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Nearly 40% of the new molecular entities coming from discovery were never brought to the market because of biopharmaceutical issues e.g. low solubility, low dissolution rate, low permeability and first-pass metabolism in the liver.
Moreover, in the Biopharmaceutical Classification Systems marketed drugs and new molecular entities are classified in four groups according to their solubility and intestinal permeability. Class 1 contains drugs with a high solubility and permeability. Those drugs are well absorbed and their absorption rate is usually higher than excretion. Class 2 contains drugs with a low solubility and high permeability. The bioavailability of those drugs is limited by their dissolution rate. In addition, Class 3 drugs are highly soluble, although permeability is limited by the permeation rate but the drug is dissolved very fast. Finally, Class 4 drugs have poor bioavailability because of low solubility and permeability. Usually they are not well absorbed over the intestinal mucosa and a high variability is expected. In comparison with marketed drugs the new molecular entities show increased solubility and permeability problems (Class 2 & 4), further decreasing the output of the big pharmaceutical and biopharmaceutical industry.
SEPS Pharma develops lipophilic prodrug systems (LIPS) and self emulsifying prodrug systems (SEPS) to overcome solubility, dissolution rate and/or permeability problems.
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