Biorelevant dissolution studies of platelet aggregation inhibitor: Ticagrelor hydrochloride and its co-crystal with sodium salt of Aspirin

INDIAN JOURNAL OF CHEMICAL TECHNOLOGY(2022)

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Abstract
The comparative dissolution characteristics of poorly soluble platelet aggregation inhibitor Ticagrelor hydrochloride and its co-crystal with sodium salt of Aspirin in biorelevant media have been demonstrated. The API and co-crystal both are subjected to simulated gastric fluid (SGF) and fasted intestinal fluid without micelle forming components (blank FASSIF). The release of API is online monitored through reverse phase liquid chromatography. Prior to online monitoring, the chromatographic method is statistically validated in accordance with ICH guidelines. Chromatographic data reveals that the overall release of Ticagrelor after 3 h is about 6 mu g/mL higher in co-crystal (24.5 mu g/mL) compared to unaccompanied API (18.6 mu g/mL) in simulated gastric fluid (SGF). Whereas in fasted intestinal fluid without micelle forming components (blank FASSIF) more than threefold high release of API is observed in co-crystal (12.14 mu g/mL) compared to API (4.22 mu g/mL) in free form. Results clearly indicate the improved solubility in the lower regions of the gastrointestinal tract and better absorption of drug. This type of co-crystal would also allow the simultaneous dosing in suitable formulation.
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Key words
Biorelevant, Co-crystal, Dissolution, HPLC, Ticagrelor
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