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Oral formulations and uses thereof

A tablet and diluent technology, applied in their production, can solve the problems of changing the physical and chemical properties of the preparation, production problems, product instability, etc.

Pending Publication Date: 2020-09-15
EUSTRALIS PHARMA LIMITED TRADING AS PRESSURA NEURO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Further, adding diluents to the formulation may also change the physicochemical properties of the formulation, which may make the product unstable and may cause problems in production

Method used

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  • Oral formulations and uses thereof
  • Oral formulations and uses thereof
  • Oral formulations and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0155] preformulation research

[0156] Characterization of Active Pharmaceutical Ingredient (API)

[0157] Compound (Ia) HCl(API) is an acidic compound with a pH of about 2.5. Compounds of formula (I), especially compound (Ia) shown below, especially the dihydrochloride salt of compound (Ia) (compound (Ia) 2HCl), were used in all examples.

[0158]

[0159] granularity

[0160] The particle size distribution of compound (Ia)2HCl(API) was determined using a Malvern Mastersizer. The results obtained are summarized in Table 1. D(0.1) means that 10% of the sample is present as particles smaller than this size. D(0.5) means that 50% of the sample is present in the form of particles smaller than this size. D(0.9) means that 90% of the sample is present in the form of particles smaller than this size.

[0161] Table 1: Particle size distribution of compound (Ia)

[0162]

[0163] bulk density and tap density

[0164] Measurements of bulk density and tap density ...

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Abstract

Disclosed are therapeutic oral formulations comprising particular substituted pyridine based compounds, their manufacture, and methods and uses of said formulations in treating substance P mediated pathways in the brain such as elevated intracranial pressure or the modification of expression of (hyper)-phosphorylated tau protein (tau) in the brain for indications such as, but not limited to concussion, post-concussive (or post-concussion) syndrome (PCS), chronic traumatic encephalopathy (CTE), traumatic brain injury (TBI) and stroke.

Description

technical field [0001] The present invention generally relates to therapeutic oral formulations comprising specific substituted pyridine-based compounds, their manufacture, and the formulations for indications in the treatment of substance P-mediated pathways in the brain such as elevated intracranial pressure or in the brain (ultrasonic ) methods and uses for altering the expression of phosphorylated tau protein (τ), such as but not limited to concussion, post-concussion (or post-concussion) syndrome (PCS), chronic traumatic encephalopathy (CTE), Traumatic brain injury (TBI) and stroke. Background technique [0002] Traumatic brain injury (TBI), also known as an intracranial injury, occurs when an external force injures the brain. TBI can be classified according to severity, mechanism (closed or penetrating brain injury), or other characteristics (eg, occurrence in a specific location or broad area). TBI can cause physical, cognitive, social, emotional, and behavioral sym...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/26A61P25/00
CPCA61K31/496A61P43/00A61P9/10A61K9/20A61P25/00A61K9/2018A61K9/2054A61K9/2059A61K9/2009A61K9/2013A61K9/1611A61K9/1623A61K9/1641A61K9/1652A61K9/2081A61K9/5047A61K9/1617
Inventor P·万坎A·萨萨曼G·B·威尔姆布里克
Owner EUSTRALIS PHARMA LIMITED TRADING AS PRESSURA NEURO
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