Abstract
Ticagrelor is acts by interacting with platelet P2Y12 ADP receptor and prevent platelet activation. It is prescribed for reduction of rate of thrombotic cardiovascular events in patients suffering from acute coronary syndrome like unstable angina, non-ST or ST elevation myocardial infarction. Appearance of Ticagrelor is off-white to pale pink colored crystalline powder. It is belongs to BCS class IV molecule, poorly soluble and permeable. The absolute bioavailability of Ticagrelor is in range 30%-42%. The rate of drug release is a crucial and limiting step for drugs with low gastrointestinal solubility and low permeability for oral drug bioavailability. Among the different solubility enhancement techniques, solid dispersion of poorly soluble drug (s) in a hydrophilic carrier has been proven to be one of the most promising strategies for augmenting solubility and bioavailability. Hence, solubility and thereby in vitro drug release profiles were improved by formulating solid dispersions in hydrophilic polymers by solvent evaporation technique. There was an appreciable enhancement in solubility of Ticagrelor in solid dispersions as compared to solubility of plain drug substance. The rate of in vitro drug release from TSE8 was found to be similar and from TSE13 was on higher side against drug release profiles of BRILINTA® 90 mg Tablets in pH 3.0 Phosphate buffer with 0.2% Tween 80. The percentage of crystallinity of Ticagrelor has been reduced significantly within solid dispersion (TSE13), it has been confirmed by p-XRD. It can be concluded that solid dispersion by solvent evaporation might be an efficacious strategy for augmenting the therapeutic potential of Ticagrelor.
