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Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique

1999; Elsevier BV; Volume: 187; Issue: 2 Linguagem: Inglês

10.1016/s0378-5173(99)00191-x

1873-3476

Jae‐Young Jung, Sun Dong Yoo, Sang-Heon Lee, Kye-Hyun Kim, Doo-Sun Yoon, Kyuhyun Lee,

Analytical Chemistry and Chromatography

The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, itraconazole, by a solid dispersion technique. Solid dispersion particles of itraconazole were prepared with various pH-independent and -dependent hydrophilic polymers and were characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. Of the polymers tested, pH-dependent hydrophilic polymers, AEA and Eudragit E 100, resulted in highest increases in drug solubility (range, 141.4-146.9-fold increases). The shape of the solid dispersion particles was spherical, with their internal diameter ranging from 1-10 microm. The dissolution rate of itraconazole from the tablets prepared by spray drying (SD-T) was fast, with > 90% released within 5 min.SD-T prepared with AEA or Eudragit E 100 at a 1:1 drug hydrophilic polymer ratio (w/w) showed approximately 70-fold increases in the dissolution rate over a marketed product.