PHARMACEUTICAL DEVELOPMENT OF A PARENTERAL LYOPHILIZED FORMULATION OFTHE NOVEL INDOLOQUINONE ANTITUMOR AGENT E09

The aim of this study was to design a stable parenteral dosing form of the investigational cytotoxic drug, encoded EO9. EO9 exhibits poor aq ueous solubility and stability characteristics. Freeze-drying was sele cted as the manufacturing process. Differential scanning calorimetry s tudies were conducted to determine the freeze-drying cycle parameters. A stable lyophilized formulation of EO9 was developed. The prototype, containing 8.0 mg EO9 and 200 mg lactose/vial, was found to be the op timal formulation in terms of solubility, length of the freeze-drying cycle, stability, and dosing requirements for phase I clinical trials. Quality control of the freeze-dried formulation showed that the manuf acturing process does not change the integrity of EO9. Shelf-life stud ies demonstrated that the formulation remains stable for at least 1 ye ar when stored at +4 degrees C in a dark environment.