Stabilization of Octastatin, a somatostatin analogue. Preparation of freeze-dried products for parenteral injection.
Octastatin (RC-160, vapreotide INN) is a somatostatin analogue being developed for use in oncological, enterologic and neuroendocrine applications. The pharmaceutical form is a freeze-dried preparation for parenteral injection use. Three dosage forms containing 0.5, 1.5 and 15 mg of vapreotide base have been investigated. Various freeze-drying conditions, stabilizing agents, membranes for sterile filtration and heating procedures have been examined. The formulation with glutamic acid-sodium glutamate buffer as a stabilizing agent, the type of membrane for filtration and the freeze-drying procedure have been found appropriate for subsequent industrial production. No evident degradation was observed either after manufacturing, or after a three-week accelerated stability study at 50 degrees C and 70% relative humidity.
D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D002021:Buffers; D002851:Chromatography, High Pressure Liquid; D004220:Disulfides / Q000737:chemistry; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients; D005612:Freeze Drying; D018698:Glutamic Acid; D006863:Hydrogen-Ion Concentration; D007785:Lactose; D008353:Mannitol; D008969:Molecular Sequence Data; D010865:Pilot Projects; D013004:Somatostatin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013696:Temperature
D000970:Antineoplastic Agents; D002021:Buffers; D004220:Disulfides; D005079:Excipients; C051458:vapreotide; D018698:Glutamic Acid; D008353:Mannitol; D013004:Somatostatin; D007785:Lactose