Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

Research output: Contribution to journalJournal articleResearchpeer-review

Weiwei Fan, Aohua Wang, Yue Wu, Jorrit J. Water, Stephen T. Buckley, Lars Hovgaard, Mingshi Yang, Yong Gan

Absorption enhancers are often a major component of solid oral peptide formulations as compared to the active pharmaceutical ingredient and excipients. This commonly results in poor tabletability that is hard to mitigate in direct compaction by addition of small amounts of excipients. To improve the tabletability of bulky absorption enhancers, the model absorption enhancers, sodium cholate and deoxycholic acid, were co–spray-dried with hydroxypropyl methylcellulose E5, where the percentage of absorption enhancers was not lower than 90% (w/w). The physicochemical properties of the resulting powders were assessed by laser diffraction, scanning electron microscopy, X-ray powder diffraction, thermogravimetric analysis, and differential scanning calorimetry. The powders were compressed into tablets, and the tabletability was evaluated. Co–spray drying with 10% of hydroxypropyl methylcellulose significantly improved the tabletability of the both absorption enhancers. Moreover, it was demonstrated that small particle size and amorphous state rather than high moisture content contributed to the improved tabletability of the spray-dried powders. The study suggests that spray drying technology can be promising to overcome the poor tabletability of oral peptide formulation consisting of large amounts of absorption enhancers.

Original languageEnglish
JournalJournal of Pharmaceutical Sciences
Volume108
Issue number6
Pages (from-to)2128-2135
Number of pages8
ISSN0022-3549
DOIs
Publication statusPublished - 1 Jun 2019

    Research areas

  • absorption enhancers, amorphism, compaction, physicochemical properties, spray drying, tableting

ID: 221825240