Characterization of itraconazole semisolid dosage forms prepared by hot melt technique

Sang Young Shim, Chang Won Ji, Hongkee Sah, Eun Seok Park, Beom Jin Lee

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The objective of this study was to formulate itraconazole semisolid dosage forms and characterize their physicochemical properties. Itraconazole and excipients such as polysorbate 80, fatty acids, fatty alcohols, oils and organic acids were melted at 160°C. The fused solution was then cooled immediately at -10°C to make wax-like semisolid preparations. Their physicochemical attributes were first characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectrometry. The solubility of itraconazole in semisolid preparations and their dispersability in the simulated gastric fluid were also determined. Our semisolid preparations did not show any distinct endothermic peak of a crystalline form of itraconazole around 160-163°C. This suggested that it was changed into amorphous one, when it was formulated into semisolid preparations. In addition, the distinctive functional peaks and chemical shifts of itraconazole were well retained after processing into semisolid preparations. It could be inferred from the data that itraconazole was stable during incorporation into semisolid preparations by the hot melt technique. In particular, itraconazole semisolid preparations composed of polysorbate 80, fatty acids and organic acids showed good solubility and dissolution when dispersed in an aqueous medium. It was anticipated that the semisolid dosage forms would be industrially applicable to improving the bioavailability of poorly water-soluble drugs.

Original languageEnglish
Pages (from-to)1055-1060
Number of pages6
JournalArchives of Pharmacal Research
Issue number11
StatePublished - 30 Nov 2006

Bibliographical note

Funding Information:
The work was partially supported by a grant of the Ministry of Science and Technology-NRL program (M1-0302-00-0080), Korea. The authors are grateful to Dr. Choon-Young Choi for his helpful contribution to the experiment. We also thank the Research Institute of Pharmaceutical Sciences, Kangwon National University for allowing us to use HPLC systems.


  • Dissolution
  • Itraconazole
  • Semisolid dosage forms
  • Solubility


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