Formulation and Comparative In-Vitro/In-Vivo Evaluation of Floating Gastroretentive Tablets Versus Conventional Tablets of Famotidine for Prolonged Gastric Residence Time and Improved Bioavailability in Peptic Ulcer Management

Sandeep Sharma

Department of Industrial Pharmacy, Manipal College of Pharmaceutical Sciences (MCOPS), Manipal (Karnataka)

1. Abstract

Peptic ulcer disease (PUD) continues to be a widespread gastrointestinal condition that contributes significantly to global morbidity and healthcare costs. Famotidine, a histamine H₂-receptor blocker, is frequently used to treat gastric and duodenal ulcers due to its strong ability to suppress acid. Nonetheless, traditional oral forms of famotidine have drawbacks such as low bioavailability (around 40–45%), a short biological half-life (2.5–4 hours), and inconsistent absorption due to rapid gastric emptying and site-specific uptake in the upper gastrointestinal tract. These issues require frequent dosing and diminish therapeutic effectiveness. Gastroretentive drug delivery systems (GRDDS), especially floating gastroretentive tablets, have been developed as promising methods to extend gastric retention time, sustain effective drug levels in the stomach, and improve bioavailability. This research article thoroughly formulates and compares floating gastroretentive tablets with conventional immediate-release famotidine tablets. The floating tablets were crafted using hydrophilic polymers (HPMC K4M, HPMC K15M, Carbopol 934P) and gas-generating agents (sodium bicarbonate and citric acid) to achieve buoyancy and prolonged drug release. The formulations underwent detailed pre-compression and post-compression assessments, including evaluations of flow properties, hardness, friability, drug content uniformity, swelling index, buoyancy lag time, total floating duration, and in-vitro dissolution studies. Additionally, pharmacokinetic and in-vivo bioavailability comparisons were simulated using existing data to evaluate improved therapeutic outcomes in managing peptic ulcers. The findings revealed that floating gastroretentive tablets exhibited extended buoyancy (>12–24 hours), sustained drug release (up to 24 hours), and significantly increased gastric residence time compared to conventional tablets. In-vivo assessments indicated enhanced plasma concentration profiles and prolonged therapeutic effects, suggesting improved bioavailability and reduced dosing frequency. Overall, the floating gastroretentive formulation of famotidine offers a promising approach to enhancing ulcer healing, patient adherence, and therapeutic effectiveness in the management of peptic ulcer disease.

2. Keywords

Famotidine; Gastroretentive Drug Delivery System; Buoyant Tablets; Peptic Ulcer Disease; Bioavailability; Gastric Retention Duration; Prolonged Release; HPMC; Pharmacokinetics; In-Vitro and In-Vivo Assessment.