DEVELOPMENT AND MICROMERITIC EVALUATION OF FLOATING GRANULES OF CINNARIZINE

Aman Mittal*, Ritu Saini and Gaurav Kumar

ABSTRACT

The objective of study was to design and optimized a controlled release system of cinnarizine to increase its bioavailability by increasing the residence time in the stomach without contact with the mucosa and was achieved through the preparation of floating granules by melt granulation and melt solidification techniques. Cinnarizine, a H1-receptor antagonist, prescribed medication for the treatment for vestibular vertigo disorders and motion sickness was chosen as the drug candidate to be formulated as gastro retentive multiparticulate system as it is a weekly basic drug with a short half life of 5 hrs, showing gastric pH dependent bioavailability. Gelucire 43/01 was selected as a lipid carrier in different ratio (1:0.5, 1:1, 1:1.5) along with drug. The formulation F1 to F9 were prepared and evaluated for dependent variable (in vitro floating ability) and formulation F4 to F9 were evaluated for micromeritic properties, drug content and percentage yield, in-vitro drug release, percentage in-vitro floating ability and formulation F5 was selected as optimized formulation that exhibited good floating ability. In conclusion, hydrophobic lipid, Gelucire 43/01 can be considered as an effective carrier for design of a multiple unit floating drug delivery system of cinnarizine.

Keywords: Cinnarizine; Bioavailability; Floating; Hydrophobic.