Abstract
Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.
Highlights
The oral route is the most convenient and extensively used route for drug administration in the body
Various approaches have been hypothesized to control the residence of DDS in the upper part of the gastrointestinal tract (GIT) such as the incorporation of passage delaying food agents, ion exchange resins, raft system, high-density DDS, floating drug delivery systems (FDDS), swelling or expandable DDS and mucoadhesive DDS [5, 6, 22]
The benefit of gastric retention is for those drugs that are absorbed in the proximal portion of the GIT, and the drugs that are having a solubility less or a dip in the alkaline pH may advantage of gastric retention [8]
Summary
The oral route is the most convenient and extensively used route for drug administration in the body. The common property of conventional controlled release (CR) technologies is that a large part of the drug load is released in the colon, where the dosage form stays for a relatively long period. This delivery approach, while desirable for many molecules, was found to be inappropriate for drugs that are poorly absorbed from the lower portion of the GIT. Drug delivery to the proximal small intestine and local and sustained drug delivery to the abdominal to treat certain diseases, extending gastric retention of the therapeutic substance may offer several benefits including enhancement of therapeutic efficacy and possible reduction of the dose size, improved bioavailability [9]. Compare to all the DDS the FDDS have a bulk density is lesser than gastric fluids and so linger buoyant in the stomach without disturbing GE rate for an extended period of time [22]
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