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Md Abdul Khader
Roshan S


Ticagrelor, solid dispersion, fusion (melt) method, poloxamer 188, platelet aggregation inhibitor.


Introduction: The current study is aimed at enhancing the solubility and release rates of ticagrelor (TGL), an oral antiplatelet agent by adopting solid dispersion (SD) technique.

Material and Methods: Forty formulations of TGL SD prepared by solvent evaporation method(TGL1-TGL20) and fusion(melt) method(TGL20-TGL40) using varying ratios of water soluble carriers(poloxamer 188, labrafil M1944, PEG 8000and gelucire 44/14).All the formulations evaluated for pre compression parameters,% practical yield,% drug content and drug dissolution. The optimized formulation further subjected to characterization by FTIR, PXRD and SEM studies.

Results: The solubility of ticagrelor(TGL) checked in various polymers indicate that  pure drug exhibited maximum solubility in  phosphate  buffer(0.152 mg/ml) while drug and poloxamer 188 mixture exhibited maximum solubility of 3.8 mg/ml in phosphate buffer . The SD formulation TGL35 containing poloxamer 188 exhibited maximum solubility of 6.992±0.04 mg/ml which is 46 folds that of pure drug. Similar enhancement trends observed in % drug content, %practical yield and in-vitro dissolution rates of TGL35 (99.55% in 60 minutes) when compared to pure drug. FTIR study displayed the compatibility amongst drug and polymer used. The XRD and SEM studies showed TGL35 existed in amorphous state which fetched in better drug release rates of SD formulation in comparison to pure drug.

Conclusion: The results indicate that the formulation technology employed with a potential of enhancing bioavailability and solubility of ticagrelor.

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