How do you make the Lincoln Memorial, the Venus de Milo, The Taj Mahal and the Great Wall of China disappear? 

Ask a pharmaceutical formulation scientist.

It is reported that around ninety percent of new chemical entities discovered by the pharmaceutical industry today are poorly soluble compounds, as are some 40% of drugs currently on the market. Rendering the drug formulations soluble has been described to me, by some pharmaceutical scientists, as “trying to dissolve the Lincoln Memorial” or the Venus de Milo, or Taj Mahal, or the Great Wall of China, depending on where the scientist is in the World and their perspective on highly insoluble icons.

It is well accepted throughout the scientific community that drug substance solubility and particularly aqueous drug substance solubility is an issue for the drug discovery as well as the early and late stage pharmaceutical development process and therefore needs to be addressed very early on, during compound design and optimization.

The solubility or dissolution of the drug substance can be mainly altered on two levels, through material engineering of the drug substance or through formulation approaches. Whatever route is taken to enhance or modify the solubility and/or dissolution of a lead substance, it needs to be scalable to a commercially viable process later on in the development.

At pre-clinical stage, for example, these highly insoluble compounds are often dosed orally as aqueous based suspensions. Later, as the drug candidate moves into clinical trials, the drug product may still be an oral dose but now in solid form rather than a suspension. Accurate and repeatable particle size is a key attribute that must be controlled throughout the discovery, development and manufacturing process.

So, how does one make the Lincoln Memorial disappear?  It needs the scientific skill of a formulation scientist with a little magic from Malvern Instruments.