title: Compatibility and stability of the novel anticancer agent ES-285 x HCl formulated with 2-hydroxypropyl-beta-cyclodextrin in infusion devices.
abstract: ES-285 x HCl is a novel marine-derived anticancer agent isolated from the clam Spisula polynyma. The compound is pharmaceutically formulated as a lyophilised product containing 25 or 50 mg ES-285 x HCl and 500 or 1000 mg 2-hydroxypropyl-beta-cyclodextrin per dosage unit and requires reconstitution with sterile water for injection before intravenous administration. The aim of this study was to determine the stability and compatibility of ES-285 x HCl in infusion devices. ES-285 x HCl was shown to be stable at concentrations of 10-1400 microg/ml after dilution in 5% dextrose in water and compatible with PE infusion containers and PE and silicone tubing. No sorption on- or into the administration set was observed at concentrations equal to or above 20 microg/ml. In conclusion, ES-285 x HCl infusion solutions can be administered without stability or sorption problems using a PE infusion container and PE or silicone tubing in concentrations equal or above 20 microg/ml in 3-hour or 24-hour infusion administration schedules.
authors.affiliation: Slotervaart Hospital/The Netherlands Cancer Institute, Department of Pharmacy & Pharmacology, Amsterdam, The Netherlands. apmbk@slz.nl
authors.forename: M W J
authors.initials: MW
authors.lastname: Den Brok
authors.forename: B
authors.initials: B
authors.lastname: Nuijen
authors.forename: J L
authors.initials: JL
authors.lastname: García
authors.forename: E
authors.initials: E
authors.lastname: Miranda
authors.forename: P
authors.initials: P
authors.lastname: Calvo
authors.forename: C
authors.initials: C
authors.lastname: Manada
authors.forename: J H
authors.initials: JH
authors.lastname: Beijnen
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000473:Alkanes / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry*; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D004355:Drug Stability; D007262:Infusions, Intravenous; D008055:Lipids / Q000737:chemistry*; D012995:Solubility; D012996:Solutions; D013056:Spectrophotometry, Ultraviolet; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000473:Alkanes; D000970:Antineoplastic Agents; D008055:Lipids; D012996:Solutions; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C408363:spisulosine