Medical purpose of NMDA acceptor antagonist and pharmaceutical composition thereof

A receptor antagonist and composition technology, which can be applied to drug combinations, medical preparations containing active ingredients, and pharmaceutical formulations, etc., can solve the problems of inability to reach brain tissue, high drug elimination rate, and poor administration compliance. Achieve the effect of avoiding irritation and liver first-pass effect, high bioavailability and reducing dosage

Inactive Publication Date: 2016-02-17
SHANGHAI HANSOH BIOMEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] It is worth noting that the above-mentioned administration methods all deliver the drug to the blood and then reach the central nervous system through the systemic circulation, so before reaching the brain, GLYX-13 will be mostly eliminated by the body and cannot reach the brain tissue
In addition, the intravenous injection method itself still has the problem of patient compliance, because patients cannot inject intravenously by themselves, and must go to a medical institution to complete the administration, which brings great inconvenience to patients
[0012] Therefore, it is very necessary to solve the problems of high drug elimination rate and poor drug compliance caused by current drug delivery methods through new drug delivery methods and preparations.

Method used

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  • Medical purpose of NMDA acceptor antagonist and pharmaceutical composition thereof
  • Medical purpose of NMDA acceptor antagonist and pharmaceutical composition thereof
  • Medical purpose of NMDA acceptor antagonist and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 1. Formulation

[0050] Component

Mass (g)

Composition (W / V,%)

GLYX-13

200

20

Poloxamer 407

100

10

Poloxamer 188

10

1

[0051] Azone

5

0.5

Sodium chloride

9

0.9

Ethyl p-hydroxybenzoate

1

0.1

Hydrochloric acid / sodium hydroxide

Right amount

/

Water for Injection

Add to 1000ml

/

[0052] 2. Preparation method

[0053] Take 900ml of water for injection, add the prescription amount of ethyl p-hydroxybenzoate, sodium chloride and azone, stir to dissolve. Take the prescription amount of Poloxamer 407 and Poloxamer 188, and disperse them in the above solution to make the volume swell completely into a clear solution. Add the prescription amount of GLYX-13, and adjust the pH to 5.0-7.4 after dissolution. Get it in subpackages.

Embodiment 2

[0055] 1. Formulation

[0056] Component

Mass (g)

Composition (W / V,%)

GLYX-13

200

20

Poloxamer 407

200

20

Poloxamer 188

50

5

Azone

15

1.5

Sodium chloride

9

0.9

Ethyl p-hydroxybenzoate

3

0.3

Hydrochloric acid / sodium hydroxide

Right amount

/

Water for Injection

Add to 1000ml

/

[0057] 2. Preparation method

[0058] Take 900ml of water for injection, add the prescription amount of ethyl p-hydroxybenzoate, sodium chloride and azone, stir to dissolve. Take the prescription amount of Poloxamer 407 and Poloxamer 188, and disperse them in the above solution to make the volume swell completely into a clear solution. Add the prescription amount of GLYX-13, and adjust the pH to 5.0-7.4 after dissolution. Dispense into the squeeze type nasal cavity drug delivery device.

Embodiment 3

[0060] 1. Formulation

[0061] Component

Mass (g)

Composition (W / V,%)

GLYX-13

50

5

Poloxamer 407

255

25.5

[0062] Poloxamer 188

50

5

Bezoar Sodium Deoxycholate

50

5

Sodium chloride

9

0.9

Ethyl p-hydroxybenzoate

1

0.1

Hydrochloric acid / sodium hydroxide

Right amount

/

Water for Injection

Add to 1000ml

/

[0063] 2. Preparation method

[0064] Take 900ml of water for injection, add the prescription amount of ethyl p-hydroxybenzoate, sodium chloride and sodium bezoar deoxycholate, stir to dissolve. Take the prescription amount of Poloxamer 407 and Poloxamer 188, and disperse them in the above solution to make the volume swell completely into a clear solution. Add the prescription amount of GLYX-13, and adjust the pH to 5.0-7.4 after dissolution. Dispense it into a spray-type nasal cavity drug delivery device.

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PUM

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Abstract

The invention discloses a medical purpose of an NMDA acceptor antagonist and a pharmaceutical composition thereof. The invention concretely discloses a medicine for using the NMDA acceptor antagonist, a pharmaceutically acceptable salt or a pharmaceutical composition thereof for treating or preventing central nervous system disease and/or mental diseases, and the NMDA acceptor antagonist is delivered to a human central nervous system through target administration. An application of the pharmaceutical composition can increase the concentration of the NMDA acceptor antagonist in brain tissue, medicine amount is greatly reduced, and systematic side effect is reduced; biology availability in the brain is high, autonomous drug administration can be carried out by patients, no pain is generated, usage is convenient, and thus the pharmaceutical composition has good patient compliance, and has wide clinical medical science application.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the medical use of an NMDA receptor antagonist and a pharmaceutical composition containing the NMDA receptor antagonist. Background technique [0002] Depression is a kind of mental disorder, with significant and lasting depression as the main clinical feature, and it is the main type of affective disorder. Clinically, it can be seen that depression is not commensurate with the situation. Emotional depression can range from gloomy to grief, low self-esteem, depression, or even pessimism, suicide attempts or behavior; even stupor; some cases have obvious anxiety and motor agitation; In severe cases, psychotic symptoms such as hallucinations and delusions may occur. Each attack lasts for at least 2 weeks, the elderly or even several years. Most cases have a tendency to recur. Most of each attack can be relieved, and some may have residual symptoms or become chronic. [0003]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K45/06A61K9/06A61K9/12A61K9/14A61P25/24A61P25/28A61P25/08A61P25/04A61P25/36
CPCA61K31/4025A61K38/07
Inventor 王培全张磊周夏君李成海包如迪徐耀昌
Owner SHANGHAI HANSOH BIOMEDICAL
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