Effect of pluronic gels on the rectal absorption of indomethacin in rabbits.

Abstract

Indomethacin gel preparations made by dissolving the drug in Pluronic aqueous gels were administered rectally to rabbits and the drug plasma levels were determined. When indomethacin gel preparations with 20% (w/w) Pluronic F-127 were given to rabbits, the plasma concentration reached the maximum level 0.5 h after administration. On the other hand, the 25% (w/w) Pluronic F-127 gel preparation did not show a sharp peak of plasma concentration and produced a sustained-release effect. The 30% (w/w) gel preparation also gave a sustained-release effect, but it was not a desirable preparation because its [A U C]100 was only half that of a commercial suppository. Pluronic F-108 and Pluronic F-98 did not give a sustained-release effect at the concentration of 25% (w/w).Damage to the mucosal membrane by Pluronic F-127 was rarely found in the rectum. In addition, the individual differences in drug plasma levels following rectal administration of the 25% (w/w) Pluropic F-127 gel preparation were small compared with those of other preparations.These results suggest that the 25% (w/w) Pluronic F-127 gel is most suitable for use as a vehicle for rectal administration of indomethacin with prolonged action and with reduced side effects.

In Vitro Evaluation of Pluronic F127-Based Controlled-Release Ocular Delivery Systems for Pilocarpine

“…2 Another study reported that a PF127 suppository formulation of indomethacin was the most suitable of three pluronics tested in rabbits due to its prolonged action and minimal side effects. 3 A PF127-based dental gel, Protect (Butler Brush), has been in use several years for treating patients with sensitive gums and teeth. 4 The PF127 gel was first used clinically as a vehicle for silver salts to treat topical burns.…”

Preparation and investigation of acetyl salicylic acid-caffeine complex for rectal administration

“…Then, the slices were stained with hematoxylin-eosin and observed under a light microscope (Leitz Laborlux 12 Pols; Ernst Leitz GmbH, Wetzlar, Germany). [28,29] The changes in rectal tissues were evaluated blindly using an inflammation changes scores scale reported by Møller et al [30] The scale was categorized as follows: score 0, no signs of inflammation; score 1, slight infiltrations in lamina propria by mononuclear cells; score 2, moderate mononuclear cell infiltration of lamina propria, increased mitotic activity in lamina epithelialis; score 3, as in 2 but patchy mononuclear cell infiltration in the tela submucosa; score 4, as in 3, but some crypt destruction and epithelial metaplasia. …”

Physicochemical Characterization of Diclofenac Sodium-Loaded Poloxamer Gel as a Rectal Delivery System with Fast Absorption

“…[12] The entrance of the anus was then blocked with a cyanoacrylate adhesive, since the preparations might leak out from the anus during the pharmacokinetic experiment, leading to inaccurate pharmacokinetic data. A polyethylene tube was inserted into the right femoral artery of the rat.…”