spectra, disintegration and in-vitro drug release were evaluated. Due to .... Fig. (2). Modelisation of interactions between β-cyclodextrin polymer and nimesulide.
Letters in Drug Design & Discovery, 2008, 5, 000-000
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Release of a Poorly Soluble Drug from Cross-Linked -Cyclodextrin-Based Polymer Pellets Prepared via Extrusion/Spheronisation Pierre Bon1,2,†, Samer Joudieh1,†, Malika Lahiani-Skiba1, Frederic Bounoure1,2, Pierre Dechelotte3 and Mohamed Skiba*,1 1
Laboratoire de Pharmacie Galénique ADEN EA 3234 (IFR 23, institute for Biomedical research). 22 Bd Gambetta76000- Rouen- France 2
In-cyclo® - 22 Bd Gambetta- 76000- Rouen- France
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ADEN EA 3234 (IFR 23, Institute for Biomedical research). CHU of Rouen, 22 Bd Gambetta- 76000- Rouen- France Received: May 16, 2007; Revised: July 22, 2008; Accepted: July 28, 2008
Abstract: The aim of this study was to evaluate the use of a -cyclodextrin-based polymer, and more exactly a highly crosslinked cyclodextrin-based polyester, as an excipient to accelerate the release of poorly soluble drugs from pellets obtained by extrusion-spheronisation. The cross-linked -cyclodextrin based polymer was associated to microcrystalline cellulose to facilitate the process of extrusion/spheronisation, and nimesulide was chosen as a poorly soluble model drug. Different formulations with natural and -cyclodextrins, or a -cyclodextrin-based polymer associated to microcrystalline cellulose and 10 % (w/w) of nimesulide were compared. Yield between 800 and 1000 m, pellets dimensions and surface morphology by scanning electron microscopy (SEM), Fourier Transform - Infrared Spectroscopy (FT-IR) spectra, disintegration and in-vitro drug release were evaluated. Due to pellet disintegration, accelerated dissolution of nimesulide was achieved with -cyclodextrin-based polymer, i.e. 75±2% in 120 min vs. 12±1% for pellets with only microcrystalline cellulose (p
