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Traditional Chinese medicine sharpening-mind and inducing-consciousness microemulsion nasal cavity spraying agent and preparation method thereof

A nasal spray, resuscitating and brain-invigorating technology, which is applied in medical formula, aerosol delivery, drug combination, etc., can solve the problems of lower patient compliance, complicated process, and poor stability of traditional Chinese medicine injections, etc., so as to improve bioavailability The effect of reducing toxicity, reducing side effects, and convenient administration

Inactive Publication Date: 2009-12-09
广东同德药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The traditional pills have the following disadvantages in the first aid of cerebrovascular diseases: ①The drug is destroyed by enzymes in the gastrointestinal tract and the first-pass effect of the liver; ②It is difficult to break through the blood-brain barrier, and it is difficult to quickly and effectively treat brain diseases
(2) After the drug is absorbed, it enters the systemic circulation directly, without the first-pass effect of the liver, and the activity of proteolytic enzymes in the nasal mucosa is low. Drug-like drug is an effective route of administration
[0006] Patent No. 200410097167.0 "A Xingnaojing Dropping Pill for the Treatment of Encephalitis and Hepatic Coma and Its Preparation Method" is made of four traditional Chinese medicines such as musk, turmeric, borneol, and gardenia as the main medicine, and is made with various auxiliary materials Dropping pills; Patent No. 200610072942.6 "Xingnaojing solid dispersion pharmaceutical composition and its preparation and preparation method" is based on musk, turmeric volatile oil, turmeric total curcumin, borneol, gardenia total glycosides, etc. Dispersion preparations made of a variety of excipients, such as: dropping pills, capsules, tablets, etc.; the above dosage forms are oral pharmaceutical preparations, and oral preparations, especially traditional Chinese medicine oral preparations, have long dissolution time and low dissolution rate after taking , poor absorption, hepatic and intestinal first-pass effect, and low bioavailability, which affect the efficacy of the drug and directly affect the therapeutic effect; at the same time, the preparation process of oral preparations is complicated and the production cost is high, which leads to the cost of medication The subsequent increase is not conducive to improving the ability of the majority of patients to seek medical treatment, and is not conducive to improving the level of social health
[0007] Patent No. 200510077199.9 "A Nano-Xingnaojing Injection Preparation and Its Preparation Method" is a traditional Chinese medicine injection based on the four medicinal materials of musk, turmeric, borneol, and gardenia; Changes in pH value, darker appearance, and even turbidity and precipitation appear, which seriously affect the safety of drugs; at the same time, because Chinese medicine injections contain proteins, polysaccharides, polypeptides and other substances, the extraction purity is not enough, and the components interact. Factors such as compatibilizers are likely to lead to allergies; and injections reduce patient compliance, and the use is subject to certain restrictions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] (1) Take 30 parts of turmeric and 40 parts of gardenia, grind them, add 1500ml of purified water to distill, and collect 1000ml of distillate;

[0031] (2) Grind 10 parts of artificial musk into fine powder and set aside; grind 2 parts of borneol into fine powder and set aside;

[0032] (3) Measure the extract, add 10 parts of 1,2-propanediol and 10 parts of glycerin, heat to clarify, continue heating and stirring to make the temperature reach 62°C and keep it constant;

[0033] (4) Take borneol powder, 1 part of egg yolk phospholipid, 1 part of lecithin, and 2 parts of soybean lecithin, add appropriate amount of absolute ethanol to dissolve, then add 10 parts of refined soybean oil, 2 parts of vitamin E, and 2 parts of cholic acid, and heat Stir to bring the temperature to 60°C and keep it constant;

[0034] (5) Slowly add the solution obtained in step 3 to the solution obtained in step 4 at constant temperature, while stirring evenly, add 10 parts of polyoxyethylene-...

Embodiment 2

[0038] (1) Get 35 parts of turmeric and 45 parts of gardenia and grind them into pieces, add 1500ml of purified water to distill, and collect 1000ml of distillate;

[0039] (2) Grind 15 parts of artificial musk into fine powder and set aside; grind 4 parts of borneol into fine powder and set aside;

[0040] (3) Measure the extract, add 15 parts of 1,2-propanediol and 15 parts of glycerin, heat to clarify, continue heating and stirring to make the temperature reach 62°C and keep it constant;

[0041] (4) Take borneol powder, 3 parts of egg yolk phospholipids, 1 part of lecithin, 3 parts of soybean lecithin, add appropriate amount of absolute ethanol to dissolve, then add 15 parts of refined soybean oil, 2 parts of vitamin E, 2 parts of cholic acid, heat Stir to bring the temperature to 60°C and keep it constant;

[0042] (5) Slowly add the solution obtained in step 3 to the solution obtained in step 4 at constant temperature, while stirring evenly, add 15 parts of polyoxyethyl...

