Design, development and In vitro characterization of Clopidogrel bisulfate floating drug delivery system

Dwarakanadha Peram, Sreenivasulu Reddy Nagireddy, Swarnalatha Dugasani, Badarinath Attuluri Venkata, Ravikumar Reddy, Juturi
2015 Dwarakanadha Reddy Peram /J Compr Phar   unpublished
Floating drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increase the bioavailability. Orally Clopidogrel bisulfate has a short elimination half-life (7-8 hrs.), low oral bioavailability (50%) undergoes extensive first pass metabolism (85%) and frequent high doses (75 mg) are required to maintain the therapeutic level as a result, dose development toxic effect. The purpose of this research work was to formulation and evaluation of floating
more » ... ion of floating drug delivery system of Clopidogrel bisulfate using various polymers such as Agar, SCMC, and Eudragit RS-100 with different proportions by wet granulation technique. The FTIR study revealed no physical or chemical interactions between Clopidogrel bisulphate and exciepients. Partition co efficient present in between 2-6 for this drug so it is suitable for the floating tablets. The prepared formulations were evaluated for different physicochemical characteristics like thickness, hardness, drug content, percentage drug content, friability, and weight variation. The result of dissolution studies shows that formulation, F8 (Agar-20mg, SCMC-10mg and Eudragit RS-100-20mg) showed maximum release of 99.25 % in 12hrs, whereas F1 (Agar-50mg) showed minimum release of 96.26% in 8hrs. Based on the drug release and physicochemical values obtained the formulation F8 is considered as an optimized formulation which shows higher percentage of drug release of 98.82 % in 11 hr. The developed floating tablets increase the therapeutic efficacy and reduced toxic effect of Clopidogrel bisulfate.