Abstract
The aim of this study was to enhance the solubility and dissolution rate of sulfamethoxazole (SMZ) by preparing the inclusion complexes with β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HPβ-CD) and γ-cyclodextrin (γ-CD). The effect of the type of cyclodextrins used for the preparation of complexes, on the in vitro dissolution profiles and solubilities in different mediums (pH 4.5 and 7.0) was also evaluated. The interaction between SMZ and cyclodextrins in solution was studied by the phase-solubility method. Inclusion complexation was confirmed by the results from the studies of infrared spectoroscopy (IR) and differential scanning calorimetry (DSC). The effect of water-soluble polymers, that is, polyethylene glycols 4000, 10000, 20000 and non-ionic surfactants, that is, polysorbate 20, 40 and 60 on the complexation of SMZ with CDs were also investigated by the same methods. The rates of release of the active material from the complexes were determined from dissolution studies using USP XXII paddle method. As a result of this study, it was found that the solubility of SMZ was significantly enhanced by inclusion of β-CD, especially when the water soluble additives are added (from 0.086 to 0.377 mg/ml with SMZ:β-CD:PEG20000). Key words: Cyclodextrins, sulfamethoxazole, solubility, dissolution rate.
Highlights
Sulfonamides are bacteriostatic agents which are systematically used in the treatment of bacterial infections
Inclusion complexation was confirmed by the results from the studies of infrared spectoroscopy (IR) and differential scanning calorimetry (DSC)
Sulfamethoxazole (SMZ) was obtained from Fako Medical (Turkey); in addition, the following were used in the study: β-cyclodextrin, hydroxypropyl-β-cyclodextrin (HPβ-CD), γ-cyclodextrin (γ-CD) (Fluka), polyethylene glycol 4000 (PEG4000), polyethylene glycol 10000 (PEG10000), polyethylene glycol 20000 (PEG20000), hydroxypropyl methylcellulose (HPMC) polysorbate 20 (PS20), polysorbate 40 (PS40) and polysorbate 60 (PS60) (Merck)
Summary
Sulfonamides are bacteriostatic agents which are systematically used in the treatment of bacterial infections. SMZ, a derivative of sulfonamide, inhibits the synthesis of folic acid, which is an important metabolite of bacteria’s DNA synthesis (Martindale, 1993; Raja et al, 2009). SMZ is absorbed from gastro-intestinal area; its absorption and bioavailability are limited with its dissolution rate, due to its low solubility like all the other sulfonamide groups. The aim of the study was to prepare the inclusion complexes of SMZ using CDs to enhance the solubility, dissolution rate and oral bioavailability. The commonly available CDs are α-, β- and γ-
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
