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1. WO2020088306 - POLYELECTROLYTE COMPLEX FOR ORAL DELIVERY OF INSULIN

Publication Number WO/2020/088306
Publication Date 07.05.2020
International Application No. PCT/CN2019/112522
International Filing Date 22.10.2019
IPC
A61K 47/36 2006.01
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
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 47/34 2017.01
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
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 38/28 2006.01
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
A61P 3/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
Applicants
  • 南方医科大学 SOUTHERN MEDICAL UNIVERSITY [CN]/[CN]
Inventors
  • 曾庆冰 ZENG, Qingbing
  • 陈婷婷 CHEN, Tingting
  • 李顺英 LI, Shunying
  • 朱雯婷 ZHU, Wenting
  • 王俊 WANG, Jun
  • 秦婷婷 QIN, Tingting
Agents
  • 北京市诚辉律师事务所 BEIJING CHENGHUI LAW FIRM
Priority Data
201811286230.331.10.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) POLYELECTROLYTE COMPLEX FOR ORAL DELIVERY OF INSULIN
(FR) COMPLEXE POLYÉLECTROLYTIQUE POUR ADMINISTRATION ORALE D'INSULINE
(ZH) 一种用于胰岛素口服递送的聚电解质复合物
Abstract
(EN)
A composite carrier for oral delivery of insulin. The composite carrier uses a two-block copolymer, MePEG-PLGA, as a matrix to prepare two kinds of nanoparticles having positive charge and negative charge, respectively, which are cross-linked after mixing to form a polyelectrolyte complex. After oral administration of the insulin polyelectrolyte complex, the complex can prevent environmental factors such as gastric acid and enzymes from destroying insulin activity when a medicament passes through the stomach, so that the medicament can smoothly reach the intestinal absorption site, rendering the medicament sensitive to pH. The oral preparation has a good hypoglycemic effect and a slow and controlled release effect, and can be used for oral delivery of insulin and protein medicaments.
(FR)
L'invention concerne un support composite pour administration orale d'insuline. Le support composite utilise un copolymère à deux blocs, du MePEG-PLGA, en tant que matrice pour préparer deux types de nanoparticules ayant une charge positive et une charge négative, respectivement, qui sont réticulées après mélange pour former un complexe polyélectrolyte. Après l'administration orale du complexe polyélectrolyte d'insuline, le complexe peut empêcher des facteurs environnementaux tels que l'acide gastrique et des enzymes de détruire l'activité de l'insuline lorsqu'un médicament passe à travers l'estomac, de sorte que le médicament puisse atteindre facilement le site d'absorption intestinale, rendant le médicament sensible au pH. La préparation orale a un bon effet hypoglycémiant et un effet de libération lente et contrôlée, et peut être utilisée pour l'administration orale d'insuline et de médicaments protéiques.
(ZH)
一种用于胰岛素口服递送的复合载体,其由两嵌段共聚物MePEG-PLGA为基质,分别制备成带有正带电荷和带有负电荷的两种纳米粒,混合后相互交联形成聚电解质复合物。该胰岛素聚电解质复合物口服给药后,能避免药物通过胃时胃酸及酶等环境对胰岛素活性的破坏,使药物顺利到达肠道吸收部位,具有pH敏感性。这一口服制剂具有良好的降血糖效果及缓控释作用,可以用于胰岛素和蛋白类的药物的口服递送。
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