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Allicin fatty milk injection and preparation technics thereof

A technology of allicin and fat emulsion, which is applied in the directions of emulsion delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low water solubility, phlebitis in patients, and influence on clinical use of drugs

Inactive Publication Date: 2008-01-30
福州璐珈医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current clinical use of garlicin injection has a special odor and irritation, which is difficult for patients to accept
The water solubility of allicin is very low, and cosolvents and solubilizers need to be added during the preparation process to increase water solubility. Cosolvents and solubilizers are usually Tween-80 substances, which can also cause hemolytic reactions and are harmful to patients. Major side effects
The stability of the allicin aqueous solution is relatively poor, and it is easy to decompose when exposed to light and air during storage, resulting in a decrease in the content and an increase in adverse reactions; clinically, the allicin injection is mostly administered intravenously, and it needs to be instilled slowly, accompanied by The feeling of tingling and fever on the vessel wall makes the patient's pain unbearable, and some patients may have side effects such as phlebitis, which affects the clinical use of the drug

Method used

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  • Allicin fatty milk injection and preparation technics thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0030] Take 2 grams of egg yolk lecithin, 0.50 grams of oleic acid, 0.5 grams of vitamin E, and 10 grams of soybean oil in the prescribed amount, mix, heat to 70 ° C, and stir to dissolve. Then add 100 mg of allicin and stir until dissolved. After 0.22 μm The polytetrafluoroethylene microporous filter membrane is pressurized at 5 MPa to filter to obtain the filtrate; take 1 gram of glycerin in the prescribed amount, add 90 grams of water for injection at normal temperature, add 50 mg of disodium edetate, and 0.5 gram of Pluronic F68 to mix, and stir until Dissolved, filtered through a 0.22 μm polytetrafluoroethylene microporous filter membrane and pressurized at 5 MPa to obtain the filtrate; the two filtrates were mixed at room temperature, stirred with a high-speed mixer at a speed of 8000 rpm, and the high-pressure homogenizer was controlled at a pressure of 50000 psi, and the pH of the mixed solution was 7.2, namely It is an allicin fat emulsion product. The oil phase partic...

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Abstract

The invention discloses an allicin fat emulsion injection and a preparation process thereof; the invention is the drug which is made by the materials with the following mix ratios by weight, while the pH value of which is 6.5 to 7.5, the average particle size of the emulsion particles is 200nm, and the particle size thereof is 100 to 300nm and the Zeta potential is minus 50 to 80mv. The raw materials are: allicin, egg yolk lecithin, pluronic F68, oleic acid, and injection water and so on. The preparation process is that the egg yolk lecithin, oleic acid, vitamin E and soya bean oil are taken at first under the aseptic conditions for mixing, heating, agitating and dissolving, then the allicin is added to agitate till dissolution, and the filtrate can be obtained after the pressure filtration by a microporous membrane; the glycerol is taken at first and the injection water, disodium ethylene diamine tetraacetate and pluronic F68 are added for mixing and agitating till the dissolution, then the filtrate can be obtained after the pressure filtration by the microporous membrane; after the mixture of the two filtrates, a high speed agitator is used for agitating, the product is finally obtained through a high pressure homogenizer. The invention is characterized by no irritating effect and good stability, etc.

Description

Technical field: [0001] The invention relates to an allicin fat emulsion injection and a preparation process thereof. Background technique: [0002] Allicin is a hydrophobic drug, which has good antiviral effects and is easily soluble in oil-phase solvents. The current clinical use of allicin injection has a special odor and irritation, which is difficult for patients to accept. The water solubility of allicin is very low, and cosolvents and solubilizers need to be added during the preparation process to increase water solubility. Cosolvents and solubilizers are usually Tween-80 substances, which can also cause hemolytic reactions and are harmful to patients. Larger toxic side effects. The stability of the allicin aqueous solution is relatively poor, and it is easy to decompose when exposed to light and air during storage, resulting in a decrease in the content and an increase in adverse reactions; clinically, the allicin injection is mostly administered intravenously, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/10A61K36/8962A61K47/18A61P31/12
Inventor 谢开智
Owner 福州璐珈医药科技有限公司
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