Cyanocobalamin low viscosity aqueous formulations for...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/714 (2006.01) A61K 9/08 (2006.01) A61M 15/08 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2656823

A stable pharmaceutical 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 yields a bioavailability of cyanocobalamin when administered intranasally of at least about 5% relative to an intramuscular injection of cyanocobalamin. The present invention is also directed towards a method for elevating the vitamin B 12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a cyanocobalamin solution so as to increase the average ratio of vitamin B 12 in the CSF to that in the blood serum (B12 CSF/B12 Serum x 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 5% relative to an intramuscular injection of a cyanocobalamin.

Solution aqueuse pharmaceutique stable de cyanocobalamine constituée de cyanocobalamine et d'eau, ladite solution de cyanocobalamine convenant pour une administration intra-nasale, ayant une viscosité inférieure à environ 1000 cPs et produisant une biodisponibilité de la cyanocobalamine lorsqu'elle est administrée de façon intra-nasale d'au moins environ 5 % par rapport à une injection intramusculaire de cyanocobalamine. La présente invention concerne également un procédé servant à élever les niveaux de vitamine B12 dans le liquide céphalorachidien (LCR) consistant à administrer de façon intra-nasale une quantité suffisante d'une solution de cyanocobalamine de façon à augmenter le rapport moyen de la quantité de vitamine B12 dans le LCR sur celle dans le sérum sanguin (B12 LCR/B12 sérum x 100) à au moins environ 1,1 consistant à administrer de façon intra-nasale une solution aqueuse d'une cyanocobalamine, ladite solution de cyanocobalamine ayant une biodisponibilité d'au moins 5 % par rapport à une injection intramusculaire d'une cyanocobalamine.

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