Formulation
of Fast-Release Gastroretentive Solid Dispersion of
Glibenclamide with Gelucire 50/13
Prashant Upadhyay1* and Jayanta Kumar Pandit2
1Department of Pharmaceutics,
College of Pharmacy, I.F.T.M, Delhi Road,
Moradabad-244001 and Gautam Buddh Technical University,
Lucknow, 2Department of Pharmaceutics,
Institute of Technology, Banaras Hindu University,
Varanasi-221005, Uttar Pradesh, India
*For correspondence:
Email:
p23upadhyay@yahoo.com Tel: +91-9719915567,
5912360817; Fax: +91-5912360818
Received:
18 November
2011 Revised
accepted: 5 April 2012
Tropical
Journal of Pharmaceutical Research, June 2012;
11(3): 361-369
http://dx.doi.org/10.4314/tjpr.v11i3.4
Abstract
Purpose: Fast-release gastroretentive solid dispersions of
glibenclamide using gelucire were prepared to achieve
improved bioavailability.
Methods: Hot melt granulation technique was adopted to
prepare solid dispersions (SDs) of glibenclamide in
gelucire 50/13 and were compared with pure glibenclamide
and physical mixtures of drug and gelucire using hot stage polarized microscopy, powder x-ray
diffraction (PXRD), Fourier-transform infrared
spectroscopy FTIR, bouyancy as well as by in vitro
release and in vivo studies. Further aging studies were
carried out for the samples.
Results: PXRD showed that glibenclamide was present in SD
in an amorphous form while FTIR spectroscopy revealed
the presence of hydrogen bonding in the SDs. In vitro
buoyancy was found for 11 h and there was improvement in
solubility and dissolution rate for all test
formulations. Formulations were found to follow Zero
order kinetic. . During aging study, no decrease of in
vitro drug dissolution was observed over 3-month
period. Crystallinity in the SDs was observed following
aging. A more pronounced lowering of blood glucose level
in Wistar rats compared with the pure drug, suggests
that the test formulations are superior.
Conclusion: This study demonstrates the high potential of
hot melt technique for obtaining stable fast-release
gastroretentive solid dispersions of poorly water
soluble drug using polyglycolized glycerides as
carriers
Keywords: Glibenclamide, Gelucire, Solid dispersion,
Gastro-retentive multi-particulates, Hot melt technique.
