Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process

Dong Han Won, Min Soo Kim, Sibeum Lee, Jeong Sook Park, Sung Joo Hwang

Research output: Contribution to journalArticlepeer-review

166 Citations (Scopus)

Abstract

Solid dispersions of felodipine were formulated with HPMC and surfactants by the conventional solvent evaporation (CSE) and supercritical anti-solvent precipitation (SAS) methods. The solid dispersion particles were characterized by particle size, zeta potential, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), solubility and dissolution studies. The effects of the drug/polymer ratio and surfactants on the solubility of felodipine were also studied. The mean particle size of the solid dispersions was 200-250 nm; these had a relatively regular spherical shape with a narrow size distribution. The particle size of the solid dispersions from the CSE method increased at 1 h after dispersed in distilled water. However, the particle sizes of solid dispersions from the SAS process were maintained for 6 h due to the increased solubility of felodipine. The physical state of felodipine changed from crystalline to amorphous during the CSE and SAS processes, confirmed by DSC/XRD data. The equilibrium solubility of the felodipine solid dispersion prepared by the SAS process was 1.5-20 μg/ml, while the maximum solubility was 35-110 μg/ml. Moreover, the solubility of felodipine increased with decreasing drug/polymer ratio or increasing HCO-60 content. The solid dispersions from the SAS process showed a high dissolution rate of over 90% within 2 h. The SAS process system may be used to enhance solubility or to produce oral dosage forms with high dissolution rate.

Original languageEnglish
Pages (from-to)199-208
Number of pages10
JournalInternational Journal of Pharmaceutics
Volume301
Issue number1-2
DOIs
Publication statusPublished - 2005 Sep 14

Bibliographical note

Funding Information:
This work was supported in part by the National Research Laboratory program (M1-0302-00-0016) in the series of MOST-NRDP in the Ministry of Science and Technology, Korea.

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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