Friday, 6 October 2006 - 4:20 PM
Southern Tier (Holiday Inn Binghamton - Arena)
312

Engineered porous silicates for sustained release of poorly water-soluble drugs

Isabelle Lagadic, Rupali Shah, Melissa Zastrow, Shannon Verissimo, and Jannette Novy. University of Connecticut, Storrs, CT

Improving the solubility of poorly water-soluble drugs in order to increase their oral bioavailability remains an important challenge for the pharmaceutical industry. Poorly water-soluble drugs are usually mechanically ground with silicate substrates (e.g. calcium silicate) to amorphize them, and hence enhance their dissolution rates. Our objective was to investigate the loading of poorly water-soluble Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), such as ibuprofen and naproxen onto ordered porous silicates and their organically functionalized derivatives by impregnation methods. The solids were characterized by FT-IR, powder XRD, surface and porosity analyses, and TGA and impregnated with organic drug solutions in various solid to drug weight ratios. The drugs, in their amorphous forms, quickly adsorb onto the solids to a loading amount of up to 300 mg of drug per gram of solid. The type of drug-solid interactions was investigated. Drug release studies were carried out at 37ºC in simulated body fluid (SBF, pH = 7.4) and simulated gastric fluid (SGF, pH = 1.2). The drug release profiles were determined by monitoring the drug concentration in the release medium over time by UV-Visible spectroscopy. Negligible amount of drugs were released in SGF, while significant release occurs in SBF over an extended period of time, indicating that these materials can effectively prevent drug release in the gastric environment and can act as effective carriers fro the sustained delivery of poorly water-soluble NSAIDs.

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