spectroscopy) and DSC (Differential Scanning Calorimetry) analyses indicated no significant drug-excipient incompatibilities and revealed partial conversion of Linezolid to an amorphous form, facilitating faster dissolution. The optimized formulation (KP8) showed rapid disintegration (41.3 ± 1.2&#xa0;s), high drug content (99.5 ± 0.8%), and the highest cumulative drug release (97.70 ± 1.3% within 90&#xa0;s). Drug release kinetics were best described by the Korsmeyer–Peppas and Higuchi models, suggesting a diffusion-controlled non-Fickian mechanism. Stability studies conducted for six months under accelerated conditions (40 ± 2&#xa0;°C/75 ± 5% RH) (Relative Humidity) demonstrated consistent physicochemical parameters and dissolution behavior. In vivo evaluation using the carrageenan-induced paw edema model confirmed measurable anti-inflammatory effects (2.79% inhibition at 3&#xa0;h), supporting potential secondary immunomodulatory activity in addition to antibacterial effects.</p> Conclusion <p>Fast-release Linezolid tablets offer a promising alternative to conventional formulations, providing a rapid onset, improved patient compliance, and potential benefits in the management of acute infections.</p>

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Formulation and Characterization of Rapidly Disintegrating Linezolid Tablets for Enhanced Oral Delivery

  • 期刊论文

  • 发表日期：

    2026年5月7日

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  • Km Kalpana,
  • Arvind Raghav,
  • Prashant Upadhyay,
  • Km Anjali

摘要

Background

This study developed and evaluated fast-release tablets of Linezolid to achieve rapid disintegration, enhanced dissolution, and improved therapeutic outcomes. Linezolid, an oxazolidinone antibiotic prescribed for multidrug-resistant Gram-positive bacterial infections, exhibits a slow onset of action in conventional dosage forms.

Methods

Fast-release tablets were prepared using wet granulation with superdisintegrants Kyron T-314 and Kyron T-316 in varying ratios (KP1–KP8). They evaluated tablet weight variation, hardness, friability, thickness, wetting time, disintegration time, drug content, and in vitro drug release studies.

Results and Discussion

FTIR (Fourier Transform Infrared Spectroscopy) and DSC (Differential Scanning Calorimetry) analyses indicated no significant drug-excipient incompatibilities and revealed partial conversion of Linezolid to an amorphous form, facilitating faster dissolution. The optimized formulation (KP8) showed rapid disintegration (41.3 ± 1.2 s), high drug content (99.5 ± 0.8%), and the highest cumulative drug release (97.70 ± 1.3% within 90 s). Drug release kinetics were best described by the Korsmeyer–Peppas and Higuchi models, suggesting a diffusion-controlled non-Fickian mechanism. Stability studies conducted for six months under accelerated conditions (40 ± 2 °C/75 ± 5% RH) (Relative Humidity) demonstrated consistent physicochemical parameters and dissolution behavior. In vivo evaluation using the carrageenan-induced paw edema model confirmed measurable anti-inflammatory effects (2.79% inhibition at 3 h), supporting potential secondary immunomodulatory activity in addition to antibacterial effects.

Conclusion

Fast-release Linezolid tablets offer a promising alternative to conventional formulations, providing a rapid onset, improved patient compliance, and potential benefits in the management of acute infections.