Formulation of Sustained Release Floating Microspheres of Furosemide from Ethylcellulose and Hydroxypropyl Methylcellulose Polymer Blends

Abstract

Furosemide is a potent and commonly used loop diuretic. It is absorbed largely in the stomach and upper small intestine. This narrow absorption window is responsible for its low bioavailability of about 50%, and variable and erratic absorption. The objective of the present investigation was to formulate and evaluate floating microspheres of furosemide for prolonged buoyancy with sustained delivery of the drug into the gastric content. Furosemide loaded microspheres were prepared by the solvent evaporation method. The drug entrapment efficiency was high for all of the formulations ranging from 86.2 to 98.4%. The yield of microspheres production was good partticularly at increased EC/HPMC ratio and lower temperatures. Drug amount and EC/HPMC ratio showed highly significant effects (p<0.0001) on cumulative drug release and buoyancy of microspheres. Floating microspheres that effectively sustain the drug release more than 12 h and exhibit buoyancy of greater than 77% in 12 h were developed. Finally the study confirmed that various furosemide loaded EC/HPMC microspheres formulations could be developed that effectively sustain the drug release for a desired period by varing the ratio of EC and HPMC, and drug amount.

Formulation and In Vitro Evaluation of Furosemide Floating Matrix Tablets Using Boswellia papyrifera Resin as Matrix Forming Polymer

“…The 3395 cm −1 band is assigned to the NH 2 stretching vibration of Ar-NHCH 2 (secondary amine), 3347 and 3254 cm −1 band is assigned to the stretching vibration of SO 2 NH 2 primary amines, and the broad band observed at 2953 cm -1 is assigned to the acidic OH group. The sharp bands observed at 1668 cm −1 band are assigned to the bending vibration of the amino group, and the 1560 cm −1 band is due to the asymmetric stretching vibration of the carbonyl group [17,25]. These characteristic peaks also appear in the spectrum of the floating furosemide tablet formulations at the same wave numbers indicating that there was no interaction between the drug and formulation excipients.…”

“…The sample mixture was then placed onto the face of a potassium bromide (KBr) disk, and the second window was placed on top of the first salt plate to form a thin film of the mull by compression between two plates. The sandwiched plates were placed in the spectrometer, and the spectra were obtained by scanning between wave numbers 4000-400 cm -1 using potassium bromide discs [17].…”

“…Aliquot samples of 10 ml were withdrawn at prescheduled intervals (0.5, 1, 2, 4, 6, 8, 10, and 12 hr) and replaced with an equal volume of fresh dissolution medium which was kept at 37 ± 0 5 °C to maintain sink condition. Then, it was filtered (membrane pore filter 0.45 μm) and diluted suitably and analyzed for the drug content at the scanned λ max (234.75 nm) using a UV/ visible spectrophotometer [8,17,22] (9) Drug Release Kinetics and Mechanism. The dissolution data were fitted into different equations of drug release kinetic models to evaluate the rate and mechanism [10,23] of furosemide release from prepared floating matrix tablets.…”

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“…Then dissolved in buffer solution with the help of stirrer and filtered. The filtrate is assayed by UV spectrophotometer at particular wavelength by using calibration curve [34][35] .…”

Design and Optimizations of Aceclofenac Bioadhesive Extended Release Microspheres

“…For many decades, medication of an acute disease or a chronic disease has been accomplished by delivering drugs to the patients via various pharmaceutical dosage forms like tablets, capsules, pills, creams, ointments, liquids, aerosols, injectable and suppositories as carriers [1]. To achieve and then to maintain the concentration of drug administered within the therapeutically effective range needed for medication, it is often necessary to take this type of drug delivery systems several times in a day.…”