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KMID : 0380020040190040321
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Korean Journal of Biotechnology and Bioengineering
2004 Volume.19 No. 4 p.321 ~ p.326
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Preparation of Microparticulate Itraconazole/Hydroxypropyl-β-cyclodextrin Inclusion Complexes Using a Supercritical Anti-Solvent [SAS] Process
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Lee Sang-Yoon
Kim Jung-Kyu
Kim Woo-Sik
Ryu Jong-Hoon
Lim Kyo-Bin
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Abstract
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Microparticles of an inclusion complex between itraconazole and 2-hydroxypropyl--cyclodextrin (HP--CD) were prepared using an environmentally-benign supercritical anti-solvent (SAS) process. In order to evaluate the degree of complexation, the thermal behavior of solid micro particulate complexes was investigated using differential scanning calorimetry. The experimental results obatined for the solubility and dissolution rate of the microparticulate inclusion complexes in a buffer solution of pH 1.2 showed that the complexation of itraconazole with HP--CD results in a significant increase in the solubility and dissolution rate of itraconazole. For the microparticulate itraconazole/Hp--CD inclusion complexes prepared by the SAS process, about 80% of itraconazole was found to dissolve in the buffer solution. Our experimental results confirmed that the SAS process is a promising method for the preparation of microparticles of water-insoluble drug/cyclodextrin inclusion complexes.
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KEYWORD
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Itraconazole, cyclodextrin, inclusion complex, supercritical fluid, anti-solvent
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