Powder engineering technique of ibuprofen crystal using combination of complexation and phase partition method

Abstract

By combinding phase partition technique and using dispersion carriers such as polyvinylpyrrolidone (PVP K 30) and polyethylene glycol (PEG) to produce the spherical pellets could improve the dissolution property including physical property of a poorly water soluble drug, ibuprofen. Ibuprofen pellets produced with PVP K 30 had uniform size and spherical in shape. Whereas, ibuprofen pellets with PEG had rough surface and size variation. Physicochemical properties of pellets were characterized by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectrometry and 13C nuclear magnetic resonance (13c NMR). Chemical interaction between drug and polymer (PVP K 30) were found during the dispersion state of ibuprofen and PVP K 30. This chemical interaction was due to complex formation of ibuprofen with PVP K 30 by hydrogen bonding. Whereas, X-ray diffractogram and DSC thermogram of the dispersion of ibuprofen and PEG showed the evidence like the interstitial solid solution between ibuprofen and PEG had formed. The other reason, by disorientation of the structure between ibuprofen and PEG in this mixture. In the case of the dispersion of ibuprofen with both of PVP K 30 and PEG at suitable ratio, the weak hydrogen bonding may occur. However, an evidence of chemical interaction between drug and polymers in the formulations after phase partition of ibuprofen into pellets maybe found. As indicated by 13C NMR, the signal of carboxylic acid carbon of drug had shifted (except in the case of the formulations of ibuprofen with PEG alone). It may be caused by the weak hydrogen bonding between ibuprofen and PVP K 30 or by disorientation of the structure of drug. For dissolution study, ibuprofen pellets with PVP K 30 or the mixture of PVP K 30 and PEG in suitable ratio had faster release than the formulation of ibuprofen pellets with drug alone or ibuprofen pellets with PEG: Furthermore, ibuprofen pellets from a suitable ratio of drug: polymers had good physical properties.