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Drug administration preparations of ligustrazine for nasal mucosa and method for preparing the same

A technology of ligustrazine and nasal mucosa, applied in the field of medicine, can solve the problems of loss of curative effect, low oral bioavailability of ligustrazine, influence of curative effect, etc., to increase convenience, avoid first-pass effect of gastrointestinal tract and liver, capillary blood vessels, etc. rich effects

Inactive Publication Date: 2008-04-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the existence of the blood-brain barrier (blood-brain barrier.BBB), a natural physiological barrier of brain tissue, more than 95% of powerful drugs cannot pass through the blood-brain barrier and lose their curative effect.
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
However, the oral bioavailability of ligustrazine is very low, which affects its curative effect.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Preparation of Ligustrazine Nasal Drops Solution: Chitosan was weighed to make a 1% solution, and 7% nicotinamide was added as a cosolvent. Weigh the prescribed amount of ligustrazine, add it to the above-mentioned chitosan / nicotinamide mixed solution under stirring to make a solution containing ligustrazine 20 mg / ml, add the preservative benzalkonium bromide, stir, and adjust the pH value of the solution 6.0, filtered, sterilized, subpackaged, that is.

Embodiment 2

[0019] Embodiment 2: the preparation of ligustrazine nasal drop solution: take by weighing HP-β cyclodextrin and make 30% solution, take the ligustrazine of recipe quantity and join in the above-mentioned HP-β cyclodextrin solution under stirring condition , make a solution containing Ligustrazine 20 mg / ml, add preservative benzalkonium bromide, stir, adjust the pH value of the solution to 6.0, filter, sterilize, and subpackage to obtain.

Embodiment 3

[0020] Example 3: Preparation of Ligustrazine Nasal Drops Solution: Weigh HP-β cyclodextrin to make a 30% solution, add 1% chitosan and stir to dissolve. Take the Ligustrazine of recipe quantity, join in above-mentioned chitosan / HP-β cyclodextrin mixed solution under stirring condition, make the solution containing Ligustrazine 20mg / ml, add antiseptic benzalkonium bromide, stir, Adjust the pH value of the solution to 6.0, filter, sterilize, and subpackage to obtain.

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PUM

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Abstract

The invention belongs to medical technical field and discloses nasal mucosa medication agent of tetramethylpyrazine and the preparation method. The agent contains tetramethylpyrazine, pharmaceutical excipient and absorption enhancer. The weight percentage is 1:0.1 to 100:0.1 to 10. The tetramethylpyrazine includes tetramethylpyrazine prepared in various methods and salts of tetramethylpyrazine. Formula dosage of tetramethylpyrazine is put into absorption enhancer and additional pharmaceutical solutions of suitable concentration prepared in advance to produce nasal mucosa medication agent, such as nasal drops, spray, aerosol, microsphere agent, liposomes, etc. Via the special physiological structure of nasal cavity, the agent medicates via nasal mucosa and allows tetramethylpyrazine bypasses the blood-brain barrier to enhance the distribution of medicine in brain tissue. The drug can be used to treat migraine, cerebral ischemia, cerebral embolism and emergencies such as angina pectoris, coronary heart disease, myocardial infarction, etc, and the drug has the advantages of complete and rapid absorption, high treating effects, high stability, and few side effects.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a nasal mucosa administration preparation of ligustrazine and a preparation method thereof. The nasal mucosa preparation can be used for treating migraine, and can also be used for emergencies such as cerebral ischemia, cerebral embolism, angina pectoris, coronary heart disease, and acute infarction. The treatment has the advantages of good absorption, rapid absorption, high curative effect, good stability and few side effects. Background technique [0002] There are a large number of patients suffering from central nervous system (central nervous sysem.CNS) diseases, including periodic migraines, brain tumors, and central nervous system infections. However, due to the existence of the blood-brain barrier (blood-brain barrier.BBB), a natural physiological barrier of brain tissue, more than 95% of powerful drugs cannot pass through the blood-brain barrier and lose their curative ef...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61K9/12A61K9/127A61K9/16A61K9/72A61P9/10
Inventor 毛世瑞梅丹
Owner SHENYANG PHARMA UNIVERSITY
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