Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique.
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.
Jung
J Y
JY
Formulation Research Laboratory, Choongwae Pharma Co., 146-141 Annyung-ri, Taeane-up, Hwasung-kun, Kyunggi-do, South Korea.
Yoo
S D
SD
Lee
S H
SH
Kim
K H
KH
Yoon
D S
DS
Lee
K H
KH
D000935:Antifungal Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D017964:Itraconazole / Q000032:analysis / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D012995:Solubility; D014961:X-Ray Diffraction
D000935:Antifungal Agents; D017964:Itraconazole