Real-time dissolution behavior of furosemide in biorelevant media as determined by UV imaging
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Real-time dissolution behavior of furosemide in biorelevant media as determined by UV imaging. / Gordon, Sarah; Naelapää, Kaisa; Rantanen, Jukka; Selen, Arzu; Müllertz, Anette; Østergaard, Jesper.
I: Pharmaceutical Development and Technology, Bind 18, Nr. 6, 2013, s. 1407-16.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Real-time dissolution behavior of furosemide in biorelevant media as determined by UV imaging
AU - Gordon, Sarah
AU - Naelapää, Kaisa
AU - Rantanen, Jukka
AU - Selen, Arzu
AU - Müllertz, Anette
AU - Østergaard, Jesper
PY - 2013
Y1 - 2013
N2 - The potential of UV imaging as a new small scale flow-through dissolution testing platform and its ability to incorporate biorelevant media was tested. Furosemide was utilized as a model poorly soluble drug, and dissolution media simulating conditions in the small intestine (5/1.25 mM and 40/10 mM bile salt/phospholipid, pH 6.5) together with corresponding blank buffer were employed. Dissolution rates as a function of flow rate (0.2-1.0 mL/min) were determined directly from UV images, and by analysis of collected effluent using UV spectrophotometry. A good agreement in dissolution rates was observed, however repeatability of data based on measurement of collected effluent was superior to that obtained by UV imaging in the utilized prototypic flow cell. Both methods indicated that biorelevant media did not markedly increase the dissolution rate of furosemide as compared to buffer. Qualitatively, UV images indicated that uncontrolled swelling/precipitation of furosemide on the compact surface was occurring in some samples. In situ Raman spectroscopy together with X-ray diffraction analysis confirmed that the observations were not due to a solid form transformation of furosemide. The presented results highlight the complementary features of the utilized techniques and, in particular, the detailed information related to dissolution behavior which can be achieved by UV imaging.
AB - The potential of UV imaging as a new small scale flow-through dissolution testing platform and its ability to incorporate biorelevant media was tested. Furosemide was utilized as a model poorly soluble drug, and dissolution media simulating conditions in the small intestine (5/1.25 mM and 40/10 mM bile salt/phospholipid, pH 6.5) together with corresponding blank buffer were employed. Dissolution rates as a function of flow rate (0.2-1.0 mL/min) were determined directly from UV images, and by analysis of collected effluent using UV spectrophotometry. A good agreement in dissolution rates was observed, however repeatability of data based on measurement of collected effluent was superior to that obtained by UV imaging in the utilized prototypic flow cell. Both methods indicated that biorelevant media did not markedly increase the dissolution rate of furosemide as compared to buffer. Qualitatively, UV images indicated that uncontrolled swelling/precipitation of furosemide on the compact surface was occurring in some samples. In situ Raman spectroscopy together with X-ray diffraction analysis confirmed that the observations were not due to a solid form transformation of furosemide. The presented results highlight the complementary features of the utilized techniques and, in particular, the detailed information related to dissolution behavior which can be achieved by UV imaging.
KW - Buffers
KW - Furosemide
KW - Solubility
KW - Spectrophotometry, Ultraviolet
KW - Spectrum Analysis, Raman
KW - Technology, Pharmaceutical
KW - X-Ray Diffraction
U2 - 10.3109/10837450.2012.737808
DO - 10.3109/10837450.2012.737808
M3 - Journal article
C2 - 23136844
VL - 18
SP - 1407
EP - 1416
JO - Pharmaceutical Development and Technology
JF - Pharmaceutical Development and Technology
SN - 1083-7450
IS - 6
ER -
ID: 104835797