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Asarone lipidosome injection

A technology of caprylyl and injection, which is applied in the direction of liposome delivery, etc., can solve the problems of poor stability, low encapsulation rate of main drug, and decreased content.

Inactive Publication Date: 2015-03-11
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Though above-mentioned preparation has significantly improved the solubility of asarone, has reduced toxic and side effects and irritation, has improved bioavailability; Low utilization

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1 asarone liposome freeze-dried powder injection

[0054] prescription:

[0055]

[0056] Preparation Process:

[0057] (1) Dissolve 8g of asarone, 50g of soybean phosphatidylinositol, 30g of cholesterol and 40g of Span-60 in 1000ml of chloroform, and then put it in an eggplant-shaped bottle and rotate it until a uniform film is formed;

[0058] (2) Add 1000ml of phosphate buffer solution with a pH of 6.8 and an appropriate amount of glass beads to the eggplant-shaped bottle and stir for 10 minutes, then stir in a water bath at 30°C for 2 hours to obtain asarone liposomes;

[0059] (3) Add 40g of trehalose to the asarone liposomes prepared above, use a probe to sonicate for 10 minutes, dilute to 2000ml with water for injection, filter through a 0.22um microporous membrane, sub-package, freeze-dry, roll Cap, made 1000 bottles of asarone liposome freeze-dried powder injection.

Embodiment 2

[0060] Embodiment 2 Asarone liposome injection

[0061] prescription:

[0062]

[0063] Preparation Process:

[0064] (1) Dissolve 16g of asarone, 80g of soybean phosphatidylinositol, 40g of cholesterol and 60g of Span-60 in 1500ml of chloroform, and then put it in an eggplant-shaped bottle and rotary evaporate until a uniform film is formed;

[0065] (2) Add 1500ml of phosphate buffer solution with a pH of 6.8 and an appropriate amount of glass beads to the eggplant-shaped bottle and stir for 10 minutes, then stir in a water bath at 30°C for 2 hours to obtain asarone liposomes;

[0066] (3) Add 45g of sodium chloride to the asarone liposomes prepared above, ultrasonicate for 10 minutes with a probe, make the volume to 5000ml with water for injection, filter through a 0.22um microporous membrane, freeze quickly, and then return to room temperature, potting, and sterilization to prepare 1000 Asarone liposome injections.

Embodiment 3

[0067] Embodiment 3 asarone liposome injection

[0068] prescription:

[0069]

[0070] Preparation Process:

[0071] (1) Dissolve 24g of asarone, 60g of soybean phosphatidylinositol, 150g of cholesterol and 100g of Span-60 in 4000ml of chloroform, then place it in an eggplant-shaped bottle and rotate it until a uniform film is formed;

[0072] (2) Add 4000ml of phosphate buffer solution with a pH of 6.8 and an appropriate amount of glass beads to the eggplant-shaped bottle and stir for 10 minutes, then stir in a water bath at 30°C for 2 hours to obtain asarone liposomes;

[0073] (3) Add 90g of sodium chloride to the asarone liposomes prepared above, ultrasonicate with a probe for 10 minutes, dilute to 10000ml with water for injection, filter through a 0.22um microporous membrane, freeze quickly, and then return to room temperature, potting, and sterilization to prepare 1000 Asarone liposome injections.

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PUM

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Abstract

The invention discloses an asarone lipidosome injection and a preparation method thereof. The asarone lipidosome injection with excellent quality is prepared by using asarone, soybean phospholipid phosphatidyl-inositol, cholesterol, span-60, trehalose or sodium chloride according to a specific weight ratio. Compared with the traditional preparation, the asarone lipidosome injection disclosed by the invention has the advantages as follows: the stability and biological availability of the preparation are greatly enhanced, drugs are stably released, the quality of the preparation is improved, toxic and side effects are reduced and a more remarkable curative effect is obtained.

Description

technical field [0001] The invention relates to a new dosage form of asarone, in particular to a liposome injection of asarone and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Asarone, also known as α-asarone, is one of the main components of the volatile oil of the traditional Chinese medicine Shichangpu. Its chemical name is: 2,4,5-trimethyl-1-propenylbenzene, and its molecular formula is: C 12 h 16 o 3 , the molecular weight is 208.26, and the structural formula is: [0003] [0004] Asarone has good cough-relieving, expectorant-relieving, asthma-relieving, sedative, antispasmodic and anti-convulsant effects; it also has varying degrees of inhibitory effects on the growth of Diplococcus pneumoniae, Staphylococcus aureus and Escherichia coli. In the clinical application of pneumonia, asthma and epileptic seizures, it has a relatively ideal effect. [0005] The currently marketed asarone preparations have t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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