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 ± 0.5 o C 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.
The objective of this research was to develop and evaluate physicochemical properties of acetaminophen and aspirin orally disintegrating strips with high loading dose. The strips were compared with conventional over the counter strips and chewable tablets for their mechanical and chemical properties. Aspirin (81 mg) and acetaminophen (80 mg) oral dissolving films were developed with 50-55% of drug loading and were compared with GAS-X ® (62.5 mg) and chewable tablets (aspirin and acetaminophen). Orally dissolving films were developed using a solvent casting method. Sonication was proven to be a more competent step in order to load a high amount of active drug substance in the thin film strips. Different film formulations were prepared by varying concentration of polymers and plasticizers. Optimization of formulation was done by conducting studies for various mechanical properties using TA-XT plus texture analyzer. Dissolution of optimized formulation was performed in 250 ml of pH 1.2 and artificial saliva (pH 6.8). The study was conducted by stirring the dissolution media at 50 rpm, 37 C for 30 minutes and was analyzed using UV/Vis spectroscopy. The dimensions of orally dissolving films were determined with the help of vernier calipers. Modulated Differential Scanning Calorimetry (MDSC) was also performed for the filmstrips to check the compatibility. The film strip was evaluated for imperfections and cuts, peelability without rupturing, folding and cracking endurance, surface roughness, tensile strength, film burst and disintegration time with the help of TA-XT plus texture analyzer. Moisture content was performed, on the fresh, as well as stability samples. Dissolution of filmstrips showed much faster release as compared to respective chewable tablets in artificial saliva as well as in pH 1.2. Disintegration times for filmstrips were also comparable to Gas-X ® and Listerine ® . After one month stability of filmstrips at room temperature, dissolution profiles perceived with negligible change. Other mechanical properties of the filmstrips were also comparable to Gas-X ® . DSC results suggest miscibility in polymer, which explains the increase in dissolution rate of filmstrips at high dose loading. Hence, in conclusion we develop a new in house method to formulate a stable and more efficient formulation for high loading dose of aspirin and acetaminophen.
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