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Method for improvement of islet signaling in diabetes mellitus and for its prevention

A technology of insulin cells and uses, applied in metabolic diseases, antiviral agents, pharmaceutical formulations, etc.

Inactive Publication Date: 2003-05-28
PROSIDION LIMITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, this mode of treatment requires enteral or parenteral administration of biologically active GLP-1 to the patient, including the possibility of surgery

Method used

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  • Method for improvement of islet signaling in diabetes mellitus and for its prevention
  • Method for improvement of islet signaling in diabetes mellitus and for its prevention
  • Method for improvement of islet signaling in diabetes mellitus and for its prevention

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The DP IV inhibitor P32 / 98 is transported via the activity of the PepT1 intestinal peptide transporter. The rapid and active transport of P32 / 98 across the intestinal mucosa is responsible for its fast onset. t max is a prerequisite for an efficient target of dipeptidyl peptidase IV (DP IV). Oral administration of P32 / 98 resulted in maximal target inhibition at 15 to 20 minutes and 30 to 40 minutes after ingestion in rats and humans, respectively. Therefore, DP IV inhibitors should be given 10-20 minutes before glucose or food intake.

[0037] In a first-in-human study with P32 / 98, pharmacokinetic parameters, such as insulin and GLP-1 concentrations in plasma, and blood glucose were studied in 36 healthy male volunteers. Oral doses of P32 / 98 are in the following concentrations: 7.5 mg, 15 mg, 30 mg, 60 mg, 120 mg and 240 mg. The results for the above pharmacokinetic parameters are summarized in Table 1.

[0038] 36 healthy male subjects were divided into 3 individu...

Embodiment 2

[0055] P32 / 98 nutrient dependence supports initial insulin secretion in obese Zucker rats. However, P32 / 98 decreased total daily insulin secretion during subchronic treatment. P32 / 98 caused insulin savings of 45% compared to the control glibenclamide which increased insulin output by 27%.

[0056] Trials were performed to determine whether P32 / 98 is the first choice to affect glucose tolerance in vivo by increasing the circulating half-life of the incretins GIP and GLP-1. Glibenclamide (Maninil  Berlin-Chemie, Berlin, Germany) as a reference material for comparative studies. Glibenclamide is one of the most effective drugs for lowering blood sugar in patients with type II diabetes and is one of the most commonly prescribed sulfonylureas.

[0057] Male Zucker fa / fa rats, which exhibit abnormalities in glucose metabolism and are an ideal animal model for type II diabetes, were studied in the following manner:

[0058] P32 / 98 and glibenclamide were given once daily for 21 da...

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PUM

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Abstract

The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic ²-cells and to cause differentiation of pancreatic epithelial cells into insulin producing ²-cells. Oral administration of a DP-IV inhibitor causes the active form of GLP-1 to be preserved longer under physiological conditions. The extended presence of GLP-1, in particular in the pancreatic tissue facilitates differentiation and regeneration of the ²-cells already present that arc in need of repair. These repaired insulin producing cells can contribute to the correction and maintenance of normal physiological glycemic levels.

Description

Background technique [0001] The pancreas consists of two glandular tissues, the collection of cells that form the exocrine function of the pancreas, where digestive enzymes are synthesized and released into the intestine, and the endocrine function of the pancreas, which synthesizes hormones and released into the loop. Most important in the endocrine function of the pancreas are the β-cells. These cells synthesize and secrete the hormone insulin. The hormone insulin plays a key role in maintaining normal physiological blood sugar levels. Effector molecules of pancreatic endocrine cells are present. Incretins are examples of such molecules. Incretins potentiate pancreatic glucose-induced insulin secretion. [0002] Incretins such as glucagon-like peptide-1 (7-36) amide ("GLP-1"; or the lizard analog Exendin-4) and gut inhibitory peptide ("GIP") have been shown to be insulinotropic , that is, their presence or stabilization can maintain acute glycemic control (Demuth, H.U....

Claims

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Application Information

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IPC IPC(8): C07D277/04A61K31/00A61K31/40A61K31/401A61K31/425A61K31/426A61K38/00A61K45/00A61K45/06A61P3/10A61P5/50A61P19/02A61P29/00A61P31/18A61P37/06A61P43/00
CPCY10S514/866A61K45/06A61K31/00A61K31/426A61K31/40A61P19/00A61P19/02A61P29/00A61P3/00A61P3/10A61P31/00A61P31/18A61P37/00A61P37/06A61P43/00A61P5/00A61P5/50A61K31/425
Inventor 汉斯-乌尔里希·德穆特康拉德·格隆德
Owner PROSIDION LIMITED
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