Case studies in swelling polymeric gastric retentive tablets

Abstract

Swelling tablets administered in the fed state have been shown to provide therapeutic advantages in two marketed products, with the duration of delivery characterised with respect to food and tablet size. Metformin extended-release tablets are a diffusion-based swelling tablet demonstrating once-daily efficacy with good gastrointestinal solubility. Ciprofloxacin extended-release tablets are based on an erosional matrix that delivers the drug to the upper gastrointestinal tract over 6 h to provide once-daily efficacy with reduced incidences of nausea and diarrhoea. Furosemide extended-release tablets are another example of an erosional matrix designed to deliver furosemide to the duodenum and upper jejunum over 6 h to provide a more gradual diuresis and naturesis compared with the immediate-release product.

Phase 3 randomized controlled study of gastroretentive gabapentin for the treatment of moderate-to-severe hot flashes in menopause

“…While they are in the stomach, G-GR tablets provide a steady and continuous delivery of gabapentin to its optimal site of absorption in the upper small intestine. 11,12 Consequently, the plasma concentration of gabapentin following G-GR administration twice per day with a meal dosed twice per day asymmetrically (600 mg AM/1,200 mg PM), results in exposure comparable to that of 1,800 mg/day immediate-release gabapentin administered as 600 mg three times a day. 10,13 The slower release afforded by the gastroretentive formulation seems to enhance tolerability and permits a more rapid titration to an efficacious dose.…”

Tolerability and safety of gastroretentive once-daily gabapentin tablets for the treatment of postherpetic neuralgia

“…But given the extensive clinical history of gabapentin TID for the treatment of neuropathic pain and the established safety of the gastroretentive technology,17 it is reasonable to expect that the safety and tolerability of G-GR would be maintained for longer treatment periods. Another limitation of this analysis is that patients who had not previously responded to gabapentin at daily doses >1200 mg or who were intolerant to gabapentin were excluded.…”

A randomized, double-blind, placebo-controlled study of the efficacy and safety of MNK-795, a dual-layer, biphasic, immediate-release and extended-release combination analgesic for acute pain

“…OC/APAP ER tablets employ a dual-layer biphasic delivery mechanism that, when administered as a single dose (i.e., two tablets; 15 mg OC/650 mg APAP), is designed to deliver 3.75 mg OC/325 mg APAP through the IR component and 11.25 mg OC/325 mg APAP through the ER component. The ER delivery technology utilizes the Acuform drug delivery systemz containing hydrophilic polymers that release the active ingredients at a steady rate into the upper gastrointestinal tract over an extended period [30][31][32] . This technology may also contribute to potential tamperresistant and abuse-deterrent properties of OC/APAP ER, which was demonstrated in in vitro 33 and phase 1 studies 34 .…”