Role of excipients in hydrate formation kinetics of theophylline in wet masses studied by near-infrared spectroscopy
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Role of excipients in hydrate formation kinetics of theophylline in wet masses studied by near-infrared spectroscopy. / Jørgensen, Anna C; Airaksinen, Sari; Karjalainen, Milja; Luukkonen, Pirjo; Rantanen, Jukka; Yliruusi, Jouko.
In: European Journal of Pharmaceutical Sciences, Vol. 23, No. 1, 09.2004, p. 99-104.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Role of excipients in hydrate formation kinetics of theophylline in wet masses studied by near-infrared spectroscopy
AU - Jørgensen, Anna C
AU - Airaksinen, Sari
AU - Karjalainen, Milja
AU - Luukkonen, Pirjo
AU - Rantanen, Jukka
AU - Yliruusi, Jouko
PY - 2004/9
Y1 - 2004/9
N2 - Hydrate formation is a phase transition, which can occur during wet granulation. This kind of processing-induced transformation (PIT) can influence the quality of a finished product. The aim of the study was to investigate the effect of excipients on the kinetics of hydrate formation in wet masses. Anhydrous theophylline was chosen as the hydrate-forming model drug compound and two excipients, silicified microcrystalline cellulose (SMCC) and alpha-lactose monohydrate, with different water absorbing properties, were used in formulation. An early stage of wet massing was studied with anhydrous theophylline and its 1:1 (w/w) mixtures with alpha-lactose monohydrate and SMCC with 0.1g/g of purified water. The changes in the state of water were monitored using near-infrared spectroscopy, and the conversion of the crystal structure was verified using X-ray powder diffraction (XRPD). SMCC decreased the hydrate formation rate by absorbing water, but did not inhibit it. The results suggest that alpha-lactose monohydrate slightly increased the hydrate formation rate in comparison with a mass comprising only anhydrous theophylline.
AB - Hydrate formation is a phase transition, which can occur during wet granulation. This kind of processing-induced transformation (PIT) can influence the quality of a finished product. The aim of the study was to investigate the effect of excipients on the kinetics of hydrate formation in wet masses. Anhydrous theophylline was chosen as the hydrate-forming model drug compound and two excipients, silicified microcrystalline cellulose (SMCC) and alpha-lactose monohydrate, with different water absorbing properties, were used in formulation. An early stage of wet massing was studied with anhydrous theophylline and its 1:1 (w/w) mixtures with alpha-lactose monohydrate and SMCC with 0.1g/g of purified water. The changes in the state of water were monitored using near-infrared spectroscopy, and the conversion of the crystal structure was verified using X-ray powder diffraction (XRPD). SMCC decreased the hydrate formation rate by absorbing water, but did not inhibit it. The results suggest that alpha-lactose monohydrate slightly increased the hydrate formation rate in comparison with a mass comprising only anhydrous theophylline.
KW - Bronchodilator Agents
KW - Cellulose
KW - Chemistry, Pharmaceutical
KW - Excipients
KW - Kinetics
KW - Lactose
KW - Solubility
KW - Spectroscopy, Near-Infrared
KW - Theophylline
KW - X-Ray Diffraction
U2 - 10.1016/j.ejps.2004.06.001
DO - 10.1016/j.ejps.2004.06.001
M3 - Journal article
C2 - 15324927
VL - 23
SP - 99
EP - 104
JO - Norvegica Pharmaceutica Acta
JF - Norvegica Pharmaceutica Acta
SN - 0928-0987
IS - 1
ER -
ID: 140622518