Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process

Junsung Park, Hee Jun Park, Wonkyung Cho, Kwang Ho Cha, Young Shin Kang, Sung Joo Hwang

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.

Original languageEnglish
Pages (from-to)239-245
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume396
Issue number1-2
DOIs
Publication statusPublished - 2010 Aug 1

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cefdinir
Solubility
Pharmaceutical Preparations
Particle Size
Needles
Hot Temperature

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Park, Junsung ; Park, Hee Jun ; Cho, Wonkyung ; Cha, Kwang Ho ; Kang, Young Shin ; Hwang, Sung Joo. / Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process. In: International Journal of Pharmaceutics. 2010 ; Vol. 396, No. 1-2. pp. 239-245.
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abstract = "The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.",
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Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process. / Park, Junsung; Park, Hee Jun; Cho, Wonkyung; Cha, Kwang Ho; Kang, Young Shin; Hwang, Sung Joo.

In: International Journal of Pharmaceutics, Vol. 396, No. 1-2, 01.08.2010, p. 239-245.

Research output: Contribution to journalArticle

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AU - Hwang, Sung Joo

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AB - The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.

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