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
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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
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
15
1.5
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
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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