Microcrystallization of indomethacin using a pH-shift method

Sung Tae Kim, Jai Hyun Kwon, Jae Jeong Lee, Chan Wha Kim

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    19 Citations (Scopus)

    Abstract

    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).

    Original languageEnglish
    Pages (from-to)141-150
    Number of pages10
    JournalInternational Journal of Pharmaceutics
    Volume263
    Issue number1-2
    DOIs
    Publication statusPublished - 2003 Sept 16

    Bibliographical note

    Copyright:
    Copyright 2017 Elsevier B.V., All rights reserved.

    Keywords

    • HT-29
    • Indomethacin
    • Microcrystallization
    • pH-shift

    ASJC Scopus subject areas

    • Pharmaceutical Science

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