Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods.
This study compares the physicochemical properties of carbamazepine (CBZ) solid dispersions prepared by either a conventional solvent evaporation versus a supercritical fluid process. Solid dispersions of carbamazepine in polyvinylpyrrolidone (PVP) K30 with either Gelucire 44/14 or Vitamin E TPGS, NF (d-alpha-tocopheryl polyethylene glycol 1000 succinate) were prepared and characterized by intrinsic dissolution, differential scanning calorimetry, powder X-ray diffraction and Fourier transform infrared spectroscopy. CBZ/PVP K30 and CBZ/PVP K30/TPGS solid dispersions showed increased dissolution rate. The best intrinsic dissolution rate (IDR) was obtained for supercritically processed CBZ/PVP K30 that was four-fold higher than pure CBZ. Thermograms of various solid dispersions did not show the melting peak of CBZ, indicating that CBZ was in amorphous form inside the carrier system. This was further confirmed by X-ray diffraction studies. Infrared spectroscopic studies showed interaction between CBZ and PVP K30 in solid dispersions. The amorphous state of CBZ coupled with presence of interaction between drug and PVP K30 suggests fewer, if any, stability problems. Because the supercritical-based process produced solid dispersions with IDR better than conventional solid dispersions augmented with amphiphilic carriers, stability issues associated with lipid carriers do not apply, which, in turn, implies easier scale up under current Good Manufacturing Practice for this technique.
Sethia
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College of Pharmacy and Allied Health Professions, St. John's University, 8000 Utopia Parkway, Jamaica, NY 11439, USA.
Squillante
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E
D002152:Calorimetry, Differential Scanning; D002220:Carbamazepine / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D025924:Chromatography, Supercritical Fluid; D011092:Polyethylene Glycols / Q000737:chemistry; D011205:Povidone / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013696:Temperature; D014810:Vitamin E / Q000031:analogs & derivatives* / Q000737:chemistry; D014961:X-Ray Diffraction
D012997:Solvents; C104509:gelucire 44-14; D014810:Vitamin E; D002220:Carbamazepine; D011092:Polyethylene Glycols; D011205:Povidone; C014225:tocophersolan