title: Enhancement of the dissolution profile of allopurinol by a solid dispersion technique.
abstract: The aim of the present study was to improve the solubility, and therefore the dissolution of poorly water-soluble allopurinol. Solid dispersions of allopurinol were prepared with different polymers or carriers such as polyvinylpyrrolidone (PVP K30 and PVP K90), polyethylene glycol (PEG 4000 and PEG 6000), urea and mannitol at two drug : carrier ratios (1:1) and (1:2). Different methods such as melting and solvent evaporation methods were used to improve dissolution characteristics and solubility of allopurinol. The solid dispersions were characterized using a differential scanning calorimeter (DSC) and X-ray diffraction (XRD) while the interactions which took place were identified with fourier transform infrared (FTIR) spectroscopy. Due to formation of hydrogen bonds between allopurinol and urea and mannitol, a transition of allopurinol from the crystalline to amorphous state was achieved. The DSC thermograms of the solid dispersions indicated the potential of heat induced interactions between allopurinol and the carriers used could influence dissolution rate of the drug. The dissolution amount (%) of pure allopurinol was 80% at 45 min. F5, F3, F6, F7, and F1 showed better dissolution percentages of 100, 93, 92.4, 90.6, and 89%, respectively, at 45 min.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
authors.forename: A M
authors.initials: AM
authors.lastname: Samy
authors.forename: M A
authors.initials: MA
authors.lastname: Marzouk
authors.forename: A A
authors.initials: AA
authors.lastname: Ammar
authors.forename: M K
authors.initials: MK
authors.lastname: Ahmed
mesh_terms: D000493:Allopurinol; D002152:Calorimetry, Differential Scanning; D011092:Polyethylene Glycols / Q000737:chemistry; D011205:Povidone; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D011092:Polyethylene Glycols; D000493:Allopurinol; D011205:Povidone