TY - JOUR
T1 - Microcrystallization of indomethacin using a pH-shift method
AU - Kim, Sung Tae
AU - Kwon, Jai Hyun
AU - Lee, Jae Jeong
AU - Kim, Chan Wha
N1 - Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.
PY - 2003/9/16
Y1 - 2003/9/16
N2 - This study developed a microcrystallization process for indomethacin, a nonsteroidal anti-inflammatory drug (NSAID), using a pH-shift method in aqueous solution. The physicochemical properties of the microcrystals produced were similar to those of the standard crystalline powder in X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR) analyses, except for a lower XRD peak height and a slightly lower melting temperature (Tm) (1.5°C). Phase contrast microscopy and scanning electron microscopy (SEM) showed that the indomethacin microcrystals were plate-like with a uniform size distribution (mean diameter=10.4±0.4μm). In the initial phase, the dissolution rate of the indomethacin microcrystals was about 2.2 times higher than that of the standard crystalline powder. The biological activity of the indomethacin microcrystals was about 20% higher than that of the standard crystalline powder in their ability to inhibit the proliferation of colon cancer cells (HT-29).
AB - This study developed a microcrystallization process for indomethacin, a nonsteroidal anti-inflammatory drug (NSAID), using a pH-shift method in aqueous solution. The physicochemical properties of the microcrystals produced were similar to those of the standard crystalline powder in X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR) analyses, except for a lower XRD peak height and a slightly lower melting temperature (Tm) (1.5°C). Phase contrast microscopy and scanning electron microscopy (SEM) showed that the indomethacin microcrystals were plate-like with a uniform size distribution (mean diameter=10.4±0.4μm). In the initial phase, the dissolution rate of the indomethacin microcrystals was about 2.2 times higher than that of the standard crystalline powder. The biological activity of the indomethacin microcrystals was about 20% higher than that of the standard crystalline powder in their ability to inhibit the proliferation of colon cancer cells (HT-29).
KW - HT-29
KW - Indomethacin
KW - Microcrystallization
KW - pH-shift
UR - http://www.scopus.com/inward/record.url?scp=0042884302&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0042884302&partnerID=8YFLogxK
U2 - 10.1016/S0378-5173(03)00358-2
DO - 10.1016/S0378-5173(03)00358-2
M3 - Article
C2 - 12954189
AN - SCOPUS:0042884302
SN - 0378-5173
VL - 263
SP - 141
EP - 150
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -