Abstract
The aim of the present investigation was to formulate and evaluate floating-bioadhesive tablets of amoxicillin trihydrate (ATFBT), to provide local action in the treatment of Helicobacter pylori (H. pylori) by prolonging the gastric residence time. The FBT were prepared by direct compression method using hydroxy propyl methyl cellulose (HPMC K4M) / chitosan (CH), carbopol (CP974P) / polymethacrylic acid (PMA) as release retarding agent / bioadhesive respectively, sodium bicarbonate (NaHCO3) as a gas-former. The prepared tablets were evaluated for their physical characters such as drug content, in vitro buoyancy, swelling index, drug release and stability. Further, the bioadhesive strength (BS) was determined using porcine gastric mucosa. DSC studies indicate the compatibility of the drug and excipients used in the formulation. The floating lag time, total floating time, bioadhesive strength and swelling index of the optimized formulation (F7) was 32 ± 2.7 sec, more than 12 h, 1.86 ± 0.14 N and more than 3.5 respectively. Formulation (F7) was also found to be physically stable when stored at 40oC / 75% RH for 3 months. The drug release profiles of all the formulations were fitted into various kinetic models. The optimized formulation followed the Peppas model (r2 > 0.99) with a non-Fickian diffusion mechanism (n = 0.625). From the results, a matrix floatingbioadhesive tablet incorporating an insoluble active substance such as amoxicillin trihydrate was developed for the successful eradication of H. pylori.
Highlights
Helicobacter pylorus (H. pylori) is a bacterium that causes chronic inflammation in the stomach and is a common cause of ulcers worldwide
The treatment of H. pylori remains a challenging proposition; it is highly sensitive to most antibiotics, difficult to eradicate from human body even with the current best therapies
Conventional formulations such as immediate release tablets are used for eradication therapy, but they do not remain in the stomach for longer time
Summary
Helicobacter pylorus (H. pylori) is a bacterium that causes chronic inflammation in the stomach and is a common cause of ulcers worldwide. In order to extend the gastric residence period, gastro retentive drug delivery systems have been developed, which is an approach to prolong gastric residence time and to provide site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects [9]. These include high density (sinking) systems, low density (floating) systems, mucoadhesive systems, swelling and expanding systems, modified shape systems, [10], floating-bioadhesive drug delivery systems [11] and other delayed gastric emptying devices which would improve the therapeutic effects of many drugs
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