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

被引:6
|
作者
Siahi-Shadbad, Mohammad Reza [1 ,2 ]
Ghanbarzadeh, Saeed [2 ,3 ,4 ]
Barzegar-Jalali, Mohammad [1 ,2 ]
Valizadeh, Hadi [2 ]
Taherpoor, Alireza [2 ]
Mohammadi, Ghobad [5 ]
Barzegar-Jalali, Azim [6 ]
Adibkia, Khosro [1 ,2 ,4 ]
机构
[1] Tabriz Univ Med Sci, Drug Appl Res Ctr, Tabriz, Iran
[2] Tabriz Univ Med Sci, Fac Pharm, Tabriz, Iran
[3] Tabriz Univ Med Sci, Student Res Comm, Tabriz, Iran
[4] Tabriz Univ Med Sci, Res Ctr Pharmaceut Nanotechnol, Tabriz, Iran
[5] Kermanshah Univ Med Sci, Sch Pharm, Kermanshah, Iran
[6] Islamic Azad Univ, Fac Med, Ardabil Branch, Ardebil, Iran
关键词
Furosemide; Solid dispersion; Dissolution rate; Release kinetic;
D O I
10.5681/apb.2014.058
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:391 / 399
页数:9
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