Soluble platform construction of insoluble and active phamaceutical & Nutraceutical molecules and industrialization
In ten years, in the lead compound library, high solubility and high permeability, high solubility and low permeability, low solubility and high permeability compounds have been a hot research object. To improve the bioavailability of new drugs, the Lipinski Screen Five Principles are summarized based on the experience, namely, a molecular weight of less than 500 Dalton, the hydrogen bond acceptor number, no more than 10, the number of hydrogen bond donors of not more than 5, the lipid water partition coefficient (logP) is between -2 to 5. In the process of screening lead compounds, for the considerations of compounds bioavailability, most active compound molecules are abandoned after first round screening. Now the compound library resources (Lipinski drug screening five principles) is full developed, the compound whcih has good efficacy, but bad bioavailability (not comply with the Lipinski screen five principles) has become the gold mining to be developed for new drugs.
Present market on research topic
By the polymeric micelles technology of the solid dispersion, a series of compounds with good efficacy and insolubility were successfully developed into the listed drugs.
By the SEDDS technology of the solid dispersion, a series of compounds with good efficacy and insolubility were successfully developed into the listed drugs.