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Merck

Formulation and evaluation of swellable and floating gastroretentive ciprofloxacin hydrochloride tablets.

AAPS PharmSciTech (2009-03-12)
Ramji Anil Kumar Arza, Chandra Sekhara Rao Gonugunta, Prabhakar Reddy Veerareddy
RESUMEN

Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Swellable, floating, and sustained release tablets are developed by using a combination of hydrophilic polymer (hydroxypropyl methylcellulose), swelling agents (crospovidone, sodium starch glycolate, and croscarmelose sodium) and effervescent substance (sodium bicarbonate). Formulations are evaluated for percentage swelling, in vitro drug release, floating lag time, total duration of floating, and mean residence time (MRT) in the stomach. The drug release of optimized formulation follows the Higuchi kinetic model, and the mechanism is found to be non-Fickian/anomalous according to Krosmeyer-Peppas (n value is 0.68). The similarity factor (f (2)) is found to be 26.17 for the optimized formulation, which the release is not similar to that of marketed produced (CIFRAN OD). In vivo nature of the tablet at different time intervals is observed in the radiographic pictures of the healthy volunteers and MRT in the stomach is found to be 320 +/- 48.99 min (n = 6). A combination of HPMC K100M, crospovidone, and sodium carbonate shows the good swelling, drug release, and floating characters than the CIFRAN OD.

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USP
Sodium Starch Glycolate Type A, United States Pharmacopeia (USP) Reference Standard