Drug precipitation inhibitors in supersaturable formulations |
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Authors: | Sen Xu Wei-Guo Dai |
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Affiliation: | 1. Department of Chemical & Biological Engineering, Drexel University, 3100 Chestnut St., Philadelphia, PA 19104, United States;2. Janssen Research and Development, Johnson and Johnson, 145 King of Prussia Road, Radnor, PA 19087, United States |
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Abstract: | Use of supersaturable formulations has been demonstrated as an effective approach to improve solubility and oral absorption of poorly water-soluble compounds. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when the formulations are exposed to the gastrointestinal fluids and drug might precipitate before being absorbed, resulting in delayed response, and reduced efficacy or compromised bioavailability. Polymer based drug precipitation inhibitors have been used to inhibit or retard such precipitation. In this manner one can maintain a drug in the supersaturated concentration for an extended period of time, leading to significantly improved bioavailability of the poorly water-soluble drugs. This review article discusses different types of precipitation inhibitors, working hypotheses, and case studies with improved oral bioavailability. |
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Keywords: | Drug precipitation Precipitation inhibitors Supersaturable formulations Poorly water-soluble compounds Bioavailability |
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