Development of predictive tools for amorphous solid dosage forms

Background

Since the introduction of modern medicine in the 19th century, oral delivery has remained the preferred route for drug administration due to increased patient safety and compliance, as well as reduced production costs compared to topical and parenteral drug delivery1. Upon ingestion of an oral dosage form, the drug must undergo disintegration and dissolution in the gastrointestinal fluid in order to reach the systemic circulation, as only molecules in solution are able to permeate the intestinal epithelial wall2. It is generally recognized that the rate and extent of drug absorption is controlled by two fundamental parameters: drug solubility and permeability3. An increasing number of new drug candidates have limited oral bioavailability due to poor water-solubility. Therefore, the development of strategies to improve the dissolution profile of these drugs constitutes one of the biggest challenges in pharmaceutical drug formulation4-6.

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