Raising the thermodynamic activity of a drug substance by the supersaturated state and thereby improving topical drug absorption was proposed four decades ago and now it is possible to achieve enhanced absorption by means of supersaturatable formulations. Increasing the free drug concentration by generating and sustaining a temporarily supersaturated state in vivo with S-SEDDS formulations is the fundamental concept in this approach. The S-SEDDS formulation approach may be useful in overcoming the solubility- and dissolution-limited absorption of other poorly soluble drugs. The three case studies including PNU-91325, pacli-taxel, and Drug X discussed in this chapter demonstrate the utility of the S-SEDDS formulation approach in improving the oral bioavailability of poorly soluble, lipophilic drugs. The other main advantage of the S-SEDDS approach is the reduction in the amount of surfactant in the formulation, thereby achieving an improved tox/safety profile with the S-SEDDS formulations.
We are exploring further applications of the supersaturatable formulation technology and acquiring a scientific understanding of the precipitation kinetics and the mechanism of supersaturation with the use of the polymeric substances. The advances in this area will allow a better control of the supersaturated state and improved oral delivery of poorly soluble drugs.
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