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1. CN101495132 - Insulin composition

Office China
Application Number 200780028627.6
Application Date 08.06.2007
Publication Number 101495132
Publication Date 29.07.2009
Publication Kind A
IPC
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 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
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.
CPEX药品公司
Inventors Gyurik Robert J.
R·J·久里克
Reppucci Carl
C·雷伯慈
Li Zhengmao
Z·李
Agents zhang anyu jiang jiancheng
北京北翔知识产权代理有限公司
北京北翔知识产权代理有限公司
Priority Data 60/811,913 08.06.2006 US
Title
(EN) Insulin composition
(ZH) 胰岛素组合物
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.

(ZH)

本发明公开了使用胰岛素来治疗患者的组合物和方法,其中其形式适合通过鼻部送递给患者的组合物包含治疗有效量的胰岛素、渗透促进剂、液体载体和存在于所述组合物中的酸,其量足以提供酸性pH、但是pH不高于4.5,所述酸选自一种(或多种)单价无机酸、硫酸和醋酸。优选地,所述组合物基本不含一种(或多种)柠檬酸盐,并且基本不含一种(或多种)磷酸盐。因而,设计所述组合物的目的在于提供基本不含小纤维形式的(或β折叠)胰岛素多晶型物的组合物。同样公开了用于通过鼻部给予人、或通过鼻部给予温血动物的药物组合物,它含有:(A)治疗有效量的胰岛素、(B)渗透促进剂和(C)液体载体,所述组合物可进一步含有以下的任何一种或每一种物质,或由其表征:(D)非离子型表面活性剂的结合物;其中所述非离子型表面活性剂的结合物包含(i)糖或糖醇的至少一种脂肪酸酯,和(ii)糖或糖醇的至少一种聚乙二醇修饰的脂肪酸酯;(E)具有酸性pH,但pH不高于4.5;(F)重量渗克分子浓度<200mOsmol/Kg H2O。