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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Preparation of Tiagabine HCl/2-HPβCD Complex Pellets by Extrusion-Spheronization Using Glycerol Monostearate as Pellet-Aid

Author(s): Abdussalam Sughir, Malika Lahiani-Skiba and Mohamed Skiba

Volume 7, Issue 1, 2010

Page: [63 - 69] Pages: 7

DOI: 10.2174/157018010789869389

Price: $65


Glycerol monostearate was used as a pellet-aid to prepare tiagabine HCl/2-HPβCD inclusion complex pellets (an antiepileptic agent partially included into the 2-HPβCD cavity to improve its stability). The pellitization of tiagabine HCl/2-HPβCD inclusion complex (1:1 stoichiometric composition) using 27.3% of melted GMS (60°C) in its liquid form as wetting agent, 30% of microcrystalline cellulose (pellet-forming agent) and 3% of kollidone-30 (binder) was studied. Pellitization was prepared using extrusion/spheronization method. > b 80% of pellets, size ranging between 800-1000μm, were obtained indicating a significant pellet yield. The disintegration test of the pellets complied with the Eur. Ph. Limit (0.8%). The TGB pellets formed were better sized and spherically shaped than when GMS was used in its liquid form. Pellets obtained using tiagabine HCl/2-HPβCD inclusion complex after addition of GMS with very little water content ( < 5%) have also a spherical shape, retain their integrity in dissolution medium, which suggested that coatings will not burst prematurely due to granule swelling and release their TGB load rapidly 65-85% in 15min in a phosphate buffered dissolution medium.

Keywords: Tiagabine, Cyclodextrins, Glycerol Monostearate, Pellets, Extrusion-Spheronization

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