Physicochemical Characterization and Dissolution Study of Solid Dispersions of Furosemide with Polyethylene Glycol 6000 and Polyvinylpyrrolidone K30

Abstract

Solid dispersions traditionally have been used as effective methods to improve the dissolution properties and bioavailability of poorly water-soluble drugs. The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, furosemide, by a solid dispersion technique. Solid dispersions were prepared using polyethylene glycol 6000 (PEG 6000) and polyvinylpyrrolidone K30 (PVP K30) in different drug-to-carrier ratios. Dispersions with PEG 6000 were prepared by fusion-cooling and solvent evaporation, while dispersions containing PVP K30 were prepared by solvent evaporation technique. These new formulations were characterized in the liquid state by phase solubility studies and in the solid state by differential scanning calorimetry, powder X-ray diffraction, and FTIR spectroscopy. The aqueous solubility of furosemide was favored by the presence of both polymers. Solid state characterizations indicated that furosemide was present as an amorphous material and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure furosemide, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with PEG showed the most improvement in wettability and dissolution rate of furosemide. Even physical mixtures of furosemide prepared with both polymers also showed better dissolution profiles as compared with that of pure furosemide. Tablets prepared using solid dispersions showed significant improvement in the release profile of furosemide as compared with conventional tablets prepared using furosemide without PEG or PVP.

Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems

“…The drug also exhibits absorption at 2251 and 3317 cm −1 indicating the exocyclic tricyclic triple bond and the stretching of N-H, respectively[20]. Important vibrations detected in the spectrum of PEG 8000 were the C-H stretching at 2880 cm −1 and the C-O (ether) stretching at 1110 cm −1 [2122]. The spectrum of PVP K30 showed important bands at 1652 cm −1 which indicates C=O stretch in the cyclic amide and a broad band at about 2850-3000 cm −1 attributed to aliphatic C-H stretch.…”

Tadalafil oral disintegrating tablets: an approach to enhance tadalafil dissolution

“…It shows excellent water solubility. Its molecular size (ranging from 10,000 to 700,000) favors the formation of interstitial solid solutions; it has been demonstrated to retard the drug crystallization giving amorphous solid dispersions with increased drug dissolution rates and solubilities (Patel et al 2008). PVP is capable of forming molecular adducts with many compounds; the presence of hydroxyl or carbonyl groups in the repeat units of the polymer tends to increase the water solubility and stability of the drug and also improves its bioavailability (Anant et al 2004).…”

Physicochemical Characterization of Febuxostat Microcomplexes with Parent and Modified Cyclodextrins

“…The more negative values of the entropy (ΔS) indicated the high orderness of complexes in case of all the systems. 12 These values indicated that the system was releasing the energy upon complexation forming a ordered complexes respectively, implying highly stable physical state of all the complexes.…”