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1. EP2035031 - INSULIN COMPOSITION

Office European Patent Office
Application Number 07809400
Application Date 08.06.2007
Publication Number 2035031
Publication Date 18.03.2009
Publication Kind A4
IPC
A61K 9/107
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions
A61K 38/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
28Insulins
CPC
A61K 9/0043
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0043Nose
A61K 9/107
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions ; ; Emulsion preconcentrates; Micelles
A61K 9/1075
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions ; ; Emulsion preconcentrates; Micelles
1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
A61K 38/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
28Insulins
A61K 47/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
02Inorganic compounds
A61K 47/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
08containing oxygen, ; e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
Applicants CPEX PHARMACEUTICALS INC
Inventors GYURIK ROBERT J
REPPUCCI CARL
LI ZHENGMAO
Designated States
Priority Data 81191306 08.06.2006 US
Title
(DE) INSULINZUSAMMENSETZUNG
(EN) INSULIN COMPOSITION
(FR) COMPOSITION D'INSULINE
Abstract
(EN)
Compositions and methods are disclosed for treating a patient with insulin, wherein a composition in a form suitable for nasal delivery to a patient comprises a therapeutically effective amount of insulin, a permeation enhancer, a liquid carrier, and an acid present in said composition in an amount sufficient to provide an acidic pH, but not greater than a pH of 4.5, said acid being selected from the group consisting of: monovalent inorganic acid(s), sulfuric acid, and acetic acid. Preferably the composition is essentially-free of citrate(s) and essentially-free of phosphate(s). The composition being thus designed with the intent to provide a composition that is essentially-free of fibrilliform (or beta-sheet) insulin polymorphs. Also disclosed are pharmaceutical compositions for nasal administration to humans, or to warm-blooded animals, comprising: (A) a therapeutically effective amount of insulin; (B) a permeation enhancer; and (C) a liquid carrier; the compositions being further comprised of, or characterized by, any, or each, of: (D) a combination of non-ionic surfactants; wherein the combination of non-ionic surfactants comprises: (i) at least one fatty acid ester of a sugar or sugar alcohol and (ii) at least one pegylated fatty acid ester of a sugar or sugar alcohol; (E) an acidic pH, but no greater than a pH of 4.5; and (F) an osmolality of < 200 mOsmol/Kg H2O.

(FR)
L'invention concerne une composition et procédés servant à traiter un patient avec de l'insuline, ladite composition sous une forme convenant pour une administration nasale à un patient comprenant une quantité efficace du point de vue thérapeutique d'insuline, un agent augmentant la perméation, un véhicule liquide et un acide présent dans ladite composition en quantité suffisante pour fournir un pH acide, mais inférieure ou égale à 4,5, ledit acide étant sélectionné dans le groupe constitué d'acide(s) inorganique(s) monovalent(s), de l'acide sulfurique et de l'acide acétique. De préférence la composition est sensiblement exempte de citrate(s) et sensiblement exempte de phosphate(s). La composition est ainsi destinée à former une composition qui est sensiblement exempte de polymorphes en forme de fibrilles (ou en feuillets bêta) de l'insuline. L'invention concerne également des compositions pharmaceutiques destinées à une administration nasale à des humains ou à des animaux à sang chaud, comprenant : (A) une quantité efficace du point de vue thérapeutique d'insuline; (B) un agent augmentant la perméation; et (C) un véhicule liquide, les compositions comprenant en outre, ou étant en outre caractérisées par, l'un quelconque ou chacun de : (D) une association de tensioactifs non ioniques, ladite association de tensioactifs non ioniques comprenant (i) au moins un ester d'acide gras d'un sucre ou d'un alcool de sucre et (ii) au moins un ester d'acide gras pégylé d'un sucre ou d'un alcool de sucre; (E) un pH acide, mais inférieur ou égal à 4,5; et (F) une osmolalité < 200 mOsmol/kg de H2O.