2004•Chinese Journal of Hospital PharmacyRequires access

Preparation of itraconazole solid dispersion with PVP and dissolution experiment in vitro

Qing Pang

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Abstract

OBJECTIVE The aim of present study is to improve the solubility and dissolution rate of itraconazole,which is sparingly soluble in water by a solid dispersion technique.METHODS Solid dispersion (SD) particles of itraconazole were prepared with PVP K30 by spray drying and were characterized by differential scanning calorimetry, powder X-ray diffraction.RESULTS The result of differential scanning calorimetry and powder X-ray diffraction test showed that spray drying resulted in the formation of an amorphous solid dispersion of itraconazole and PVP. Dissolution measurements demonstrated that a significantly increased dissolution rate was obtained with the amorphous solid dispersion compared to the physical mixture. Dissolution rate of itraconazole/PVP (1∶4 w/w) was 11.5 times than itraconazole powder at 45 min. Solubility of itraconazole in solid dispersion with PVP was 67 times than itraconazole.CONCLUSION Itraconazole solid dispersion can significantly increase it's solubility and dissolution rate.

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OBJECTIVE The aim of present study is to improve the solubility and dissolution rate of itraconazole,which is sparingly soluble in water by a solid dispersion technique.METHODS Solid dispersion (SD) particles of itraconazole were prepared with PVP K30 by spray drying and were characterized by differential scanning calorimetry, powder X-ray diffraction.RESULTS The result of differential scanning calorimetry and powder X-ray diffraction test showed that spray drying resulted in the formation of an amorphous solid dispersion of itraconazole and PVP. Dissolution measurements demonstrated that a significantly increased dissolution rate was obtained with the amorphous solid dispersion compared to the physical mixture. Dissolution rate of itraconazole/PVP (1∶4 w/w) was 11.5 times than itraconazole powder at 45 min. Solubility of itraconazole in solid dispersion with PVP was 67 times than itraconazole.CONCLUSION Itraconazole solid dispersion can significantly increase it's solubility and dissolution rate.

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Available abstract

OBJECTIVE The aim of present study is to improve the solubility and dissolution rate of itraconazole,which is sparingly soluble in water by a solid dispersion technique.METHODS Solid dispersion (SD) particles of itraconazole were prepared with PVP K30 by spray drying and were characterized by differential scanning calorimetry, powder X-ray diffraction.RESULTS The result of differential scanning calorimetry and powder X-ray diffraction test showed that spray drying resulted in the formation of an amorphous solid dispersion of itraconazole and PVP. Dissolution measurements demonstrated that a significantly increased dissolution rate was obtained with the amorphous solid dispersion compared to the physical mixture. Dissolution rate of itraconazole/PVP (1∶4 w/w) was 11.5 times than itraconazole powder at 45 min. Solubility of itraconazole in solid dispersion with PVP was 67 times than itraconazole.CONCLUSION Itraconazole solid dispersion can significantly increase it's solubility and dissolution rate.

Key concepts: Itraconazole, Dissolution, Differential scanning calorimetry, Dispersion (optics), Solubility, Amorphous solid, Materials science, Dissolution testing

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