Effect of moisture sorption on the performance of crospovidone

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• 作者：Tze Ning Hiew^a ; Nur Atiqah Binte Johan^a ; Parind Mahendrakumar Desai^b ; Siang Meng Chua^c ; Zhi Hui Loh^d ; Paul Wan Sia Heng^a ; ^{phapaulh@nus.edu.sg" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Crospovidone ; Disintegration ; Water activity ; Relative humidity ; Wetting ; Moisture sorption isotherm
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：30 November 2016
• 年：2016
• 卷：514
• 期：1
• 页码：322-331
• 全文大小：1346 K

文摘

Crospovidone is a commonly used tablet disintegrant. However, the synthetic disintegrant has been known to be hygroscopic and high moisture content in crospovidone used could exert deleterious effects on tablets formulated with it. The objective of this study was to elicit a better understanding between crospovidone-water interaction and its effect on disintegrant performance. Moisture sorption and desorption isotherms were obtained together with the enthalpy of immersion. Crospovidone samples stored at four relative humidities were used to formulate tablets and the resultant tablets were evaluated for their mechanical, dimensional and disintegratability attributes. Analyses of the moisture sorption isotherms indicated that externally adsorbed moisture accounted for the bulk of the total moisture content in crospovidone, with minimal amount of moisture absorbed intramolecularly. Enthalpy of immersion became less exothermic with crospovidone samples stored at increasing storage humidity. Correspondingly, improvement in disintegration time became less pronounced. This was postulated to be a consequence of premature wetting of the particle surfaces by externally adsorbed moisture. High humidity was also detrimental to tablet hardness and thickness. In conclusion, the impact of moisture sorption during storage by excipients such as crospovidone could be better understood by the appreciation of crospovidone-water interaction and its consequence on tablet quality.