Mohammad Reza Siahi-Shadbad1, Saeed Ghanbarzadeh2, Mohammad Barzegar-Jalali1, Hadi Valizadeh3, Alireza Taherpoor3, Ghobad Mohammadi4, Azim Barzegar-Jalali5, Khosro Adibkia6. 1. Drug Applied Research Center, Tabriz University of Medical Science, Tabriz, Iran. ; Faculty of Pharmacy, Tabriz University of Medical Science, Tabriz, Iran. 2. Faculty of Pharmacy, Tabriz University of Medical Science, Tabriz, Iran. ; Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran. ; Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz, Iran. 3. Faculty of Pharmacy, Tabriz University of Medical Science, Tabriz, Iran. 4. School of Pharmacy, Kermanshah University of Medical Science, Kermanshah, Iran. 5. Faculty of Medicine, Islamic Azad University, Ardabil branch, Ardabil, Iran. 6. Drug Applied Research Center, Tabriz University of Medical Science, Tabriz, Iran. ; Faculty of Pharmacy, Tabriz University of Medical Science, Tabriz, Iran. ; Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz, Iran.
Abstract
PURPOSE: The purpose of this study was to prepare and characterize solid dispersion formulation of furosemide to enhance dissolution rate. METHODS: Solid dispersions with different drug: carrier ratios were prepared by cogrinding method using crospovidone and microcrystalline cellulose as carrier. The physical state and interactions between the drug and carrier were characterized by Fourier transform infrared spectroscopic (FT-IR) and X ray diffraction (XRD). RESULTS: Solid dispersions (especially with drug: Carrier ratio of 1:2) showed a higher dissolution rate than their respective physical mixture and pure furosemide. Dissolution rate in pH 5.8 was also higher than pH 1.2. The XRD analysis showed that crystalline form was changed to the amorphous state in the solid dispersions. FT-IR analysis did not show any physicochemical interactions in the solid dispersion formulations. Release kinetic of formulations were fitted best to the Weibull and Wagner log probability (linear kinetic) as well as suggested 2 and Gompertz (non-linear kinetic) models. CONCLUSION: The dissolution properties of furosemide were improved with the use of hydrophilic carriers in solid dispersions due to change in the crystalline form of the drug and more intimate contact between drug and carriers which was dependent on the type and ratio of carrier as well as dissolution medium pH.
PURPOSE: The purpose of this study was to prepare and characterize solid dispersion formulation of furosemide to enhance dissolution rate. METHODS: Solid dispersions with different drug: carrier ratios were prepared by cogrinding method using crospovidone and microcrystalline cellulose as carrier. The physical state and interactions between the drug and carrier were characterized by Fourier transform infrared spectroscopic (FT-IR) and X ray diffraction (XRD). RESULTS: Solid dispersions (especially with drug: Carrier ratio of 1:2) showed a higher dissolution rate than their respective physical mixture and pure furosemide. Dissolution rate in pH 5.8 was also higher than pH 1.2. The XRD analysis showed that crystalline form was changed to the amorphous state in the solid dispersions. FT-IR analysis did not show any physicochemical interactions in the solid dispersion formulations. Release kinetic of formulations were fitted best to the Weibull and Wagner log probability (linear kinetic) as well as suggested 2 and Gompertz (non-linear kinetic) models. CONCLUSION: The dissolution properties of furosemide were improved with the use of hydrophilic carriers in solid dispersions due to change in the crystalline form of the drug and more intimate contact between drug and carriers which was dependent on the type and ratio of carrier as well as dissolution medium pH.
Authors: Nicola De Zordi; Mariarosa Moneghini; Ireneo Kikic; Mario Grassi; Antonio Esau Del Rio Castillo; Dario Solinas; Michael B Bolger Journal: Eur J Pharm Biopharm Date: 2012-01-17 Impact factor: 5.571
Authors: Hiba Al-Hamidi; Alison A Edwards; Mohammad A Mohammad; Ali Nokhodchi Journal: Colloids Surf B Biointerfaces Date: 2009-11-11 Impact factor: 5.268