Issue link: https://www.e-digitaleditions.com/i/238663
c-Kheurart_10-15_Masters 12/30/13 1:55 PM Page 10 10 January 2014 Tablets & Capsules formulation A rapid vehicle-screening approach for formulating a low-solubility compound into liquid-filled capsules Amol Kheur, Anil Kane, Mohammad Aleem, and Maureen McLaughlin Patheon Pharmaceutical Development Services Kiran Kumar Tumbalam and Shivaprakash Poojary Formerly of Patheon For a drug product to exert its therapeutic effect, it must be soluble in an aqueous environment. This ensures that the active pharmaceutical ingredient (API) will provide sufficient concentration to induce gastrointestinal (GI) tract absorption. Hence, molecules with promising pharmacodynamics yet poor solubility may be rejected during the drug discovery stage. This article summarizes how an excipient-mixture approach can enhance the solubility, the in vitro dissolution, and the bioavailability profile of a low-solubility compound. A s drug development costs continue to rise, it has become increasingly important for companies to assess early on whether a new molecular entity (NME) will succeed in clinical trials. Analyzing the structure of a new compound is an especially crucial step in the discovery stage for orally active drugs, as their solubility and permeability properties are two of the strongest predictors of whether Phase II (proof-of-concept) studies will commence [1]. Companies profile NMEs so they can incorporate certain desirable characteristics into the molecule; select lead compounds that are likely to survive in the pipeline;