Abstract
A bladder instillation of EO-9 (EOquin™) is currently used in phase II clinical trials for the treatment of superficial bladder cancer. Three alternative formulations were developed to improve its pharmaceutical properties and clinical acceptability. Freeze-dried products composed of EO-9, 2-hydroxypropyl-β-cyclodextrin (HPβCD), tri(hydroxymethyl) aminomethane (Tris), and sodium bicarbonate (NaHCO 3) were tested. Selection of one formulation for further development was based on stability studies. These studies comprised stability of the freeze-dried products, stability after reconstitution and dilution and stability during bladder instillation in an experimental set-up. The stability study of the freeze-dried products showed that the formulation composed of EO-9/HPβCD/Tris (4/600/1 mg/vial) was most stable. After reconstitution and dilution all products were stable for at least 8 h. The product composed of EO9/HPβCD/NaHCO 3 (4/600/20 mg/vial) was the least stable product both as freeze-dried formulation and after reconstitution and dilution. The bladder instillation simulation experiment showed that all products were stable when mixed with urine of pH 8 and unstable in urine of pH 4 and 6. The degradation products formed in urine were EO-5a and EO-9-Cl.Based on these results, the product composed of EO-9/HPβCD/Tris (4/600/1 mg/vial) was selected for further pharmaceutical development.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
