Design and preparation of controlled floating gastroretentive delivery systems for enhanced fexofenadine hydrochloride oral bioavailability

Abstract

Purpose: To design and prepare effervescent floating gastroretentive tablets for controlled fexofenadine 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 rabbits Results: The formulation consisting of hydroxypropyl methylcellulose K15M/hydroxypropyl methylcellulose 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 (R 2 = 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. This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest

Preparation, Characterization and Evaluation of Flavonolignan Silymarin Effervescent Floating Matrix Tablets for Enhanced Oral Bioavailability

“…The system’s overall density reduced as a result of the developed gas being trapped, and there was an instantaneous floating of the tablets [ 42 ]. These findings agreed with past research that suggested that larger levels of the effervescent agent led to enhanced gas generation and, subsequently, quicker floating [ 43 ]. Due to the fact that the effervescence reaction only happens when the tablet makes its initial contact with the dissolved media, it has been demonstrated that the amount of the effervescent agent only serves to improve the FLT, and the viscosity of the polymer will be the controlling element for the TFT [ 44 ].…”

“…A shorter FLT is also a result of the presence of a low-viscosity polymer (HPMC K4M), which causes an initial quick and larger drug release from the pores generated by gel formation. Next, the formation of strong gel owing to the higher-viscosity polymer controls the drug release, further contributing to the longer TFT, i.e., 12 h [ 43 ]. This may be the most likely reason for the observed drug release behavior.…”

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“…It was observed from the results that there was no significant change in the lab values of control and treated group. No sign & symptoms of toxicity were appeared during seven days of toxicity study so it was concluded that the prepared microspheres were safe [25].…”

Advances in the Preparation Techniques of Floating Microspheres with Exploration of AI Tool in Product Development

“…In this region, the shear stress is minimal, providing valuable insights into the obtained results. It should be noted, however, that this artificial setup may yield more informative measurements but might not accurately reflect in-vivo behavior due to its limited physiological relevance [70,71].…”