Towards functional characterization of excipients for oral solid dosage forms using UV-vis imaging. Liberation, release and dissolution
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Towards functional characterization of excipients for oral solid dosage forms using UV-vis imaging. Liberation, release and dissolution. / Li, Zhuoxuan; Sun, Yu; Bar-Shalom, Daniel; Mu, Huiling; Larsen, Susan Weng; Jensen, Henrik; Ostergaard, Jesper.
In: Journal of Pharmaceutical and Biomedical Analysis, Vol. 194, 113789, 2021.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Towards functional characterization of excipients for oral solid dosage forms using UV-vis imaging. Liberation, release and dissolution
AU - Li, Zhuoxuan
AU - Sun, Yu
AU - Bar-Shalom, Daniel
AU - Mu, Huiling
AU - Larsen, Susan Weng
AU - Jensen, Henrik
AU - Ostergaard, Jesper
PY - 2021
Y1 - 2021
N2 - The purpose of this study was to investigate whole-dosage form UV-vis imaging as a potential tool for functional characterization of excipients used in solid oral dosage forms. To this end, tablets (average mass 260.0 mg, 224.5 mg and 222.1 mg) containing theophylline anhydrate (20 % w/w), 1% (w/w) magnesium stearate, and 79 % (w/w) of either microcrystalline cellulose (MCC, Avicel PH 101) or hydroxypropyl methylcellulose (HPMC, Methocel K15 M or K100 M) were prepared as model systems. Drug liberation from tablets was studied in 0.01 M HCl at 37 degrees C using a Sirius SDi2 equipped with a USP IV type flow cell comprising a UV-vis imaging detector operating at 255 nm and 520 nm. The effluent from the flow cell was passed through a downstream spectrophotometer, and UV-vis spectra in the wavelength range 200-800 nm were recorded every 2 min. The erosion and swelling behavior of the MCC tablets and HPMC K15 M and K100 M tablets were visualized in real time. The swelling of HPMC K15 M and K100 M containing tablets was assessed quantitatively as changes in tablet diameter measured at 520 nm, and was clearly distinguished from the swelling of the MCC tablets. Namely, an increment of 2.5 mm in diameter was determined for the HPMC tablets while the MCC tablets increased by 0.5-1 mm in diameter. Gel layers of variable thickness were observed only for the HPMC K15 M and K100 M tablets. In addition, a relatively high initial liberation rate of theophylline was found for the MCC tablets as compared to the HPMC tablets. UV-vis imaging revealed features of liberation not revealed by simply measuring drug concentration in the dissolution media or by visual assessment. It may be sufficiently sensitive to be further developed for functional characterization of excipients and provide insights into drug-excipient interactions likely to be useful in formulation development. (C) 2020 Elsevier B.V. All rights reserved.
AB - The purpose of this study was to investigate whole-dosage form UV-vis imaging as a potential tool for functional characterization of excipients used in solid oral dosage forms. To this end, tablets (average mass 260.0 mg, 224.5 mg and 222.1 mg) containing theophylline anhydrate (20 % w/w), 1% (w/w) magnesium stearate, and 79 % (w/w) of either microcrystalline cellulose (MCC, Avicel PH 101) or hydroxypropyl methylcellulose (HPMC, Methocel K15 M or K100 M) were prepared as model systems. Drug liberation from tablets was studied in 0.01 M HCl at 37 degrees C using a Sirius SDi2 equipped with a USP IV type flow cell comprising a UV-vis imaging detector operating at 255 nm and 520 nm. The effluent from the flow cell was passed through a downstream spectrophotometer, and UV-vis spectra in the wavelength range 200-800 nm were recorded every 2 min. The erosion and swelling behavior of the MCC tablets and HPMC K15 M and K100 M tablets were visualized in real time. The swelling of HPMC K15 M and K100 M containing tablets was assessed quantitatively as changes in tablet diameter measured at 520 nm, and was clearly distinguished from the swelling of the MCC tablets. Namely, an increment of 2.5 mm in diameter was determined for the HPMC tablets while the MCC tablets increased by 0.5-1 mm in diameter. Gel layers of variable thickness were observed only for the HPMC K15 M and K100 M tablets. In addition, a relatively high initial liberation rate of theophylline was found for the MCC tablets as compared to the HPMC tablets. UV-vis imaging revealed features of liberation not revealed by simply measuring drug concentration in the dissolution media or by visual assessment. It may be sufficiently sensitive to be further developed for functional characterization of excipients and provide insights into drug-excipient interactions likely to be useful in formulation development. (C) 2020 Elsevier B.V. All rights reserved.
KW - Dissolution behavior
KW - Dissolution imaging
KW - Drug liberation
KW - Excipient
KW - UV-vis imaging
KW - Whole dosage form
KW - FORMULATION VARIABLES
KW - POLYMER RELEASE
KW - DRUG
KW - HPMC
KW - BIOAVAILABILITY
KW - MATRICES
KW - IMPACT
U2 - 10.1016/j.jpba.2020.113789
DO - 10.1016/j.jpba.2020.113789
M3 - Journal article
C2 - 33298380
VL - 194
JO - Journal of Pharmaceutical and Biomedical Analysis
JF - Journal of Pharmaceutical and Biomedical Analysis
SN - 0731-7085
M1 - 113789
ER -
ID: 257745023