Supercritical antisolvent versus coevaporation - Preparation and characterization of solid dispersions

Viktor Majerik, G. Horváth, László Szokonya, Gérard Charbit, Elisabeth Badens, Nathalie Bosc, Eric Teillaud

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The objective of this work was to improve the dissolution rate and aqueous solubility of oxeglitazar. Solid dispersions of oxeglitazar in PVP K17 (polyvinilpyrrolidone) and poloxamer 407 (polyoxyethylene-polyoxypropylene block copolymer) were prepared by supercritical antisolvent (SAS) and coevaporation (CoE) methods. Drug-carrier formulations were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, gas chromatography, UV/VIS spectroscopy and in vitro dissolution tests. The highest dissolution rate (nearly 3-fold higher than raw drug) was achieved by preparation of drug/PVP K17 coevaporate. Oxeglitazar/PVP K17 solid dispersions were stabilized by hydrogen bonding but contained higher amount of residual dichloromethane (DCM) than poloxamer 407 formulations regardless of the method of preparation. SAS prepared oxeglitazar/poloxamer 407 dissolved more than two times faster than raw drug. However, unlike PVP K17, poloxamer 407 did not form a single phase amorphous solid solution with oxeglitazar which has been manifested in higher degrees of crystallinity, too. Among the two techniques, evaluated in this work, conventional coevaporation resulted in higher amorphous content but SAS reduced residual solvent content more efficiently.

Original languageEnglish
Pages (from-to)975-983
Number of pages9
JournalDrug Development and Industrial Pharmacy
Volume33
Issue number9
DOIs
Publication statusPublished - Sep 2007

Fingerprint

Poloxamer
Dispersions
Drug Compounding
Dissolution
Pharmaceutical Preparations
Drug Carriers
Methylene Chloride
Fourier Transform Infrared Spectroscopy
Hydrogen Bonding
Ultraviolet spectroscopy
X-Ray Diffraction
Gas chromatography
Gas Chromatography
Electron Scanning Microscopy
Powders
X ray powder diffraction
Solubility
Block copolymers
Solid solutions
Spectrum Analysis

Keywords

  • Coevaporation
  • Oxeglitazar
  • Poorly water-soluble drug
  • Solid dispersion
  • Supercritical antisolvent

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology
  • Molecular Medicine

Cite this

Supercritical antisolvent versus coevaporation - Preparation and characterization of solid dispersions. / Majerik, Viktor; Horváth, G.; Szokonya, László; Charbit, Gérard; Badens, Elisabeth; Bosc, Nathalie; Teillaud, Eric.

In: Drug Development and Industrial Pharmacy, Vol. 33, No. 9, 09.2007, p. 975-983.

Research output: Contribution to journalArticle

Majerik, Viktor ; Horváth, G. ; Szokonya, László ; Charbit, Gérard ; Badens, Elisabeth ; Bosc, Nathalie ; Teillaud, Eric. / Supercritical antisolvent versus coevaporation - Preparation and characterization of solid dispersions. In: Drug Development and Industrial Pharmacy. 2007 ; Vol. 33, No. 9. pp. 975-983.
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