Novel use of dipeptidyl peptidase-iv inhibitor

An enzyme activity inhibitor, dipeptidyl peptidase technology, applied in the direction of organic active ingredients, non-central analgesics, anti-inflammatory agents, etc.

Inactive Publication Date: 2010-04-07
PROSIDION LIMITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] 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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Examples

Experimental program
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Effect test

Embodiment 1

[0038] 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.

[0039] 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.

[0040] 36 healthy male subjects were divided into 3 individu...

Embodiment 2

[0063] 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%.

[0064] 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.

[0065] 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:

[0066] P32 / 98 and glibenclamide were given once daily for 21 day...

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PUM

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Abstract

The present invention discloses a use of dipeptidyl peptidase-IV inhibitor in producing a medicine which is used for long-term oral medicine taking for preventing Type II Diabetes in mammal, wherein the peptidase-IV inhibitor converts the cells in pancreas to cells generating insulin, so that the pancreatic cell proliferate to functional active islet cells and / or the insensitive or damaged pancreatic cells convert to functional active islet cells.

Description

[0001] This application is a divisional application of Chinese patent application 01807402.2 filed on April 2, 2001, and the invention title is "Methods for Improving Islet Signal Transduction in Diabetes and Its Prevention". Background technique [0002] 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. [0003] Incretins such as glucagon-like pe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61P3/10C07D277/04A61K31/00A61K31/40A61K31/401A61K31/425A61K31/426A61K38/00A61K45/06A61P5/50A61P19/02A61P29/00A61P31/18A61P37/06A61P43/00
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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