Development of novel sibutramine base-loaded solid dispersion with gelatin and HPMC: Physicochemical characterization and pharmacokinetics in beagle dogs

Our results suggested that the solid dispersion and commercial product produced a similar correlation of dissolution profiles at all pH ranges

Hyun-Tae Lim

2010

Scholarcy highlights

  • To develop a novel sibutramine base-loaded solid dispersion with enhanced solubility and bioavailability, various solid dispersions were prepared using a spray drying technique with hydrophilic polymers such as gelatin, HPMC and citric acid
  • The sibutramine base-loaded solid dispersions containing hydrophilic polymer and citric acid showed higher drug solubility compared to sibutramine base and sibutramine hydrochloride monohydrate
  • Among the formulations tested, the solid dispersion composed of sibutramine base/gelatin/HPMC/citric acid at the weight ratio of 1/0.8/0.2/0.5 gave the highest solubility of 5.03 ± 0.24 mg/ml
  • Our DSC and powder X-ray diffraction results showed that the drug was present in an altered amorphous form in this solid dispersion
  • Our results suggested that the solid dispersion and commercial product produced a similar correlation of dissolution profiles at all pH ranges
  • The sibutramine base-loaded solid dispersion prepared with gelatin, HPMC and citric acid is a promising candidate for improving the solubility and bioavailability of the poorly water-soluble sibutramine base

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