Supersaturable formulations

Abstract

Numerous methodologies have been suggested and practically applied to improve the ability to market drug candidates whose development is limited by drug solubility and dissolution rate. These include the use of wetting agents, complexing agents such as cyclodextrins, preparation of high energy drug states related to polymorphic transformations and the use of particle size manipulation. One suggested path forward is the use of a "spring and parachute" approach wherein a technique such as self emulsifying systems allow rapid dissolution of a poorly water-soluble drug at a supersaturated concentration.
However, this in vivo supersaturated system has the potential to precipitate which will impact negatively on the pharmacokinetics and efficacy of the drug. A formulation component which hinders crystal growth or nucleation then acts as a parachute to stabilise the metastable supersaturated system in vivo is the key to improve the oral absorption of a drug^1,2).