Nasal formulations of insulin

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/28 (2006.01) A61K 47/22 (2006.01) G01N 33/15 (2006.01) G01N 33/66 (2006.01) G01N 33/74 (2006.01)

Patent

CA 2726641

The present invention provides a method for achieving a therapeutically effective plasma levels of insulin by admmiste.pi..pi.g at least two doses of pharmaceutical formulation of insulin sequentially into the same nostril The administration of the second dose in the same nostril gives substantially higher plasma levels of insulin when compared with sequential administration in two different nost.pi.ils Without being limited to any specific physiological mechanism, it is believed that the first dose of insulin acts as a loading dose This loading dose is required to achieve the subsequent plasma levels of insulin that are observed with subsequent doses The Cmax of plasma insulin achieved by the methods and formulations of the present invention is at least about 7Q microU/ml when plasma insulin is measured from about 0 to about 45 minutes after administration of a second dose The AUC achieved is at least about 1800 microU/(ml* mm)

La présente invention concerne un procédé permettant dobtenir des niveaux plasmatiques dinsuline thérapeutiquement efficaces par ladministration séquentielle de deux doses dune formulation pharmaceutique dinsuline dans la même narine. Ladministration de la seconde dose dans la même narine produit des niveaux plasmatiques dinsuline sensiblement élevés comparée à ladministration dans deux narines différentes. Sans quelle soit limitée à un mécanisme physiologique quelconque, on considère que la première dose dinsuline agit comme une dose de charge. Cette dose de charge est nécessaire pour obtenir des niveaux plasmatiques ultérieurs dinsuline qui sont observés avec des doses ultérieures. Le pic de concentration dinsuline plasmatique obtenu par les procédés et formulations selon la présente invention est égal ou supérieur à environ 7Q microU/ml lorsque linsuline plasmatique est mesurée entre environ 0 et environ 45 minutes après ladministration dune seconde dose. La surface sous la courbe obtenue est égale ou supérieure à 1800 microU/ml (ml* mm).

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