DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE FLOATING TABLETS OF DOMPERIDONE MALEATE AND FAMOTIDINE USING HYDROPHILIC POLYMER MATRIX.

Abstract

Background Gastroretentive dosage forms are designed to remain in the stomach for an extended period and may improve drug delivery when absorption is favored in the upper gastrointestinal tract or is influenced by gastrointestinal pH. Domperidone maleate and famotidine are used in the management of upper gastrointestinal disorders and associated symptoms. Their incorporation into a sustained-release floating matrix may provide prolonged gastric residence and extended drug release compared with conventional immediate-release administration. Objective The study was undertaken to formulate, optimize, and evaluate a gastroretentive floating matrix tablet containing domperidone maleate and famotidine with prolonged buoyancy and sustained drug-release characteristics. Materials and Methods Twelve formulations (F1–F12) were developed by wet granulation, employing hydroxypropyl methylcellulose HPMC K4M and HPMC K15M as matrix-forming polymers and sodium bicarbonate as the effervescent gas-generating component. Preformulation investigations comprised melting-point determination, solubility assessment, FTIR characterization, and evaluation of drug–excipient compatibility. A UV spectrophotometric procedure was employed for simultaneous quantification of the two drugs. The granules and compressed tablets were evaluated for pre- and post-compression quality attributes, respectively. Floating lag time, total floating duration, swelling index, drug content, in vitro dissolution behavior, release kinetics, and accelerated stability were also investigated. Results The FTIR profiles showed no major spectral changes suggestive of incompatibility between the drugs and selected excipients. The prepared blends exhibited acceptable flow characteristics, while the resulting tablets showed satisfactory physical and pharmaceutical quality attributes. Based on the combined assessment of tablet properties, buoyancy, swelling, and dissolution behavior, F11 was identified as the optimized formulation. The HPMC K4M/HPMC K15M-based F11 formulation exhibited a short floating lag period and maintained buoyancy for more than 12 h. At the end of 12 h, cumulative drug release reached 93.26% for domperidone maleate and 97.62% for famotidine. Kinetic analysis indicated predominantly first-order release behavior with a non-Fickian release mechanism. No substantial alterations in the evaluated quality characteristics were observed during accelerated stability testing. Conclusion The optimized F11 formulation provided prolonged floating behavior together with sustained release of both domperidone maleate and famotidine over 12 h. The findings demonstrate the feasibility of incorporating the two drugs into a gastroretentive floating matrix tablet and provide a basis for further pharmaceutical and in vivo evaluation. One important scientific change: I would avoid stating that the formulation “successfully achieved prolonged gastric retention” unless an in vivo gastric-retention study (e.g., imaging) was actually conducted. An in vitro floating study demonstrates prolonged buoyancy, not direct evidence of gastric retention in humans or animals.