Comparative evaluation of ibuprofen/beta-cyclodextrin complexes obtained by supercritical carbon dioxide and other conventional methods.
OBJECTIVE
The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared with other conventional methods.


METHODS
Ibuprofen/beta-cyclodextrin complexes were prepared with different techniques and characterized using FTIR-ATR spectroscopy, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). In addition, the influences of the processing technique on the drug content (HPLC) and the dissolution behavior were studied.


RESULTS
Employing the CPD-process resulted in a drug content of 2.8+/-0.22 wt.% in the carrier. The material obtained by CPD showed an improved dissolution rate of ibuprofen at pH 5 compared with the pure drug and its physical mixture with beta-cyclodextrin. In addition CPD material displays the highest dissolution (93.5+/- 2.89% after 75 min) compared to material obtained by co-precipitation (61.3 +/-0.52%) or freeze-drying (90.6 +/-2.54%).


CONCLUSIONS
This study presents the CPD-technique as a well suitable method to prepare a drug/beta-cyclodextrin complex with improved drug dissolution compared to the pure drug and materials obtained by other methods.
Hussein
Khaled
K
1 Pharmazeutische Technologie, Eberhard-Karls-Universität Tübingen, Auf der Morgenstelle 8, D-72076 Tübingen, Germany.
Türk
Michael
M
Wahl
Martin A
MA
D002245:Carbon Dioxide / Q000737:chemistry*; D025924:Chromatography, Supercritical Fluid / Q000295:instrumentation / Q000379:methods*; D005612:Freeze Drying / Q000295:instrumentation / Q000379:methods; D007052:Ibuprofen / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D012995:Solubility; D013055:Spectrophotometry, Infrared / Q000379:methods; D013678:Technology, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D013696:Temperature; D013816:Thermodynamics; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics
D047392:beta-Cyclodextrins; D002245:Carbon Dioxide; D007052:Ibuprofen