Embodiment 3

[0046] (1) Get 40 parts of turmeric and 50 parts of gardenia, grind them, add 1500 ml of purified water to distill, and collect 1000 ml of distillate;

[0047] (2) Grind 20 parts of artificial musk into fine powder and set aside; grind 8 parts of borneol into fine powder and set aside;

[0048] (3) Measure the extract, add 20 parts of 1,2-propanediol and 15 parts of glycerin, heat to clarify, continue heating and stirring to make the temperature reach 62°C and keep it constant;

[0049] (4) Take borneol powder, 6 parts of egg yolk phospholipids, 4 parts of lecithin, 10 parts of soybean lecithin, add appropriate amount of absolute ethanol to dissolve, then add 30 parts of refined soybean oil, 4 parts of vitamin E, 4 parts of cholic acid, and heat Stir to bring the temperature to 60°C and keep it constant;

[0050] (5) Slowly add the solution obtained in step 3 to the solution obtained in step 4 at constant temperature, while stirring evenly, add 20 parts of polyoxyethylene-9-l...

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Abstract

The invention relates to a traditional Chinese medicine sharpening-mind and inducing-consciousness microemulsion nasal cavity spraying agent and a preparation method thereof. The traditional Chinese medicine sharpening-mind and inducing-consciousness microemulsion nasal cavity spraying agent comprises 10 to 20 parts of artificial musk, 2 to 8 parts of borneol, 30 to 40 parts of turmeric, 40 to 50 parts of gardenia, 10 to 20 parts of polyoxyethylene-9-laurel ether, 5 to 8 parts of sulfo-lauryl alcohol, 1 to 6 parts of yolk phospholipid, 1 to 4 parts of lecithin, 2 to 10 parts of bean phospholipid, 2 to 4 parts of vitamin E, 10 to 30 parts of refined soybean oil, 10 to 20 parts of 1,2-propylene glycol, 10 to 15 parts of glycerol, 2 to 4 parts of cholic acid, a right amount of ethanol, a right amount of purified water, a right amount of essence and a right amount of propellant. The traditional Chinese medicine sharpening-mind and inducing-consciousness microemulsion nasal cavity spraying agent has the functions of clearing away heat and toxic material, removing heat from the blood, cooling blood, promoting blood circulation, sharpening mind and inducing consciousness, is natural, innoxious, safe, effective and biodegradable, is clinically used for treating various cerebrovascular diseases and is especially effective to central coma diseases, such as disturbance of consciousness, serious symptom craniocerebral injury, cerebral hemorrhage, cerebral infarction, drug poisoning, and the like; and the medicine realizes cerebral targeting administration by the approach of a nose, can break through blood-brain barriers, can rapidly exert actions and also has convenient administration.

Description

technical field [0001] The invention relates to a traditional Chinese medicine resuscitating and refreshing microemulsion nasal cavity spray, in particular to a traditional Chinese medicine microemulsion nasal cavity spray with the functions of clearing away heat and detoxification, cooling blood and promoting blood circulation, and resuscitating and refreshing the brain, belonging to the technical field of medicines. Background technique [0002] Traditional pills have the following disadvantages in first aid for cerebrovascular diseases: ① drugs are destroyed by enzymes in the gastrointestinal tract and first-passed by the liver; ② it is difficult to break through the blood-brain barrier, and it is difficult to quickly and effectively treat brain diseases. [0003] Nasal drug delivery system (NDDS) refers to preparations that are used in the nasal cavity and absorbed through the nasal mucosa to exert local or systemic effects. The total volume of the human nose is 15ml, an...

Claims

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Application Information

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IPC IPC(8): A61K36/9066A61K9/12A61K9/107A61K47/44A61P25/00A61K31/122A61K31/045
Inventor 周小萍林文辉蒋宇亮林柳清
Owner 广东同德药业有限公司
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