Cancer Chemotherapy and Pharmacology

, Volume 34, Issue 5, pp 416–422 | Cite as

Pharmaceutical development of a parenteral lyophilized formulation of the novel indoloquinone antitumor agent EO9

  • Jantine D. Jonkman-de Vries
  • Herre Talsma
  • Roland E. C. Henrar
  • Jantien J. Kettenes-van den Bosch
  • Auke Bult
  • Jos H. Beijnen
Original Articles EO9, Parenteral Formulation, Lyophilization


The aim of this study was to design a stable parenteral dosing form of the investigational cytotoxic drug, encoded EO9. EO9 exhibits poor aqueous solubility and stability characteristics. Freeze-drying was selected as the manufacturing process. Differential scanning calorimetry studies were conducted to determine the freezedrying 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 optimal formulation in terms of solubility, length of the freezedrying cycle, stability, and dosing requirements for phase I clinical trials. Quality control of the freeze-dried formulation showed that the manufacturing process does not change the integrity of EO9. Shelf-life studies demonstrated that the formulation remains stable for at least 1 year when stored at +4°C in a dark environment.

Key words

EO9 Parenteral formulation Lyophilization 


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Copyright information

© Springer-Verlag 1994

Authors and Affiliations

  • Jantine D. Jonkman-de Vries
    • 1
  • Herre Talsma
    • 2
  • Roland E. C. Henrar
    • 3
  • Jantien J. Kettenes-van den Bosch
    • 4
  • Auke Bult
    • 4
  • Jos H. Beijnen
    • 1
  1. 1.Department of PharmacySlotervaart Hospital/Netherlands Cancer InstituteAmsterdamThe Netherlands
  2. 2.Department of Pharmaceutics, Faculty of PharmacyUtrecht UniversityUtrechtThe Netherlands
  3. 3.EORTC-NDDOFree University HospitalAmsterdamThe Netherlands
  4. 4.Department of Pharmaceutical Analysis, Faculty of PharmacyUtrecht UniversityUtrechtThe Netherlands

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