title: Solubility, dissolution rate and bioavailability enhancement of irbesartan by solid dispersion technique.
abstract: The objective of present work was to enhance the solubility and bioavailability of poorly aqueous soluble drug Irbesartan (IBS). The solid dispersions were prepared by spray drying method using low viscosity grade HPMC E5LV. Prepared solid dispersions were characterized by dissolution study, fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction studies (XRD). Results of the SEM, DSC and XRD study showed the conversion of crystalline form of IBS to amorphous form. The dissolution rate was remarkably increased in case of solid dispersion compared to pure IBS. Solubility and stability of solid dispersion was increased due to surfactant and wetting property, slowing devitrification and having anti-plasticization effect of HPMC E5LV. In vivo studies were performed in healthy rabbits (New Zealand grey) and compared with plain IBS. Solid dispersions showed increase in relative bioavailability than the plain IBS suspension. In conclusion, the prepared solid dispersions showed remarkable increase in solubility, dissolution rate and hence bioavailability of poorly water soluble drug Irbesartan.
authors.affiliation: Department of Pharmaceutics and Quality Assurance, R. C. Patel Institute of Pharmaceutical Education and Research, Near Karwand Naka, Shirpur, Maharashtra, India
authors.forename: Rikisha Jaysukhbhai
authors.initials: RJ
authors.lastname: Boghra
authors.forename: Pranita Chandrakant
authors.initials: PC
authors.lastname: Kothawade
authors.forename: Veena Shailendra
authors.initials: VS
authors.lastname: Belgamwar
authors.forename: Pankaj Padmakar
authors.initials: PP
authors.lastname: Nerkar
authors.forename: Avinash Ramrao
authors.initials: AR
authors.lastname: Tekade
authors.forename: Sanjay Javerilal
authors.initials: SJ
authors.lastname: Surana
mesh_terms: D000818:Animals; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000737:chemistry* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D000077405:Irbesartan; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013777:Tetrazoles / Q000737:chemistry* / Q000493:pharmacokinetics; D014783:Viscosity; D014961:X-Ray Diffraction
chemical_list: D001713:Biphenyl Compounds; D013777:Tetrazoles; D000077405:Irbesartan