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New combinations of an anti emetic agent and an enkephalinase inhibitor

An antiemetic and a composition technology, which is applied in the field of combination of an antiemetic and an enkephalinase inhibitor, can solve the problems of no suggestion or assumption, can not be used, etc., and achieves optimal single administration and optimal pharmacokinetics. , the effect of improving the effect of single administration

Inactive Publication Date: 2010-07-21
BIOPROJET
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, there is a prejudice that 5-HT should not be used in patients with diarrhea, such as those with gastroenteritis 3 receptor antagonist
Therefore, the 5-HT 3 Combination of receptor antagonists with NEP inhibitors is neither disclosed nor suggested or conceived

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0080] Example: In Vivo Activity of Combinations of the Invention

[0081] The outstanding activity of the combination according to the invention was confirmed in an animal model of experimental diarrhea. According to Niemegeers et al. (Armeim.-Forsch. (Drug Res), 1974, 24 The method of No. 10), evaluating the combination of the present invention with castor oil-induced diarrhea in rats.

[0082] Rats received a combination of ondansetron (0.1 mg / kg, p.o.) and racecadotril (40 mg / kg, p.o.). The combination elicited a nearly complete antidiarrheal effect for 6-7 hours.

[0083] In Comparative Example, ondansetron and racecadotril were administered alone at the same dose.

[0084] Ondansetron (0.1 mg / kg, p.o.) was not active in this model when administered alone.

[0085] Administration of racecadotril (40 mg / kg, p.o.) alone induced partial protection for 4 hours in this model.

[0086] In addition, ondansetron at 1 mg / kg was also inactive in this model, but when combined ...

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PUM

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Abstract

The present invention concerns new combinations of an anti-emetic agent and an enkephalinase inhibitor, the uses of said combinations for treating diarrhea and / or gastroenteritis.

Description

Background of the invention [0001] Gastroenteritis is an infectious disease caused by a variety of bacteria, viruses or parasites. [0002] Gastroenteritis basically manifests itself as diarrhea (ie net excess secretion of water and electrolytes in the intestine), nausea, vomiting and abdominal pain. Of these symptoms, those that lead to loss of fluid and electrolytes, namely vomiting and dehydration, are particularly dangerous for young children, with dehydration a potentially life-threatening condition. [0003] Infectious diseases have long been treated through the use of narcotics (or opioids), anti-infectives, and oral rehydration solutions, but each of these treatments has drawbacks. In infants, anesthetics tend to increase bacterial infection and nausea, induce vomiting and reactive constipation, and have potential CNS toxicity; anti-infective agents are effective against only a small subset of precipitating factors; rehydration solutions, although highly recommended f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/4178A61K31/439A61K31/265A61P1/12
CPCA61K45/06A61K31/439A61K31/265A61K31/4178A61P1/00A61P1/04A61P1/08A61P1/12A61P31/04A61P31/12A61P33/00A61P43/00A61K2300/00
Inventor J-C·施瓦特兹J-M·勒康特
Owner BIOPROJET
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