Crystal modifications and dissolution rate of piroxicam

Abstract

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.

Formulation and evaluation of sublingual delivery of piroxicam using thermosensitive polymer with an inverted Franz diffusion cell

“…It was concluded in their study that the needle forms showed improved dissolution but not the solubility. Similarly, the cube‐shaped crystals from the slow evaporation method which included addition of polymer such as polyvinylpyrrolidone K30 and polyethylene glycol 4000 showed improved solubility but not solubility . In our study, by the inclusion of the 15% w/v poloxamer in the formulation, not only the dissolution but also the solubility of the drug was increased as shown in the permeation profile.…”

“…Similarly, the cube-shaped crystals from the slow evaporation method which included addition of polymer such as polyvinylpyrrolidone K30 and polyethylene glycol 4000 showed improved solubility but not solubility. [27] In our study, by the inclusion of the 15% w/v poloxamer in the formulation, not only the dissolution but also the solubility of the drug was increased as shown in the permeation profile. As reported by Lyn et al, recrystallized piroxicam using slow crystallization method produced cube-shaped crystals which displayed better dissolution profile than the untreated piroxicam.…”

“…In our study, by the inclusion of the 15% w/v poloxamer in the formulation, not only the dissolution but also the solubility of the drug was increased as shown in the permeation profile. As reported by Lyn et al ., recrystallized piroxicam using slow crystallization method produced cube‐shaped crystals which displayed better dissolution profile than the untreated piroxicam . This observation correlated with 0.1% w/w piroxicam poloxamer‐based formulation where the relatively cube‐shaped crystals showed an enhanced permeation than the non‐poloxamer‐based formulation, and this suggests that recrystallization of drug crystals might have occurred at 0.1% w/w drug concentration.…”

“…© 2015 Royal Pharmaceutical Society, Journal of Pharmacy and Pharmacology, 68 (2016), pp [26][27][28][29][30][31]…”

Curcumin Promotes Cell Cycle Arrest and Inhibits Survival of Human Renal Cancer Cells by Negative Modulation of the PI3K/AKT Signaling Pathway

“…The principal effective component of curcuma is curcumin [9]. Crystal curcumin is a light yellow powder, soluble in ethanol, acetone, ethylene glycol and alkaline solution, insoluble in water, and slightly soluble in vegetable oil [10]. Curcumin exhibits antitumor, antiviral, anti-inflammatory, anti-oxidant, antiatherosclerotic, anti-fibrotic, hypo-lipidomic, and liver-and kidney-protecting features [11,12].…”