Main Article Content
bisulphate to improve bioavailability and to minimize the sideâ€‘effects of the drug such as gastric bleeding and drug
resistance development. Clopidogrel floating tablets were prepared by direct compression technique by the use of xanthan
gum at different concentrations (20%, 25% and 30% w/w). Sodium bicarbonate (15% w/w) and microcrystalline
cellulose (MCC) (30% w/w) were used as gas generating agent and diluent respectively. The effects of sodium bicarbonate and
MCC on the drug release kinetics and floating properties were investigated. A 22 factorial design was applied systematically
to optimized formulation. The percentage amount of sodium bicarbonate (X1) and percentage amount of MCC (X2) were
selected as independent variables. The drug release rate constant (K) and time required for 85% drug dissolution (T85) was
selected as dependent variables. Factorial design revealed that the percentage amount of sodium bicarbonate and MCC had
insignificant effect on drug release kinetics (K, T85) within the chosen levels and a high level of sodium bicarbonate (X1) and
the low level of MCC (X2) favor the preparation of clopidogrel floating tablets. All the Clopidogrel floating formulations
followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As
per Korsmeyerâ€‘Peppas equation, the release exponent â€œnâ€ ranged 0.455â€‘0.654 indicating that drug release from all the
formulations was by nonâ€‘fickian diffusion mechanism.
Key words: Clopidogrel bisulfate, factorial study, floating tablets, release kinetics, variables
This is an Open Access article distributed under the terms of the Attribution-Noncommercial 4.0 International License [CC BY-NC 4.0], which requires that reusers give credit to the creator. It allows reusers to distribute, remix, adapt, and build upon the material in any medium or format, for noncommercial purposes only.
Swarbrick J. Encyclopedia of Pharmaceutical Technology. 3rd ed., Vol. 2.
New York: Informa Healthcare; 2007. p. 1082â€‘103.
Kawashima Y, Takeuchi H, Yamamoto H. Handbook of Pharmaceutical
Controlled Release Technology. New York: Marcell Dekker Inc.; 2000.
Drug Bank. Canada: Open data drug and Drug target database,
Clopidogrel. Available from: http://www.drugbank.ca/drugs/
DB00758. [Last updated on 2013 Jul 15; Last cited on 2013 Jul 20].
Patel PR, Kothari JS, Roy SB. Modified release clopidogrel formulation.
Patent US20100145053 A1, 2010, Jun, 10.
Koradia V, Chawla G, Bansal AK. Qualitative and quantitative analysis
of clopidogrel bisulphate polymorphs. Acta Pharm 2004;54:193â€‘204.
Lachman L, Lieberman HA, Kanig JL. The Theory and Practice of
Industrial Pharmacy. 3rd ed. Bombay: Varghese Publication House;
General Chapters. Pharmaceutical dosage forms â€“ Powders.
USP29â€‘NF24. United States (U.S): Pharmacopeia; 2008â€‘10. Available
html. [Last cited on 2013 May 15].
Rosa M, Zia H, Rhodes T. Dosing and testing in vitro of a bioadhesive
and floating drug delivery system for oral application. Int J Pharm
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on
drug release from controlled drug delivery systems. Acta Pol Pharm