Abstract
Purpose: To design and prepare effervescent floating gastroretentive tablets for controlledfexofenadine hydrochloride (HCl) release and enhanced oral bioavailability.Method: Various tablet formulations of the drug were prepared by direct compression. A systematic approach in the design of the formulations was adopted, where, first, formulations consisting of single polymers with a high polymer : sodium bicarbonate ratio were investigated for its physicochemical properties (in-vitro floating behaviour, drug release profile, etc). Next, improvement of tablets’ properties was achieved by decreasing polymer : sodium bicarbonate ratio. Subsequently, a final optimization step involved blending polymers at different polymer : polymer ratios. The formulations were evaluated in vitro and in vivo in albino rabbitsResults: The formulation consisting of hydroxypropyl methylcellulose K15M/hydroxypropylmethyl cellulose K100LV at 1 : 2 ratio (F8) showed good floating properties (14 s floating lag time) with nearly zero order controlled drug release for 24 h (R2 = 0.9876). In-vivo bioavailability studies of F8 in albino rabbits showed a significant increase in area under the curve (AUC, 134 %, p < 0.05) and hence an improvement in its oral bioavailability, compared to a commercial conventional product.Conclusion: The good quality of the effervescent floating gastroretentive tablets of fexofenadine HCl developed is an indication that the approach used is suitable for the formulation of the drug for controlled drug release and enhanced oral bioavailabiliy.Keywords: Effervescent, Floating, Gastroretentive, Fexofenadine, Bioavailability
Highlights
Oral controlled drug delivery systems (OCDDS) have gained much attention for many years, as they offer several advantages over conventional drug delivery systems
The bioavailability of the formulation was compared with that of a conventional marketed syrup, where the results revealed an increase in the oral bioavailability of the drug by 3.76 folds [10]
Formulations based on single polymers and comprising 125 mg polymer and 25 mg sodium bicarbonate per tablet (F1 - F4) showed a significant variation in their floating properties
Summary
Oral controlled drug delivery systems (OCDDS) have gained much attention for many years, as they offer several advantages over conventional drug delivery systems. It was previously reported that GRDDS have improved the bioavailability of many drugs, such as riboflavin, L-dopa, verapamil HCl, and captopril, by controlling their release in the upper small intestine [2]. A microemulsion of Fex HCl was formulated in an attempt to improve its absorption. Effervescent floating GRDDS of Fex HCl was designed for the first time as an alternative to conventional tablets, in an attempt to control drug release over 24 h, enhance drug absorption from the proximal small intestine, and improve its bioavailability. The in-vivo floating study was carried out by administering the tablet to an overnight fasted albino rabbit (2.25 kg) with 30 mL of water. The release of Fex HCl from tablet formulations (F1 - F12) was studied using USP dissolution apparatus II. The significance of the difference between the mean AUCs and the mean AUCmp was analyzed by applying t-test, where a p value of less than 0.05 was considered statistically significant
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