STABILIZATION OF OCTASTATIN(R), A SOMATOSTATIN ANALOG, PREPARATION OFFREEZE-DRIED PRODUCTS FOR PARENTERAL INJECTION

Octastatin(R) (RC-160, vapreotide INN) is a somatostatin analogue bein g developed for use in oncological, enterologic and neuroendocrine app lications. The pharmaceutical form is a freeze-dried preparation for p arenteral injection use, Three dosage forms containing 0.5, 1.5 and 15 mg of vapreotide base have been investigated, Various freeze-drying c onditions, stabilizing agents, membranes for sterile filtration and he ating procedures have been examined, The formulation with glutamic aci d-sodium glutamate buffer as a stabilizing agent, the type of membrane for filtration and the freeze-drying procedure have been found approp riate for subsequent industrial production, No evident degradation was observed either after manufacturing, or after a three-week accelerate d stability study at 50 degrees C and 70% relative humidity.