Title:
AGGREGATE FORMED BY MEANS OF ASSEMBLING CHALCOGEN HETEROCYCLIC COMPOUND AND INSULIN, AND PREPARATION METHOD THEREFOR, AND INSULIN ORAL PREPARATION
Document Type and Number:
WIPO Patent Application WO/2023/065551
Kind Code:
A1
Abstract:
Provided in the present invention are an aggregate and a preparation method therefor, and an insulin oral preparation. Specifically provided is an aggregate, which is an aggregate formed by means of assembling a chalcogen heterocyclic compound and insulin. The aggregate can be further prepared into an insulin oral preparation. The oral preparation can be used for reducing the blood glucose level of a mammal as part of a diabetes treatment regimen. The chalcogen heterocyclic compound in the insulin oral preparation prepared by means of the method can effectively protect insulin against the three physiological barriers of an oral uptake pathway, is stable in the gastrointestinal tract environment, is subjected to a dynamic chemical exchange reaction with intestinal mucin in intestinal juice and the sulfhydryl groups of proteins inside and outside an epithelial cell membrane by means of the molecular bond of polychalcogen on the surface, and enters the circulation system from the intestinal epithelial cell to achieve the effect of reducing blood glucose. When being orally administered, the insulin oral preparation has high bioavailability, has a good hypoglycemic effect in mammals, and can be used for treating diabetes.
Inventors:
CHEN ZHAOWEI (CN)
CHEN CHEN (CN)
YANG HUANGHAO (CN)
LIU ZHENG (CN)
HE YU (CN)
CHEN CHEN (CN)
YANG HUANGHAO (CN)
LIU ZHENG (CN)
HE YU (CN)
Application Number:
PCT/CN2022/072018
Publication Date:
April 27, 2023
Filing Date:
January 14, 2022
Export Citation:
Assignee:
UNIV FUZHOU (CN)
International Classes:
A61K47/54; A61K9/00; A61K9/51; A61K38/28; A61K45/06; A61K47/22; A61K47/69; A61P3/10; B82Y5/00; B82Y40/00
Foreign References:
| CN101454019A | 2009-06-10 | |||
| CN109758588A | 2019-05-17 | |||
| CN107636017A | 2018-01-26 |
Other References:
ZHU XI, SHAN WEI, ZHANG PEIWEN, JIN YUN, GUAN SHAN, FAN TINGTING, YANG YANG, ZHOU ZHOU, HUANG YUAN: "Penetratin Derivative-Based Nanocomplexes for Enhanced Intestinal Insulin Delivery", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 11, no. 1, 20 November 2013 (2013-11-20), US , pages 317 - 328, XP093059378, ISSN: 1543-8384, DOI: 10.1021/mp400493b
LINGHUI QIAN; JIAQI FU; PEIYAN YUAN; SHUBO DU; WEI HUANG; LIN LI; SHAO Q. YAO: "Intracellular Delivery of Native Proteins Facilitated by Cell‐Penetrating Poly(disulfide)s", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, VERLAG CHEMIE, HOBOKEN, USA, vol. 57, no. 6, 8 January 2018 (2018-01-08), Hoboken, USA, pages 1532 - 1536, XP072087192, ISSN: 1433-7851, DOI: 10.1002/anie.201711651
JIANYONG SHENG, HERALD OF MEDICINE: "Research Progress of Insulin Nanoparticle Formulations for Oral Delivery", YANG XIAOZU, JITANG CHEN, TIANHAO PENG, XIANGLIANG YANG, vol. 37, no. 6, 30 June 2018 (2018-06-30), pages 703 - 707, XP093059385
CHANGMIN YU; LINGHUI QIAN; JINGYAN GE; JIAQI FU; PEIYAN YUAN; SAMANTHA C. L. YAO; SHAO Q. YAO: "Cell‐Penetrating Poly(disulfide) Assisted Intracellular Delivery of Mesoporous Silica Nanoparticles for Inhibition of miR‐21 Function and Detection of Subsequent Therapeutic Effects", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, VERLAG CHEMIE, HOBOKEN, USA, vol. 55, no. 32, 21 June 2016 (2016-06-21), Hoboken, USA, pages 9272 - 9276, XP072095506, ISSN: 1433-7851, DOI: 10.1002/anie.201602188
GASPARINI GIULIO, MATILE STEFAN: "Protein delivery with cell-penetrating poly(disulfide)s", CHEMICAL COMMUNICATIONS, ROYAL SOCIETY OF CHEMISTRY, UK, vol. 51, no. 96, 8 October 2015 (2015-10-08), UK , pages 17160 - 17162, XP093059312, ISSN: 1359-7345, DOI: 10.1039/C5CC07460F
LINGHUI QIAN; JIAQI FU; PEIYAN YUAN; SHUBO DU; WEI HUANG; LIN LI; SHAO Q. YAO: "Intracellular Delivery of Native Proteins Facilitated by Cell‐Penetrating Poly(disulfide)s", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, VERLAG CHEMIE, HOBOKEN, USA, vol. 57, no. 6, 8 January 2018 (2018-01-08), Hoboken, USA, pages 1532 - 1536, XP072087192, ISSN: 1433-7851, DOI: 10.1002/anie.201711651
JIANYONG SHENG, HERALD OF MEDICINE: "Research Progress of Insulin Nanoparticle Formulations for Oral Delivery", YANG XIAOZU, JITANG CHEN, TIANHAO PENG, XIANGLIANG YANG, vol. 37, no. 6, 30 June 2018 (2018-06-30), pages 703 - 707, XP093059385
CHANGMIN YU; LINGHUI QIAN; JINGYAN GE; JIAQI FU; PEIYAN YUAN; SAMANTHA C. L. YAO; SHAO Q. YAO: "Cell‐Penetrating Poly(disulfide) Assisted Intracellular Delivery of Mesoporous Silica Nanoparticles for Inhibition of miR‐21 Function and Detection of Subsequent Therapeutic Effects", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, VERLAG CHEMIE, HOBOKEN, USA, vol. 55, no. 32, 21 June 2016 (2016-06-21), Hoboken, USA, pages 9272 - 9276, XP072095506, ISSN: 1433-7851, DOI: 10.1002/anie.201602188
GASPARINI GIULIO, MATILE STEFAN: "Protein delivery with cell-penetrating poly(disulfide)s", CHEMICAL COMMUNICATIONS, ROYAL SOCIETY OF CHEMISTRY, UK, vol. 51, no. 96, 8 October 2015 (2015-10-08), UK , pages 17160 - 17162, XP093059312, ISSN: 1359-7345, DOI: 10.1039/C5CC07460F
Attorney, Agent or Firm:
UNITALEN ATTORNEYS AT LAW (CN)
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