Clopidogrel Case Study

Cardiovascular diseases (CVDs) is defined as a group of diseases that involve heart and blood vessels which including coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, congenital heart disease, deep vein thrombosis (DVT) and pulmonary embolism. Recently, CVDs is the most famous non-communicable disease (NCD) as it is the top one mortality cause which took 31% out of all the death causes in whole world. CVDs is also the main cause of death in Malaysia as shown in World Health Organization - Noncommunicable Diseases (NCD) Country Profiles , 2014 at which CVDs took 36% of proportional mortality in total deaths at all ages and both sexes. Besides that, Health Facts 2014 by Ministry of Health
Drugs that are categorized under BCS Class II category have greater complexity in these problems (G.Geetha et al. 2014). Clopidogrel is under Biopharmaceutics Classification System (BCS) Class II which indicating it has low solubility and high permeability properties (Takagi et al. 2006).
As the permeability of clopidogrel is high, this provides properties of good absorption orally. However, its low solubility that due its poor dissolution or low solvation rate can greatly limiting the oral bioavailability of clopidogrel (Reddy and Karunakar 2011) which is below 50% (Patel et al. 2010) and resulting in its pharmacological effect reduction in the inhibition of platelet aggregation which showing poor therapeutic effectiveness. The irreproducible in the therapeutic effect requires unnecessary consumption of drug in great amount as higher doses in order to achieve the intended therapeutic effect. This properties of drug may lead to unpredicted and uncontrolled precipitation of drugs in aqueous biological fluid which is accompanied with bioavailability problems (Sarita et al.
Based on a review article of Yadav et al. (2012), nanosuspension is solid dispersion of active pharmaceutical ingredients in size of smaller than 1 μm in a liquid vehicle with addition of surfactant for stabilisation purpose. The oral bioavailability of drugs can be improved by nanosuspension through solubility and dissolution rate enhancement due to the resulting greater surface area after particle size reduction. The smaller the size of particles, the greater the surface area which showed in improvement of both saturation solubility and dissolution velocity as the vapour pressure of particles is icreased (Mhatre et al.