Nanosuspensionen - Formulierungen fÃ¼r schwerlÃ¶sliche Arzneistoffe mit geringer BioverfÃ¼gbarkeit
1. Mitteilung: Herstellung und Eigenschaften
Rainer H. MÃ¼ller, Bernhard H. L. BÃ¶hm und Mathias J. Grau
Freie UniversitÃ¤t Berlin, Institut fÃ¼r Pharmazeutische Technologie, Berlin
Nanosuspensions - Formulations for Poorly Soluble Drugs with Poor Bioavailability / Ist Communication: Production and properties
The poor solubility of drugs is generally accompanied by a poor bioavailability and represents a major problem in drug formulation, especially in case the drugs are poorly soluble in aqueous and simultaneously in organic media. Nanosuspensions are an alternative novel formulation for such poorly soluble and bioavailable drugs. The first communication of this publication series deals with the production of nanosuspensions and their special properties -increased Saturation solubility cs and increased dissolution velocity dc/dt. Nanosuspensions are produced by high-pressure homogenisation of aqueous drug suspensions, the resulting particle size can be controlled by varying the production Parameters. The theoretical background of the increased solubility is discussed with regard to an increased dissolution pressure according to the Kelvin equation, creation of new high-energetic interfaces based on the Ostwald-Freundlich equation and a reduction in the diffusional distance according to the Prandtl equation. This section covers also the Sterilisation of nanosuspensions. The second communication will deal with physical stability, bioavailability aspects, creation of various nanosuspension-based drug formulations and also regulatory and registration aspects.
Key words BioverfÃ¼gbarkeit Â· Nanosuspensionen, Eigenschaften, Herstellung Â· SchwerlÃ¶sliche Arzneistoffe
Â© ECV- Editio Cantor Verlag (Germany) 1999