Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

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

doi:10.1016/j.xphs.2019.01.025

Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

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

^*Corresponding author for this work

1 Citation (Scopus)

Abstract

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 language	English
Journal	Journal of Pharmaceutical Sciences
Volume	108
Issue number	6
Pages (from-to)	2128-2135
Number of pages	8
ISSN	0022-3549
DOIs	https://doi.org/10.1016/j.xphs.2019.01.025
Publication status	Published - 1 Jun 2019

Keywords

absorption enhancers
amorphism
compaction
physicochemical properties
spray drying
tableting

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title = "Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology",

abstract = "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.",

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author = "Weiwei Fan and Aohua Wang and Yue Wu and Water, {Jorrit J.} and Buckley, {Stephen T.} and Lars Hovgaard and Mingshi Yang and Yong Gan",

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AU - Hovgaard, Lars

AU - Yang, Mingshi

AU - Gan, Yong

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Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

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