Formulation and Evaluation of Solid Dispersion Tablets of Furosemide Using Polyvinylpyrrolidone K-30

Abstract

Objective: The objective of the present study was to improve the aqueous solubility and dissolution characteristics of the loop diuretic furosemide (FUR); a class IV drug in the Biopharmaceutical Classification System (BCS) using solid dispersion technique.
 Methods: Solvent evaporation and kneading methods were used to produce solid dispersions of FUR in different ratios with the hydrophilic carrier polyvinylpyrrolidone K-30 (PVP-K30). The prepared solid dispersions were evaluated in terms of solubility study, percentage yield, drug content and Fourier transform infrared spectroscopic study (FT-IR). Tablets containing the optimized formula of solid dispersions ( were formulated and their dissolution characteristics were compared with commercial furosemide tablets.
 Results: The prepared solid dispersions showed an increase in aqueous solubility, especially those formulated in a 1:2 drug: carrier ratio using solvent evaporation method ( it showed a four-fold increase in solubility compared to the parent drug. The absence of drug-carrier chemical interactions that could affect the dissolution was proved by FT-IR. Solid dispersion tablets exhibited a better dissolution profile in simulated gastric fluid pH 1.2 at 37°C ± 0.5 than the commercial FUR tablets in terms of mean dissolution time (8.44 min) and dissolution efficiency in 30 min (42.54%). Both FUR solid dispersions and commercial tablets followed Weibull and Krosmeyer models as the two best models of drug release kinetics proving that they were immediate release.
 Conclusion: According to the results obtained in this study, solid dispersion techniques could be successfully used for the enhancement of aqueous solubility and dissolution rate of FUR.

Solid Dispersion of Acetosal Using Polyvinyl Pyrrolidone (PVP) K-30 in Tablets with Direct Compressing Method

“…The results of the compressibility index of the three formulas obtained a percentage of <10%, so it can be said that the test results are included in the very good compressibility index category (Arulkumaran & Padmapreetha, 2014). This also follows the literature stating that generally, a compressibility index value of 5-15% indicates excellent flow properties (Begum et al, 2019;Elmubarak et al, 2021).…”

“…This indicates that the results do not follow the literature, which states that a good tablet must have a friability of <1% (Depkes RI, 1979). According to USP, a tablet friability value of <1% is considered acceptable for most pharmaceutical tablets (Elmubarak et al, 2021). High friability affects the concentration or content of the active substance contained in the tablet, and the greater the percentage of friability, the greater the mass loss of the tablet (Gopalan & Gozali, 2018).…”

Solid Dispersion Incorporated into Dissolving Microneedles for Improved Antifungal Activity of Amphotericin B: In Vivo Study in a Fungal Keratitis Model

“…This increase in solubility was due to the increased solubilizing effect against the drug and the wetting of drug particles by hydrophilic polymers such as PEG 6000 and PVP . The concentration of the increasing amount of polymer in SD is generally able to increase the solubility of the drug. − However, in this study, the highest solubility results were found at the concentration ratio of AMB:PVP (5:5), which is the lowest concentration of the polymer. Similar to several previous studies that formulated SD using PVP and PEG 6000, in this study, SD solubility results were obtained at the lowest polymer concentration and even the increase in drug solubility did not match with the increased concentration of polymer used. − This research shows that it is important to choose the proper concentration ratio of PVP or PEG 6000 as it plays a significant role in drug solubility.…”

Formulation Development and in Vitro Characterization of Ternary Hydrotropic Solid Dispersions of Aceclofenac

“…However, increase in CP concentration above the threshold value produced no further improvement as maximum wetting and swelling of SD particles has been achieved in C2. Drug dissolution of CP-based formulations may not always follow linear relationship with CP concentration [65,66].…”