Abstract
Purpose. Piroxicam is a poorly soluble NSAID, whose solubility is enhanced when included into β-cyclodextrin. The preparation of a piroxicam-β-cyclodextrin inclusion compound using supercritical CO2 was investigated.
Methods. The solubility and the stability of piroxicam in supercritical CO2 were determined. Then, the influence of the temperature, the pressure and the time of exposure on the inclusion rate was studied.
Results. The solubility of piroxicam varied over a wide range depending on the temperature and pressure (from 0.006 to 1.500 mg/g of CO2). The temperature and the time of exposure had a great influence on the inclusion yield, while pressure did not and a complete inclusion was achieved by keeping a physical mixture of piroxicam and β-cyclodextrin (1:2.5 mol/mol) for 6 hours at 150°C and 15 MPa of CO2. This complex was characterized by Differential Scanning Calorimetry, differential solubility and Fourier Transform Infrared Spectrometry.
Conclusions. Supercritical carbon dioxide may prove to be a novel useful complexation method of drugs into β-cyclodextrin.
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Van Hees, T., Piel, G., Evrard, B. et al. Application of Supercritical Carbon Dioxide for the Preparation of a Piroxicam-β-Cyclodextrin Inclusion Compound. Pharm Res 16, 1864–1870 (1999). https://doi.org/10.1023/A:1018955410414
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DOI: https://doi.org/10.1023/A:1018955410414