title: Effect of moisture sorption on the performance of crospovidone.
abstract: 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.
authors.affiliation: GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
authors.forename: Tze Ning
authors.initials: TN
authors.lastname: Hiew
authors.affiliation: GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
authors.forename: Nur Atiqah Binte
authors.initials: NAB
authors.lastname: Johan
authors.affiliation: Novartis-MIT Center for Continuous Manufacturing, Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
authors.forename: Parind Mahendrakumar
authors.initials: PM
authors.lastname: Desai
authors.affiliation: Meggle Singapore, 45 Jalan Pemimpin, #06-00 Foo Wah Industrial Building, Singapore 577197, Singapore.
authors.forename: Siang Meng
authors.initials: SM
authors.lastname: Chua
authors.affiliation: Technical Development, Glaxo Wellcome Manufacturing Pte. Ltd, 1 Pioneer Sector 1, Singapore 628413, Singapore.
authors.forename: Zhi Hui
authors.initials: ZH
authors.lastname: Loh
authors.affiliation: GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore. Electronic address: phapaulh@nus.edu.sg.
authors.forename: Paul Wan Sia
authors.initials: PWS
authors.lastname: Heng
mesh_terms: D000327:Adsorption; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005079:Excipients / Q000737:chemistry; D006244:Hardness; D006813:Humidity; D011205:Povidone / Q000737:chemistry*; D013607:Tablets / Q000737:chemistry; D014867:Water / Q000737:chemistry*
chemical_list: D005079:Excipients; D013607:Tablets; D014867:Water; D011205:Povidone
keywords: Crospovidone; Disintegration; Moisture sorption isotherm; Relative humidity; Water activity; Wetting