Formulation and Optimization of Fast Dissolving Tablets of Terbutaline Sulphate by Novel Co-Processing Technique

Abstract

Bronchial asthma demands rapid pharmacological intervention, yet conventional oral tablets of terbutaline sulphate, a widely used ??-adrenergic bronchodilator are limited by slow disintegration and a delayed onset of action that can prove consequential during acute episodes. This study addresses that clinical gap through the formulation and optimization of fast dissolving tablets (FDTs) of terbutaline sulphate using novel co-processed superdisintegrants. Crospovidone and croscarmellose sodium were co-processed via solvent evaporation in varying ratios and incorporated into tablet formulations by direct compression. Three formulations (F1, F2, F3) were prepared with increasing superdisintegrant concentrations and evaluated for pre-compression parameters (angle of repose, bulk density, Carr\'s index, Hausner\'s ratio) and post-compression parameters (hardness, friability, weight variation, drug content, disintegration time, wetting time, and in-vitro dissolution). The optimized formulation, F3, stood out with a disintegration time of just 45 seconds and nearly complete drug release (99%) within 5 minutes, results attributable to the synergistic combination of crospovidone\'s wicking action and croscarmellose sodium\'s swelling capacity, both amplified by the intimate particle-level association achieved through co-processing. Accelerated stability testing (40°C/75% RH, 1 month) confirmed no clinically significant change in drug content or disintegration performance. These findings establish co-processed superdisintegrants as a practical and scalable strategy for developing high-performance FDTs, offering patients with asthma a faster, more accessible, and more effective dosage form.

Introduction

This study focuses on developing fast-dissolving tablets (FDTs) of terbutaline sulphate, a bronchodilator used for asthma and COPD, to overcome limitations of conventional tablets such as slow onset and difficulty swallowing. FDTs dissolve in the mouth without water, enabling rapid drug absorption, which is especially crucial during acute asthma episodes.

A key innovation is the co-processing of superdisintegrants—crospovidone (wicking action) and croscarmellose sodium (swelling action). Co-processing combines them at the sub-particle level, producing a synergistic effect that improves flow, compressibility, disintegration, and uniform drug distribution, outperforming physical mixing.

Methodology:

• Co-processed superdisintegrants were prepared in ratios 1:1 (CPS1), 1:2 (CPS2), 2:1 (CPS3).
• FDTs were formulated via direct compression into 100 mg tablets, with three variations (F1, F2, F3) differing in superdisintegrant concentration.
• Pre-compression parameters (flow, density, Carr’s index) and post-compression parameters (weight, hardness, friability, drug content, thickness) were evaluated.
• Disintegration, wetting, and in-vitro dissolution studies were performed.

Results:

• All formulations showed good flow and mechanical strength.
• Disintegration and wetting times decreased as superdisintegrant concentration increased, with F3 (highest concentration) disintegrating in 45 seconds.
• Dissolution studies showed F3 released 99% of drug within 5 minutes, demonstrating faster onset.

Conclusion

The present study successfully developed fast dissolving tablets of terbutaline sulphate using co-processed superdisintegrants (crospovidone and croscarmellose sodium) by direct compression. The co-processing approach improved flowability and compressibility of the powder blend, ensuring efficient tablet manufacturing. All formulations met pharmacopeial standards for hardness, friability, weight variation, and drug content, confirming good mechanical strength and uniformity. An increase in the concentration of co-processed superdisintegrants significantly enhanced tablet performance. The optimized formulation F3 exhibited the best results, with rapid disintegration (45 seconds), reduced wetting time, and maximum drug release (99% within 5 minutes). This improved performance is attributed to the synergistic effect of crospovidone and croscarmellose sodium, combining wicking and swelling mechanisms to accelerate tablet breakup and dissolution. Stability studies indicated no significant changes in the optimized formulation, confirming its reliability over time. Overall, the study demonstrates that co-processing of superdisintegrants is an effective and practical strategy for improving FDT performance, offering a patient-friendly dosage form with faster onset of action for the management of asthma.

References

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Copyright

Copyright © 2026 Atul Bopche, Dhanraj Vishwakarma, Dhruv Kumar Gupta, Gautam Kumar Verma, Harsh Patel, Harshit Singh, Hemant , Dr. Jagdish C. Rathi. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.