Bioavailability enhancement of a COX-2 inhibitor, BMS-347070, from a nanocrystalline dispersion prepared by spray-drying
| Autor: | Ronald L. Smith, Munir A. Hussain, Alice Hsieh, Miriam K. Franchini, Sandy Jen, Jinling Chen, Shawn X. Yin, Tu Lee |
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| Rok vydání: | 2005 |
| Předmět: |
Materials science
Biological Availability Pharmaceutical Science Excipient Poloxamer Excipients X-Ray Diffraction medicine Organic chemistry Cyclooxygenase Inhibitors Desiccation Particle Size Furans Chromatography High Pressure Liquid Mesylates Calorimetry Differential Scanning Cyclooxygenase 2 Inhibitors Microspheres Nanocrystalline material Bioavailability Amorphous solid Microcrystalline Chemical engineering Nanocrystal Cyclooxygenase 2 Prostaglandin-Endoperoxide Synthases Spray drying Microscopy Electron Scanning medicine.drug |
| Zdroj: | Journal of Pharmaceutical Sciences. 94:1598-1607 |
| ISSN: | 0022-3549 |
| DOI: | 10.1002/jps.20366 |
| Popis: | Spray drying drug with excipients is usually associated with the preparation of microcrystalline or amorphous drug in order to improve bioavailability. It was found that BMS-347070, when spray-dried with Pluronic F127 from acetone or methylene chloride, was dispersed as nanosized crystalline drug within the water-soluble Pluronic matrix. The reduction in drug particle/crystallite size, coupled with wetting by the Pluronic, resulted in a fast-onset formulation with bioavailability comparable to that of a solubilized and a NanoCrystal formulation. For this system, it is theorized that the polyethylene oxide segments of Pluronic crystallize and that the polypropylene oxide segments remain amorphous, providing a size-restricted domain in which the COX-2 drug crystallizes. This results in improved bioavailability while limiting the potential risk of conversion of an amorphous drug to its crystalline state. |
| Databáze: | OpenAIRE |
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