Pharmaceutical composition for preventing and treating central nervous system diseases containing fluoxetine and vitamin c as active ingredients

a technology of fluoxetine and active ingredients, applied in the direction of nervous disorders, pharmaceutical delivery mechanisms, medical preparations, etc., can solve the problems of secondary injury of neurons, damage to neuronal signaling, cerebral edema, etc., and achieve the effect of preventing blood-brain damage, reducing side effects, and preventing and treating blood-brain damag

Inactive Publication Date: 2020-10-08
UNIV IND COOP GRP OF KYUNG HEE UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The co-administration of fluoxetine and vitamin C at specific concentrations significantly reduces blood-brain barrier permeability and MMP-9 activity, improving treatment outcomes for blood-brain barrier disorders and central nervous system diseases with reduced side effects.

Problems solved by technology

Most brain injuries such as cerebral infarction and trauma are associated with the disruption of the blood-brain barrier, and this in turn causes a secondary injury of neurons.
As the blood-brain barrier becomes loose due to a certain reason, the permeability to the blood serum proteins increases and the blood plasma filtrate leaks out through the intercellular space thereby causing cerebral edema.
This is the major cause of dysfunction and death with symptoms such as seizure, brain infection, head injury, brain tumor, and multiple sclerosis.
Additionally, when the balance is broken in the neurotransmitters and minute ions in the extracellular fluid, it damages neuronal signaling, and subsequently the damage in the functionalization of recognition, neuropsychiatric impairment, or epileptic seizure.
However, there has been no report regarding the effect of fluoxetine and vitamin Con the alleviation of the injury of blood-brain barrier.

Method used

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  • Pharmaceutical composition for preventing and treating central nervous system diseases containing fluoxetine and vitamin c as active ingredients
  • Pharmaceutical composition for preventing and treating central nervous system diseases containing fluoxetine and vitamin c as active ingredients
  • Pharmaceutical composition for preventing and treating central nervous system diseases containing fluoxetine and vitamin c as active ingredients

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Embodiment Construction

[0043]Hereinafter, the present invention will be explained in details.

[0044]The present invention provides a pharmaceutical composition for the prevention and treatment of blood-brain barrier disorders containing fluoxetine and vitamin C as active ingredients.

[0045]Fluoxetine and vitamin C are preferably mixed in a ratio from 1:500 to 1:10, specifically, more preferably mixed in a ratio from 1:200 to 1:50, and more specifically, most preferably mixed in a ratio from 1:100, but the mixing ratio is not limited thereto.

[0046]Fluoxetine is preferably included at a concentration of 0.1 mg / kg to 10 mg / kg, specifically, more preferably included 0.5 mg / kg to 5 mg / kg, more specifically, most preferably included 0.8 mg / kg to 2 mg / kg, but the content is not limited thereto. When fluoxetine is included more than 10 mg / kg, fluoxetine alone can exhibit the effects of prevention and treatment of the blood-brain barrier disorders, whereas when fluoxetine is included equal to or less than 10 mg / kg, ...

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Abstract

The present invention relates to a pharmaceutical composition for the prevention and treatment of blood-brain barrier disorder and central nervous system diseases containing fluoxetine and vitamin C as active ingredients. Specifically, when low concentration of fluoxetine and vitamin C, which did not show any improved effect on the blood-brain barrier disorder and disruption of blood-spinal cord barrier when administered alone, were mixed and co-administered to an animal model with spinal cord injury and transient global ischemia, the co-administration significantly increased the effect of inhibiting the increase of permeability of blood-spinal cord barrier and the effect of inhibiting MMP-9 activation and the effect of alleviating the influx of blood cells in an animal model with spinal cord injury; and the effect of inhibiting the disruption of blood-brain barrier and the effect of recovering memory in a transient global ischemia animal model, compared to the single administration of fluoxetine or vitamin C at the same concentration. The results indicate the synergy effect and the decrease of side effects by the co-administration of the compound at a low concentration, and thus fluoxetine and vitamin C of the present invention can be effectively used as active ingredients for a pharmaceutical composition for the prevention and treatment blood-brain barrier disorder and central nervous system diseases.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This is a divisional of U.S. patent application Ser. No. 15 / 141,652, filed on Apr. 28, 2016, which is a continuation of PCT Application No. PCT / KR2013 / 012427, filed on Dec. 31, 2013, which claims priority under 35 U.S.C. § 119 to Korean Patent Application No. 10-2013-0131730, filed on Oct. 31, 2013. The prior applications are all incorporated herein by reference.TECHNICAL FIELD[0002]The present disclosure relates to a pharmaceutical composition for the prevention and treatment of blood-brain barrier disorders and central nervous system diseases containing fluoxetine and vitamin C as active ingredients.BACKGROUND ART[0003]There is a kind of a barrier present in the neural tissue that prevents particular materials from entering the blood vessels. This functional barrier is called blood-brain barrier (BBB, or blood-brain portal). Blood-brain barrier is in a shape in which brain capillaries capable of maintaining homeostasis of the microenvir...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/375A61K31/138A23L33/10A23L33/15A61K9/00
CPCA23V2002/00A61K9/0053A23L33/10A61K31/138A23L33/15A61K31/375A61P25/00A61K2300/00A61K31/135
InventorYUNE, TAE YOUNGBAIK, HYUNG-HWANLEE, JEE YOUNKIM, SAM
OwnerUNIV IND COOP GRP OF KYUNG HEE UNIV