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STUDIES ON UREA CO-INCLUSION COMPLEXES OF EBASTINE FOR STEEP IMPROVEMENT IN DISSOLUTION PROFILE

Journal: Indian Drugs (Vol.54, No. 8)

Publication Date:

Authors : ; ;

Page : 35-45

Keywords : ;

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Abstract

Urea co-inclusion technique has been successfully utilized for steep enhancement in dissolution rate of ebastine (EB), a BCS class II potent drug. EB is a novel second generation H1 receptor antagonist used for prevention of chronic idiopathic urticaria and allergic rhinitis. It exhibits low aqueous solubility and consequent poor bioavailability. In the present study, EB was engulfed in urea channel/tunnels along with rapidly complexing agent (RCA). Resulting complexes of EB (EBUCIC) were characterized by DSC, FTIR, XRD and 1H-NMR. Minimum proportion of RCA for incorporation of EB in hexagonal urea was determined calorimetrically. The thermal studies indicated increase in heat of decomposition with increasing molar fraction of RCA in EBUCICs, ensuring better physical stability of complexes. Content uniformity study depicted uniform composition formulation of EB. Weibull model described release kinetics of EB. Enhancement in dissolution rate ensures urea co-inclusion to be a useful approach for development of rapid/instantaneous release dosage forms.

Last modified: 2017-09-07 16:23:45