Ritonavir: An Extraordinary Example of Conformational Polymorphism

By J. Bauer, S. Spanton, R. Henry, J. Quick, W. Dziki, W. Porter, J. Morris. Pharmaceutical Research, 2001

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Strategies to Address Low Drug Solubility in Discovery and Development (2013, background): “…unstable formulations is provided by the antiviral ritonavir, a product that was initially marketed as a capsule formulation (Norvir; Abbott Laboratories) but was later withdrawn after the identification of a more stable (and less soluble) crystalline polymorph (Bauer et al., 2001).”
Current approaches to predicting molecular organic crystal structures (2011, background): “The most notorious example of the consequences of unanticipated polymorphism is the temporary withdrawal from the market of the protease inhibitor Ritonavir (1, 2); the scientists dealing with the impact of the new polymorph concluded that it ‘is highly advisable to put enough resources to carry on ”
High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids. (2004, background): “This new form (form II) was approximately 50% less soluble in the hydroalcoholic formulation vehicle, resulting in poor dissolution behavior and eventual withdrawal of the original NorvirR capsule from the market [98].”