Tuesday, December 18, 2018

Insights of #PharmaceuticalCocrystals by Fpreshita P Desai in BJSTR

Abstract

Activepharmaceuticalingredients (API) and API drug products developments are facing impending challenges as approximately 60-70% of newly discovered APIs belong to #biopharmaceutical classification system (BCS) Class II (poor solubility, good #permeability) or BCS Class IV (poor solubility, poor permeability) which results in low #oralbioavailability [1]. The conventional approaches of formulating API salts and amorphous APIs are also limiting because in most of these cases APIs either lack #ionizablefunctionalities or do not have strong ionization to allow salt formation. Also, solubility enhanced amorphous form of APIs are #thermodynamically unstable and are prone to transformation in more stable but less soluble crystalline form upon storage. Further, pH gradient across #gastrointestinaltrack adds an additional challenge as some of these APIs possess variable pH dependent solubility and some are unstable or are prone to degradation. In this context, alternative approaches are being researched extensively.


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