Microcrystallization of indomethacin using a pH-shift method

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

Research output: Contribution to journalArticle

16 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 Sep 16

Fingerprint

Indomethacin
Powders
X-Ray Diffraction
Phase-Contrast Microscopy
HT29 Cells
Differential Scanning Calorimetry
Fourier Transform Infrared Spectroscopy
Electron Scanning Microscopy
Colonic Neoplasms
Freezing
Anti-Inflammatory Agents
Temperature
Pharmaceutical Preparations

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Microcrystallization of indomethacin using a pH-shift method. / Kim, Sung Tae; Kwon, Jai Hyun; Lee, Jae Jeong; Kim, Chan Wha.

In: International Journal of Pharmaceutics, Vol. 263, No. 1-2, 16.09.2003, p. 141-150.

Research output: Contribution to journalArticle

Kim, Sung Tae ; Kwon, Jai Hyun ; Lee, Jae Jeong ; Kim, Chan Wha. / Microcrystallization of indomethacin using a pH-shift method. In: International Journal of Pharmaceutics. 2003 ; Vol. 263, No. 1-2. pp. 141-150.
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