Tablets & Capsules

TC0716

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Tablets & Capsules July 2016 29 formulation Improving the bioavailability APIs for delivery in oral solid dosage forms Robert J. Timko RhoTau Pharma Services The bioavailability of an active pharmaceutical ingredient (API) depends on its chemical, biological, and physical properties. Good aqueous solubility is a key consideration to obtaining a bioavail- able product. This article summarizes some of the techniques used to improve solubility and/or absorption. They include modifying the chemical structure, changing the physical form, reducing the particle size, and using fit-for-purpose excipients. D elivering medicine orally via a tablet or capsule is a sim- ple and easy way to administer APIs. Both solid dosage forms offer convenience, boost patient compliance, gener- ally offer good stability profiles, provide accurate doses, and are easy to produce. Historically, the speed of drug development was tied to the discovery of compounds with high biological activity and a strong affinity for receptor sites. More recently, phar- macokinetic factors such as absorption and permeability across the gastrointestinal (GI) epithelium have become key considerations.

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