Cyanocobalamin low viscosity aqueous formulations for intranasal delivery

• Main Authors: SILENO ANTHONY P, GO ZENAIDA O, QUAY STEVEN C, APRILE PETER C
• Format: Patent
• Language: English
• Published: 01.02.2011
• Subjects: BANDAGES, DRESSINGS OR ABSORBENT PADS; CHEMISTRY; DERIVATIVES THEREOF; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF,TUBULAR STRUCTURES OF THE BODY, E.G. STENTS; FILTERS IMPLANTABLE INTO BLOOD VESSELS; FIRST-AID KITS; FOMENTATION; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROSTHESES; SUGARS; TREATMENT OR PROTECTION OF EYES OR EARS

A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.