Acta Pharm. 58 (2008) 187-197
Original research paper
Formulation and evaluation of oil entrapped
gastroretentive floating gel beads of loratadine
SHASHI
KIRAN MISHRA and KAMLA PATHAK
kamla_rap@yahoo.co.in
1Advanced
2Department
of Pharmaceutics,
Accepted March 17, 2008
A gastro retentive controlled release system of loratadine was
formulated to increase the residence time in stomach and to modulate the
release behaviour of the drug. Oil entrapped floating microbeads prepared by
the emulsion gelation method were optimized by 23 factorial design
and a polymer ratio of 2.5:1.5 (pectin:sodium alginate) by mass, 15% (m/V) of oil (mineral oil or castor oil)
and 0.45 mol L-1 calcium chloride solution were
selected as the optimized processing conditions for the desired buoyancy and
physical stability. In vitro drug
release in fed state conditions demonstrated sustained release of loratadine
for 8 h, which best fitted the Peppas model with n < 0.45. The ethylcellulose coating on microbeads optimized by
22 factorial design resulted in a controlled release formulation of
loratadine that provided zero-order release for 8 h.
Keywords: loratadine, gastroretentive,
factorial design, ethylcellulose coating, zero-order release