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Asarone lipidosome injection

A technology of caprylyl and injection, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, freeze-drying delivery, etc., can solve the problems of poor stability, low bioavailability, and low encapsulation rate of main drugs, etc.

Inactive Publication Date: 2013-04-17
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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IPC IPC(8): A61K9/127A61K9/19A61K31/09A61K47/24A61P11/06A61P11/10A61P11/14A61P25/08
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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