Influence of Glass Forming Ability on the Physical Stability of Supersaturated Amorphous Solid Dispersions
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Influence of Glass Forming Ability on the Physical Stability of Supersaturated Amorphous Solid Dispersions. / Blaabjerg, Lasse Ingerslev; Bulduk, Bulut; Lindenberg, Eleanor; Löbmann, Korbinian; Rades, Thomas; Grohganz, Holger.
In: Journal of Pharmaceutical Sciences, Vol. 108, No. 8, 01.01.2019, p. 2561-2569.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Influence of Glass Forming Ability on the Physical Stability of Supersaturated Amorphous Solid Dispersions
AU - Blaabjerg, Lasse Ingerslev
AU - Bulduk, Bulut
AU - Lindenberg, Eleanor
AU - Löbmann, Korbinian
AU - Rades, Thomas
AU - Grohganz, Holger
PY - 2019/1/1
Y1 - 2019/1/1
N2 - In this study, the influence of the glass-forming ability (GFA) of a drug on its physical stability in a supersaturated solid dispersion was investigated. Nine drugs were classified according to their GFA using their respective critical cooling rate. Their respective solubility in poly(vinylpyrrolidone-co-vinyl acetate) 6:4 (PVPVA64) was predicted using the melting point depression method based on the Flory-Huggins lattice theory. Supersaturated amorphous solid dispersions at a level of 25% w/w drug above saturation solubility in the polymer were prepared by film-casting, and their respective physical stability at temperatures of 10°C or 20°C above or below their respective T g (dry conditions) was monitored by the use of polarized light microscopy. This study showed that drugs with good GFA (class 3) on average have higher physical stability in supersaturated amorphous solid dispersion compared to drug with modest GFA (class 2), which in turn have higher physical stability in supersaturated amorphous solid dispersion than drugs with poor GFA (class 1). These results indicate that the GFA of a drug and its physical stability in a supersaturated amorphous solid dispersion stored at a temperature above or below its T g are correlated.
AB - In this study, the influence of the glass-forming ability (GFA) of a drug on its physical stability in a supersaturated solid dispersion was investigated. Nine drugs were classified according to their GFA using their respective critical cooling rate. Their respective solubility in poly(vinylpyrrolidone-co-vinyl acetate) 6:4 (PVPVA64) was predicted using the melting point depression method based on the Flory-Huggins lattice theory. Supersaturated amorphous solid dispersions at a level of 25% w/w drug above saturation solubility in the polymer were prepared by film-casting, and their respective physical stability at temperatures of 10°C or 20°C above or below their respective T g (dry conditions) was monitored by the use of polarized light microscopy. This study showed that drugs with good GFA (class 3) on average have higher physical stability in supersaturated amorphous solid dispersion compared to drug with modest GFA (class 2), which in turn have higher physical stability in supersaturated amorphous solid dispersion than drugs with poor GFA (class 1). These results indicate that the GFA of a drug and its physical stability in a supersaturated amorphous solid dispersion stored at a temperature above or below its T g are correlated.
KW - amorphous
KW - crystallization
KW - formulation
KW - glass
KW - physical stability
KW - solid dispersion
KW - solid state
KW - solubility
U2 - 10.1016/j.xphs.2019.02.028
DO - 10.1016/j.xphs.2019.02.028
M3 - Journal article
C2 - 30878513
AN - SCOPUS:85063762169
VL - 108
SP - 2561
EP - 2569
JO - Journal of Pharmaceutical Sciences
JF - Journal of Pharmaceutical Sciences
SN - 0022-3549
IS - 8
ER -
ID: 217694636