Affiliation:
1. Department of Pharmaceutics, Dubai Pharmacy College for Girls, Muhaisnah-1, Dubai
Abstract
Background:
Gastroretentive drug delivery systems (GRDDSs) are designed to release the
drug in the stomach over a prolonged time; thus, they can reduce drug dosing frequency and dose size
and improve patient compliance. GRDDSs are also highly effective in enhancing the bioavailability of
the drug that exhibits window absorption in specific segments of the gastrointestinal (GI) tract. Famotidine
(FMT), an H2 receptor antagonist, is an example of these drugs. FMT is a slightly watersoluble
drug but well soluble in an acidic medium. This research aims to formulate FMT gastroretentive
floating tablets (FMT-GRFTs) to improve the bioavailability and therapeutic activity of the
drug and increase patients' adherence to treatment. In addition, the in vitro release behavior of the prepared
FMT-GRFTs was quantitatively analyzed using the DDSolver software to assist in selecting the
successful formulation that was then evaluated in vivo.
Methods:
The direct compression technique prepared numerous tablet formulations and was subjected
to the pre-and post-compression evaluation. Data of FMT dissolution in the simulated gastric medium
was analyzed by various kinetic models built in the DDSolver program. In addition, the simulated
pharmacokinetics (AUC, MDT, and MRT), R2 adjusted, AIC, MSC, correlation of the residuals, and
similarity factor (f2) were also generated.
Results:
The results revealed that FMT release from the candidate formula (FH3) fitted to the first-order
kinetic model, with a high value of R2 adjusted and MSC and a low AIC. The release behavior exhibited
the Fickian diffusion mechanism. The similarity factor showed no significant difference (p < 0.05) of
the test sample compared to the reference product. Nevertheless, the simulated pharmacokinetic parameter,
AUC, proved a two-fold enhancement in FMT bioavailability, with a significant increment in the
MDT and MRT compared with the reference product. The FT-IR spectroscopy analysis indicated the
absence of drug-excipients/polymer interaction. The in vivo X-ray studies on rabbits confirmed that the
floating tablets showed nearly eight hours of gastric residence.
Conclusion:
DDSolver software was helpful in deciding the optimized formulation of FMT floating
tablets. The radiological examination in rabbits for gastric retention was consistent with the release data
analysis in vitro.
Publisher
Bentham Science Publishers Ltd.
Cited by
3 articles.
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