Investigation of Carbohydrates and Their Derivatives as Crystallization Modifiers

Development in the field of pharmaceutical administration has resulted in the discovery of highly sophisticated drug delivery systems that allow for the maintenance of a constant drug level in an organism. Contrary to these revolution biopharmaceutical results, over the last ten years, the number of poorly soluble drugs has steadily increased. Estimates state that 40% of the drugs in the pipelines have solubility problems. Progress in high throughput screening methods leads to an even greater amount of newly discovered drugs, but a lot of them have poor water solubility. Literature states that about 60% of all drugs coming directly from synthesis are nowadays poorly soluble. Meanwhile the five key physicochemical properties, such as pKa, solubility, permeability, stability and lipophilicity, in early compound screening should be optimized. Compounds with insufficient solubility carry a higher risk of failure during discovery and development, since insufficient solubility may compromise other property assays, mask additional undesirable properties, influence both pharmacokinetic and pharmacodynamic properties of the compound and finally may affect the developability of the compound. Poor solubility in water correlates with poor bioavailability. If there is no way to improve drug solubility, it will not be able to be absorbed from the gastrointestinal tract into the bloodstream and reach the site of action (Junghanns & Müller, 2008; Payghan et al., 2008).