Abstract
Purpose: This investigation was carried out to determine if a solid dispersion of furosemide in sodium starch glycolate (SSG) would enhance the dissolution properties of the drug. Methods: Solid dispersion of furosemide in SSG was prepared in ratios of 1:1 and 1 (furosemide):2 (SSG) by kneading method. In each case, the solid dispersion was characterized by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) to ascertain if there were any physicochemical interactions between drug and carrier that could affect dissolution. Tablets containing the solid dispersion were formulated and their dissolution characteristics compared with commercial furosemide tablets. The dissolution studies were performed at 37 ± 0.5oC and 50 rpm in simulated gastric fluid (pH 1.2). Results: FTIR spectroscopy, DSC, and XRD showed a change in crystal structure toward an amorphous form of furosemide. Dissolution data indicated that furosemide dissolution was enhanced. XRD, DSC, FTIR spectroscopy and dissolution studies indicated that the solid dispersion formulated in 1:2 ratio showed a 5.40-fold increase in dissolution and also exhibited superior dissolution characteristics to commercial furosemide tablets. Conclusion: Solid dispersion technique can be used to improve the dissolution of furosemide Keywords: Solid dispersion, Furosemide, Sodium starch glycolate, Dissolution enhancement, physicochemical characterisationTropical Journal of Pharmaceutical Research Vol. 8 (1) 2009: pp. 43-51
Highlights
Furosemide (FRMD) is 5-(aminosulphonyl)-4chloro-2-[(2-fuanyl-methyl) amino] benzoic acid, and it is a potent high ceiling diuretic mainly used in the treatment of hypertension[1]
The above characteristic peaks appear in the spectra of all binary systems at the same wave number indicating no interaction between the drug and the carrier (SSG)
differential scanning calorimetry (DSC) studies showed that there no interaction between drug and carrier at a molecular level in both the solid dispersions and physical mixtures
Summary
Furosemide (FRMD) is 5-(aminosulphonyl)-4chloro-2-[(2-fuanyl-methyl) amino] benzoic acid, and it is a potent high ceiling (loop) diuretic mainly used in the treatment of hypertension[1]. A mixture (6g) of furosemide and SSG (1:1 and 1:2 by weight, respectively) was wetted with water-ethanol (1:1 ratio) till the slurry was formed and kneaded thoroughly for 60 min in a glass mortar. It was found that solid dispersion prepared by kneading in 1:2 (furosemide: SSG) ratio showed higher dissolution; this solid dispersion was used for the preparation of tablet formulations. MD3 tablets contain same amount of furosemide and magnesium stearate as MD1 plus 89 mg of Avicel PH102 and 40 mg of Crosscarmellose sodium. In vitro dissolution studies on MD3 tablets and two commercial tablets of furosemide containing 40mg of furosemide formulation A (Lasix®) and formulation B (Salinex®), respectively - were carried out in 900mL of SGF (pH-1.2) as the dissolution media as described previously
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