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Purpose <p>Tablet sticking and film surface formation upon compaction of clopidogrel bisulfate (CB) are related to the occurrence of sintering, in which particles are fused as a result of pressure in tablet compaction. Sintering might increase tablet strength, but it also prolongs tablet disintegration. Mixing CB with a disintegrant could reduce the sintering effect and enhance tablet disintegration. Yet, the mechanism by which the disintegrant could overcome sticking is still unclear. Three disintegrants were investigated: starch, partially pregelatinized maize starch (PPS), and croscarmellose sodium (CCS).</p> Methods <p>Three ratios of CB/disintegrant were prepared (90/10, 85/15, and 80/20 w/w) to produce an 800&#xa0;mg tablet with a diameter of 14&#xa0;mm, and each was compacted at compaction forces of 10,000&#xa0;N and 15,000&#xa0;N. Visual observation, tablet structure examination by SEM and XRD, tablet tensile strength, friability, and disintegration were evaluated.</p> Results <p>SEM results showed that CB underwent sintering only on its compacted surface. At 10,000&#xa0;N, CB/starch and CB/CCS 80/20 did not show sticking, but all tablets failed to pass friability test. At 15,000&#xa0;N, no tablet sticking was observed at any ratio of CB/CCS and friability was less than 2%.</p> Conclusion <p>CCS was superior in reducing tablet sticking compared to starch and PPS. The variability in particle sizes and shapes of CCS enables it to fill the void surrounding CB particles, in conjunction with its good tabletability, hence it could hinder particle fusion of CB. Yet, a higher compaction pressure or a combination with other excipients is still required to increase tablet tensile strength and reduce tablet friability.</p>

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Understanding the Role of Disintegrant in Resolving the Sticking of Clopidogrel Bisulfate Tablet

  • 期刊论文

  • 发表日期：

    2025年11月25日

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  • Maria Lucia Ardhani Dwi Lestari,
  • Nurul Hijrayanti,
  • Dwi Setyawan

摘要

Purpose

Tablet sticking and film surface formation upon compaction of clopidogrel bisulfate (CB) are related to the occurrence of sintering, in which particles are fused as a result of pressure in tablet compaction. Sintering might increase tablet strength, but it also prolongs tablet disintegration. Mixing CB with a disintegrant could reduce the sintering effect and enhance tablet disintegration. Yet, the mechanism by which the disintegrant could overcome sticking is still unclear. Three disintegrants were investigated: starch, partially pregelatinized maize starch (PPS), and croscarmellose sodium (CCS).

Methods

Three ratios of CB/disintegrant were prepared (90/10, 85/15, and 80/20 w/w) to produce an 800 mg tablet with a diameter of 14 mm, and each was compacted at compaction forces of 10,000 N and 15,000 N. Visual observation, tablet structure examination by SEM and XRD, tablet tensile strength, friability, and disintegration were evaluated.

Results

SEM results showed that CB underwent sintering only on its compacted surface. At 10,000 N, CB/starch and CB/CCS 80/20 did not show sticking, but all tablets failed to pass friability test. At 15,000 N, no tablet sticking was observed at any ratio of CB/CCS and friability was less than 2%.

Conclusion

CCS was superior in reducing tablet sticking compared to starch and PPS. The variability in particle sizes and shapes of CCS enables it to fill the void surrounding CB particles, in conjunction with its good tabletability, hence it could hinder particle fusion of CB. Yet, a higher compaction pressure or a combination with other excipients is still required to increase tablet tensile strength and reduce tablet friability.