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Compositions for delivery of ladostigil

A technology of radotidine and composition, which is applied in the field of compositions for delivering radotidine, and can solve problems such as exacerbating variability and the like

Pending Publication Date: 2022-01-28
YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is undesirable and may exacerbate any variability in response to treatment with radotege in potential patients

Method used

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  • Compositions for delivery of ladostigil
  • Compositions for delivery of ladostigil
  • Compositions for delivery of ladostigil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Comparison of Oral and Rectal Administration of Radotege in Rats

[0052] Methods: Male Wister rats weighing 250-270 g were used for these experiments. Radotege was administered by intragastric gavage at a dose of 5 mg / kg (volume 0.25ml-0.27ml). In other rats, the same dose of radotege was administered via a cannula that was gently inserted into the rectum and pushed forward to reach the colon. Rats were anesthetized with isoflurane 0 min, 15 min, 30 min, 60 min or 120 min after radotege administration and sacrificed by decapitation. Brains were removed and cortices were carefully dissected and stored at -80°C until further analysis. Blood was collected in heparinized Eppendorf tubes, centrifuged at 20,800 g for 10 min at 4°C, and plasma was stored at -80°C until further analysis.

[0053] Following methanol precipitation of proteins in plasma and cortical extracts, samples were prepared for LC-MS analysis as described in Moradov et al. (2015). Briefly, 7...

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Abstract

The invention provides compositions comprising ladostigil, being a colonic delivery composition, including methods and uses thereof.

Description

[0001] Background of the invention [0002] Oxidative stress resulting from impaired mitochondrial function and leading to overproduction of reactive oxygen species plays a key role in the etiology of Alzheimer's disease (AD) (Sayre et al. 2008; Smith et al. 2005). Impaired mitochondrial function in AD (Valla et al. 2001) is accompanied by microglial activation that increases the release of proinflammatory cytokines (Maccioni et al. 2009; Mangialasche et al. 2009). Oxidative stress and activation of microglia have been observed in the brains of subjects with mild cognitive impairment (MCI) prior to the development of AD (Butterfield et al. 2007; Okello et al. 2009; Yasuno et al. 2012; Pardo et al. 2017). [0003] Ladostigil (Scheme 1) 6-(N-Ethyl, N-methyl, carbamoyloxy)-N-propargyl-1(R)-aminoindan tartrate may be neuroprotective Metacellular cells are protected from damage induced by oxidative stress (Weinstock et al. 2001) and stimulate the activity of antioxidant enzymes (Ba...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P25/28A61K31/325A61K9/00A61K31/27
CPCA61P25/28A61K31/27A61K9/0031A61K9/0053
Inventor 玛塔·温斯塔克-罗辛
Owner YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD