Approximately 80% of high-impact pharmaceutical drugs with the potential to treat severe diseases never reach the market. Many of these drugs have very low water solubility and because they tend to precipitate or destabilize during storage or after administration, they cannot be used for the development of future-generation pharmaceuticals.
Several approaches exist to increase the bioavailability of drugs. Most of them aim at formulating the drug in a less-stable but better-soluble modification, which is intended to be stabilized with the help of excipients, e.g. polymers. However, finding the right excipient for a given drug is quite difficult and today usually established by a "trial-and'error" approach assisted by expensive high-throughput screening techniques. This results in tremendous costs for the development of advanced formulations and - when no appropriate formulation is found - even prevents a huge number of very promising drugs from being used in a medicine.
As pharmaceutical formulations usually have to be stored between manufacturing and use, it is critical that their properties do not change during this period. This is best ensured when they are thermodynamically stable, i.e. at drug concentrations that are lower than the drug solubility in the formulation. The latter is to a great extent influenced by the kind of drug, excipients, temperature, and relative humidity.
The presentation will address the thermodynamic stability of drug formulations and the factors affecting drug bioavailability in the body after administration. Particular emphasis will be placed on oral formulations, i.e. tablets. Prof. Dr. Sadowski will also explain how thermodynamic modelling today allows for reliable correlations and even predictions of conditions leading to high stability/bioavailability and thus drastically reduce the experimental effort to develop the optimal drug formulations as well as their processing.
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