Factorial study on influence of gas generating agent and diluent on drug release kinetics of clopidogrel bisulfate floating tablets

Main Article Content

K. R. Koteswara Rao
K. Rajya Lakshmi
T. E. G. K. Murthy
A. Sivarama Prasad


The purpose of present work was to formulate and characterize a floating drug delivery system for Clopidogrel
bisulphate to improve bioavailability and to minimize the side‑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 Korsmeyer‑Peppas equation, the release exponent “n†ranged 0.455‑0.654 indicating that drug release from all the
formulations was by non‑fickian diffusion mechanism.
Key words: Clopidogrel bisulfate, factorial study, floating tablets, release kinetics, variables


Download data is not yet available.

Article Details

How to Cite
Rao, K. R. K., Lakshmi, K. R., Murthy, T. E. G. K., & Prasad, A. S. (2014). Factorial study on influence of gas generating agent and diluent on drug release kinetics of clopidogrel bisulfate floating tablets. Asian Journal of Pharmaceutics (AJP), 7(4). https://doi.org/10.22377/ajp.v7i4.336


Swarbrick J. Encyclopedia of Pharmaceutical Technology. 3rd ed., Vol. 2.

New York: Informa Healthcare; 2007. p. 1082‑103.

Kawashima Y, Takeuchi H, Yamamoto H. Handbook of Pharmaceutical

Controlled Release Technology. New York: Marcell Dekker Inc.; 2000.

p. 505‑25.

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;54:193‑204.

Lachman L, Lieberman HA, Kanig JL. The Theory and Practice of

Industrial Pharmacy. 3rd ed. Bombay: Varghese Publication House;

p. 171‑96.

General Chapters. Pharmaceutical dosage forms – Powders.

USP29‑NF24. United States (U.S): Pharmacopeia; 2008‑10. Available

from: http://www.pharmacopeia.cn/v29240/usp29nf24s0_c1151s56.

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