Role of water in the physical stability of solid dosage formulations
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Role of water in the physical stability of solid dosage formulations. / Airaksinen, Sari; Karjalainen, Milja; Shevchenko, Anna; Westermarck, Sari; Leppänen, Ella; Rantanen, Jukka; Yliruusi, Jouko.
In: Journal of Pharmaceutical Sciences, Vol. 94, No. 10, 10.2005, p. 2147-65.Research output: Contribution to journal › Journal article › peer-review
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TY - JOUR
T1 - Role of water in the physical stability of solid dosage formulations
AU - Airaksinen, Sari
AU - Karjalainen, Milja
AU - Shevchenko, Anna
AU - Westermarck, Sari
AU - Leppänen, Ella
AU - Rantanen, Jukka
AU - Yliruusi, Jouko
N1 - Copyright (c) 2005 Wiley-Liss, Inc. and the American Pharmacists Association
PY - 2005/10
Y1 - 2005/10
N2 - The interaction of moisture with pharmaceutical solids is highly crucial to an understanding of water-based processes, for example, manufacturing processes or prediction of solid dosage form stability and shelf life. Both the active pharmaceutical ingredient (API) and excipients in the formulation have different moisture sorption properties that can result in unexpected processing-induced phase transitions and they can affect solid-state phase transitions in the final dosage forms. The character of excipient effects on the stability of formulation. Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The aim of the present study was to investigate the water sorption properties of different excipients, model the sorption isotherms, examine the phase transitions, and identify differences of excipients in solid dosage form stability using dynamic vapor sorption analysis, near-infrared spectroscopy, and X-ray diffraction methods. The thermal processing was carried out with a variable temperature X-ray powder diffractometer to compare the dehydration behavior of wet excipients and evaluate solid-state properties during heating. These results showed that despite some limitations, moisture sorption isotherms of excipients are useful in predicting solid-state stability, interactions at early stages of formulation development, and effects of moisture on physicochemical properties of the final dosage forms.
AB - The interaction of moisture with pharmaceutical solids is highly crucial to an understanding of water-based processes, for example, manufacturing processes or prediction of solid dosage form stability and shelf life. Both the active pharmaceutical ingredient (API) and excipients in the formulation have different moisture sorption properties that can result in unexpected processing-induced phase transitions and they can affect solid-state phase transitions in the final dosage forms. The character of excipient effects on the stability of formulation. Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The aim of the present study was to investigate the water sorption properties of different excipients, model the sorption isotherms, examine the phase transitions, and identify differences of excipients in solid dosage form stability using dynamic vapor sorption analysis, near-infrared spectroscopy, and X-ray diffraction methods. The thermal processing was carried out with a variable temperature X-ray powder diffractometer to compare the dehydration behavior of wet excipients and evaluate solid-state properties during heating. These results showed that despite some limitations, moisture sorption isotherms of excipients are useful in predicting solid-state stability, interactions at early stages of formulation development, and effects of moisture on physicochemical properties of the final dosage forms.
KW - Cellulose
KW - Chemistry, Pharmaceutical
KW - Crystallization
KW - Desiccation
KW - Drug Stability
KW - Excipients
KW - Microscopy, Electron, Scanning
KW - Particle Size
KW - Pharmaceutical Preparations
KW - Phase Transition
KW - Spectroscopy, Near-Infrared
KW - Starch
KW - Temperature
KW - Time Factors
KW - Water
KW - X-Ray Diffraction
U2 - 10.1002/jps.20411
DO - 10.1002/jps.20411
M3 - Journal article
C2 - 16136577
VL - 94
SP - 2147
EP - 2165
JO - Journal of Pharmaceutical Sciences
JF - Journal of Pharmaceutical Sciences
SN - 0022-3549
IS - 10
ER -
ID: 140621813