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Although polymers can prevent the crystallization of glassy drugs in amorphous solid dispersions, their stabilization mechanism requires further clarification for an efficient formulation design. This study examined the impact of adding trace amounts (2 or 5 w/w %) of vinylpyrrolidone−vinyl acetate copolymer (PVPVA) on the physical stability of celecoxib (CEL) glass using differential scanning calorimetry and broadband dielectric spectroscopy. Long-term isothermal crystallization studies from 35 to 60 °C revealed that CEL glass was significantly stabilized by the addition of trace amounts of PVPVA. Its stabilization was attributed to the effect of PVPVA on the nucleation process rather than on crystal growth. The addition of PVPVA slowed down the α-relaxation of CEL, whereas it accelerated Johari−Goldstein relaxation. Moreover, the addition of PVPVA effectively slowed down γ- and δ-relaxations. Of these, suppression of γ-relaxation mobility had the most important effect, as it is related to the formation of hydrogen bonding between CEL and PVPVA molecules to inhibit nucleation. Moreover, the change in molecular cooperativity of the CEL glass upon adding PVPVA contributed to the inhibition of nuclei formation due to the decreased nucleation temperature. This study provides detailed insights into the physical stabilization mechanisms of glass using polymeric excipients.

権利情報:

• Creative Commons BY Attribution 4.0 International
  

キーワード: glass, polymeric excipients, PVPVA, crystallization, broadband dielectric spectroscopy, differential scanning calorimetry

刊行年月日: 2026-01-05

出版者: American Chemical Society (ACS)

掲載誌:

• Molecular Pharmaceutics (ISSN: 15438384) vol. 23 issue. 1 p. 280-292

研究助成金:

原稿種別: 出版者版 (Version of record)

MDR DOI:

公開URL: https://doi.org/10.1021/acs.molpharmaceut.5c00934

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更新時刻: 2026-04-30 12:01:11 +0900

MDRでの公開時刻: 2026-08-19 16:24:48 +0900