Abstract
The limitations in absorption of drugs with narrow absorption window, or those unstable in the intestinal pH or those exhibiting low solubility at high pH are primary candidates for gastroretentive drug delivery systems (GRDDS). The delivery system has been widely explored for its commercial potential for a wide variety of therapeutic agents. GRDDS offer clinical therapeutics for acute and chronic management. Hypertension is a chronic disease that requires long term treatment and its management by patient compliant dosage forms would be clinically useful. Antihypertensives belonging to different classes have proved good candidates for the formulation of GRDDS. The review aims to discuss various GRDDS researched for antihypertensive drugs to increase the gastric residing time, bioavailability, henceforth to reduce the dose of the drug, dosing frequency and increase patient compliance. It also explores various marketed products and the patents filed/granted for GRRDS of antihypertensives. The GRDDS investigated include effervescent and non-effervescent floating drug delivery systems, swelling and expanding systems and bio/mucoadhesive systems. Many other systems that provided research platforms include high density systems, raft forming systems and osmotic delivery systems. In clinical context, wherein combination of antihypertensives is indicated, dual release delivery systems may also be explored.
Highlights
The drug delivery systems for oral administration such as drug release rate-controlled delivery systems, time-controlled delivery systems and site-specific delivery systems have been extensively explored due to their significant therapeutic advantages
The review aims to discuss various gastroretentive drug delivery systems (GRDDS) researched for antihypertensive drugs to increase the gastric residing time, bioavailability, to reduce the dose of the drug, dosing frequency and increase patient compliance
The current controlled release technology has made it possible to release drugs at a constant release rate for longer periods of time ranging from days to years (Sato et al, 2003; Streubel, Siepmann, Bodmeier, 2006)
Summary
The drug delivery systems for oral administration such as drug release rate-controlled delivery systems, time-controlled delivery systems and site-specific delivery systems have been extensively explored due to their significant therapeutic advantages. The current controlled release technology has made it possible to release drugs at a constant release rate for longer periods of time ranging from days to years (Sato et al, 2003; Streubel, Siepmann, Bodmeier, 2006). This benefit has not satisfied a variety of important drugs that (i) are locally active in the stomach, (ii) have an absorption window in the stomach or in the upper small intestine, (iii) are unstable in the intestinal or colonic environment, and/ (iv) exhibit low solubilities at high pH values (Streubel, Siepmann, Bodmeier, 2006; Rocca, Omidian, Shah, 2003). These systems have been researched for a wide variety of therapeutic categories including antiulcer drugs, antibiotics, anti-diabetic drugs, cardiovascular drugs, drugs for gout and NSAIDS
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