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Citicoline sodium brain-targeting thermosensitive gel and preparation method thereof

A technology of citicoline sodium and temperature-sensitive gel, which is applied in the field of citicoline sodium brain-targeted temperature-sensitive gel and its preparation, achieving the effects of strong targeting, good fluidity, and reduced toxic and side effects

Active Publication Date: 2012-07-18
四川梓橦宫药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is a paradox in the current neuropharmaceutical research: more than 99% of the global central nervous system drug development is used to find new drugs, and less than 1% is used to study drug delivery systems

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A citicoline sodium brain-targeted temperature-sensitive gel, using water as a solvent, includes the following solute components:

[0030] Citicoline sodium 200mg / ml, Tween 800.5mg / ml, phospholipid E80 1.5mg / ml, poloxamer P188 0.5mg / ml, poloxamer P40 75.0mg / ml. The pH of Citicoline Brain Targeting Thermosensitive Gel was adjusted to 6.0.

[0031] The preparation method is:

[0032] Phospholipid E80 is used to form the oil phase; citicoline sodium, poloxamer P188, and Tween 80 are dissolved in distilled water to form the water phase. The two phases are heated to 50°C respectively, and the oil phase is added to the water phase. High-speed shearing for 4 minutes to obtain colostrum;

[0033] The colostrum is subjected to high-pressure homogenization twice under the pressure of 1000 bar, and the homogenization cycle is repeated 5 times to obtain the final milk, which is adjusted to pH 6.0, and filtered with a 0.8 μm microporous membrane to obtain an emulsion;

[0034] Th...

Embodiment 2

[0036] A citicoline sodium brain-targeted temperature-sensitive gel, using water as a solvent, includes the following solute components:

[0037] Citicoline sodium 250mg / ml, Tween 803.0mg / ml, phospholipid E805.0mg / ml, poloxamer P1883.0mg / ml, poloxamer P40710.0mg / ml. The pH of Citicoline Brain Targeting Thermosensitive Gel was adjusted to 6.5.

[0038] The preparation method is:

[0039] Phospholipid E80 is used to form the oil phase; citicoline sodium, poloxamer P188, and Tween 80 are dissolved in distilled water to form the water phase. The two phases are heated to 60°C respectively, and the oil phase is added to the water phase. High-speed shearing for 5 minutes to obtain colostrum;

[0040]The colostrum is homogenized under high pressure twice under the pressure of 1100bar, and the homogenization cycle is repeated 5 times to obtain the final milk. The pH of the final milk is adjusted to 6.5, and the emulsion is obtained by filtering with a 0.8 μm microporous membrane;

...

Embodiment 3

[0043] Citicoline sodium 150mg / ml, Tween 801.0mg / ml, phospholipid E802.0mg / ml, poloxamer P1881.0mg / ml, poloxamer P4077.0mg / ml. The pH of Citicoline Brain Targeting Thermosensitive Gel was adjusted to 7.0.

[0044] The preparation method is:

[0045] Phospholipid E80 is used to form the oil phase; citicoline sodium, poloxamer P188, and Tween 80 are dissolved in distilled water to form the water phase. The two phases are heated to 70°C respectively, and the oil phase is added to the water phase. High-speed shearing for 6 minutes to obtain colostrum;

[0046] The colostrum is subjected to high-pressure homogenization twice under the pressure of 1000-1500 bar, and the homogenization cycle is repeated 5 times to obtain the end milk. The pH of the end milk is adjusted to 7.0, and the emulsion is obtained by filtering with a 0.8 μm microporous membrane;

[0047] The prescribed amount of poloxamer P407 was stirred and dispersed in the emulsion, and left to dissolve at 4°C to obtain ...

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Abstract

The invention discloses citicoline sodium brain-targeting thermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel is a preparation which can be absorbed fast and has high bioavailability. The citicoline sodium brain-targeting thermosensitive gel utilizes water as a solvent and comprises solute components of 10 to 400mg / ml of citicoline sodium, 0.1 to 3.0mg / ml of Tween-80, 0.5 to 5.0mg / ml of phosphatide E80, 0.5 to 3.0mg / ml of poloxamer P188, and 5.0 to 10.0mg / ml of poloxamer P407. The invention also discloses a preparation method of the citicoline sodium brain-targetingthermosensitive gel. The citicoline sodium brain-targeting thermosensitive gel has a high drug loading amount, is uniform and stable, has good fluidity, is in a state of gel at a temperature of 33 DEG C, has good biological adhesion strength, is suitable for being applied through a nasal cavity, has a good appearance, and does not produce floating oil and layering.

Description

technical field [0001] The embodiments of the present invention relate to a medicine and a preparation method thereof, in particular to a citicoline sodium brain-targeted thermosensitive gel and a preparation method thereof. Background technique [0002] Citicoline (CDPC) is a nucleoside derivative, the chemical name is cytosine nucleoside diphosphate choline, it participates in the biosynthesis of lecithin in the body, it is an activator of brain metabolism, and it can enhance the activation of the ascending network structure. function, reduce cerebrovascular resistance, increase cerebral blood flow, improve cerebral blood circulation, promote brain substance metabolism, and restore function. [0003] The adverse reaction of citicoline sodium is relatively small, and it is used for the treatment of ischemic stroke. It has a significant effect on dizziness, headache, insomnia, memory loss, optic atrophy, inattention, etc.; Obstacles are more satisfactory. The total effecti...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/7068A61K47/34A61P9/10A61P25/00
Inventor 唐铣刘新峰陈健蒋学华黄学兵
Owner 四川梓橦宫药业股份有限公司
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