Crystal modifications and dissolution rate of piroxicam.
Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.
School of Pharmacy and Health Sciences, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.
Lim Yee
LY
Lyn
Huan Wen
HW
Sze
Adhiyaman
A
Rajendran
Gorajana
G
Adinarayana
Kamal
K
Dua
Sanjay
S
Garg
D003460:Crystallization; D010894:Piroxicam / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility; D013997:Time Factors; D014961:X-Ray Diffraction / Q000379:methods
D010894:Piroxicam