Adv Pharm Bull. 2014;4(4):391-399.
doi: 10.5681/apb.2014.058
PMID: 25436197
PMCID: PMC4137431
Scopus id: 84906227558
  Abstract View: 353
  PDF Download: 166

Original Research

Development and Characterization of Solid Dispersion for Dissolution Improvement of Furosemide by Cogrinding Method

Mohammad Reza Siahi-Shadbad 1,2, Saeed Ghanbarzadeh 2,3,4, Mohammad Barzegar-Jalali 1,2 * , Hadi Valizadeh 2, Alireza Taherpoor 2, Ghobad Mohammadi 5, Azim Barzegar-Jalali 6, Khosro Adibkia 1,2,4

1 Drug Applied Research Center, Tabriz University of Medical Science, Tabriz, Iran.
2 Faculty of Pharmacy, Tabriz University of Medical Science, Tabriz, Iran.
3 Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
4 Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz, Iran.
5 School of Pharmacy, Kermanshah University of Medical Science, Kermanshah, Iran.
6 Faculty of Medicine, Islamic Azad University, Ardabil Branch, Ardabil, 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.
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