Abstract
AbstractPreparation of inclusion complex using cyclodextrins is a well-known formulation strategy to elevate the solubility of drugs. However, often cyclodextrins alone may not bring a considerable improvement in the solubility of low solubility drugs. In this study, the inclusion complexation of furosemide (FSM) was tried with β-cyclodextrin (β-CD) either with the use or without the use of sodium lauryl sulfate (SLS), which is a surfactant. By using the kneading method, the binary complex of FSM/β-CD in the equal molar ratio was used. FSM and β-CD were kneaded continuously until a thick past was achieved, which was evaporated for a period of about 24 h. The solid complexed product was then crushed and stored in airtight container until use. Phase solubility studies confirmed a stoichiometric ratio of 1:1 (FSM/β-CD and FSM/β-CD with SLS). The apparent stability constant and complexation efficiencies of significantly enhanced in the presence of SLS. The prepared complexes were evaluated for DSC, PXRD, 1H NMR, and in vitro release studies. The results exhibited a significant enhancement in diuresis in rats. It is evident that the addition of SLS with β-CD significantly enhances the solubilizing efficiencies and hence bioavailability of FSM.
Highlights
Furosemide (FSM) is one of the potent sulfonamide diuretics; it belongs to a loop diuretic group
Many studies reported the ability of CD complexation to improve water solubility, especially for hydrophobic drugs [15]
complexation efficiency (CE) was considered as more reliable data for complexation
Summary
Furosemide (FSM) is one of the potent sulfonamide diuretics; it belongs to a loop diuretic group. According to the BCS (Biopharmaceutics Classification System), FSM is labeled in Class IV drug because of both its limited aqueous solubility (5–20 μg/mL) and low permeability; it has limited bioavailability (60–65%) and an erratic pharmacokinetic profile [12,13,14]. Many studies reported the ability of CD complexation to improve water solubility, especially for hydrophobic drugs [15]. Inclusion complexation with β-CD is a well-known method to improve the water solubility of water-limited solubility drugs and, its stability, the kinetics of dissolution, and bioavailability [18]
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