Development of sustained release formulation of an antithrombotic drug and application of fuzzy logic

Abstract

Clopidogrel bisulphate has quite low bioavailability (40–50%). It was aimed to increase its bioavailability by designing a controlled release dosage form of clopidogrel, which is different from available current dosage forms in the market. There are also some attempts to overcome patent protection of clopidogrel by combination of active substances or preparation of controlled release tablets. Therefore, it was also aimed to determine in vitro and in vivo properties of controlled release clopidogrel tablets. The amounts of releases from formulations were subjected computer program and effects of components in the formulation on release were investigated (INFORM v.3.7 and FORMRULES, Intelligensys Ltd). Two sustained release formulations and innovator product were selected and their effectiveness was compared by in vivo tests in rabbits. In conclusion, proposed controlled release formulations were found to be an alternative and to be more effective for longer periods than the commercial one.

Keywords::

• Clopidogrel
• sustained release
• antithrombotic drug
• modelling
• fuzzy logic
• artificial neural network modelling

Acknowledgments

This study was performed for Master degree thesis at Gazi University Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Turkey. The authors are thankful to the department for support, providing equipments, chemicals and giving an opportunity to work.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.