The Effect of Croscarmellose Sodium and Crospovidone Superdisintegrants on Improving Disintegration Times of a Pediatric Oral Tablet Formulation

Purpose. Improve the disintegration times of an oral disintegration tablet intended for pediatric administration using different classes of superdisintegrants. Background: The lack of commercially available pediatric oral sedative medications has limited clinician’s options to overcome administration challenges and provide proper preanesthetic sedation to children. Rapidly disintegrating oral tablets (ODTs) offer a fast, convenient, and pediatric accepted option to delivering sedatives when they disintegrate in the mouth within 30 seconds. We believe that a tablet containing a superdisintegrant with exceptional swelling and wicking properties can be optimized for rapid disintegration fulfilling this fast administration requirement. Methods: Three ODT formulations were made by adding a fixed amount of superdisintegrant with other excipients and compressed into tablets having a total weight of 100 mg. The first formula (FM1) used croscarmellose sodium (Ac-Di-Sol) as the superdisintegrant. The remaining two formulations were comprised of two separate crospovidone grades differentiated by particle sizes 110-140 μm (PVP XL) and 25-40 μm (PVP XL 10), FM2 and FM3 respectively. All ODT formulations were evaluated and characterized for weight variation, hardness, friability, and wetting time using standard methods. A validated disintegration test for rapidly disintegrating tablets was also used for determining disintegration times. Results: Among the tested formulations with superdisintegrants, FM2 showed the fastest disintegration time. Furthermore, this tablet formulation resulted in the least friability despite possessing the lowest hardness. FM3 had comparable disintegration times to FM2, showing 4 seconds longer but still within the 30 secs. ODT parameters. FM1 containing croscarmellose sodium resulted in the greatest disintegration time and more than twice that of FM2. Conclusion: Only formulations containing crospovidone superdisintegrants resulted in rapid disintegration times less than 30 seconds. However, further optimization of these tablet formulations are needed to address additional critical tablet formulation properties. This will ultimately lead to achieving a fast, convenient, and pediatric accepted dosage form efficiently delivering preanesthetic sedatives. Grant: This study was funded by NSU HPD Grant #334604.