Arenobufagin nanoliposome and preparation method thereof

Inactive Publication Date: 2007-04-25
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug liposomes made by various methods generally have low encapsulation efficiency, particle size does not meet the requirements of NDDS or uneven distribution; and the commonly used liposomes are all in liquid state, which are stable in liquid state Poor performance, there are many problems, such as leakage of drugs, focusing of particles, oxidation and hydrolysis of phospholipids in liquid state, etc., which also affect the industrial production of liposomes, and even affect the clinical application of liposomes. application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Dissolve 0.1g of soybean lecithin and 0.05g of cholesterol in ethanol, and form a film by rotary evaporation in a water bath at 50°C; dissolve 0.3g of poloxamer 188 in 100ml of PBS buffer at pH 6.0, and then extract 0.01 g was dissolved in the solution; the prepared solution was added to the above membrane, and vortexed to obtain 100 ml of liposome suspension.

[0029] Gained toad venom nano liposomes are measured by the above method, and the average particle diameter is recorded between 10-20nm, the encapsulation efficiency is 80%, the release amount is 35% in 0.5 hours, and the leakage rate is 2% in 36 hours. The oxidation index was 0.01.

Embodiment 2

[0031] Dissolve 1g of soybean lecithin and 0.1g of cholesterol in diethyl ether, and form a film by rotary evaporation in a water bath at 30°C; g was dissolved in the buffer solution; then the prepared solution was added to the above-mentioned membrane, vortex mixed and homogenized by magnetic stirring for 0.5 hour to obtain 100 ml of liposome suspension.

[0032] Gained toad venom nano-liposomes are measured by the above method, and the average particle diameter is recorded between 20-30nm, the encapsulation efficiency is 95%, the release amount is 27% in 0.5 hours, and the leakage rate is 0.3% in 36 hours. The oxidation index was 0.03.

Embodiment 3

[0034] Dissolve 1.5g of soybean lecithin and 0.3g of cholesterol in chloroform, and form a film by rotary evaporation in a water bath at 40°C; dissolve 1.5g of poloxamer 188 in 90ml of phosphate buffer with pH 6.5, and then extract toad venom 0.1 g of the liposome was dissolved in the above solution; the prepared solution was added to the above film, oscillated to disperse and then stirred and homogenized for 1 hour to obtain 100 ml of liposome suspension.

[0035] Gained toad venom nano-liposomes are measured by the above method, and the average particle diameter is recorded between 20-40nm, the encapsulation efficiency is 94%, the release amount is 28% in 0.5 hours, and the leakage rate is 0.3% in 36 hours. The oxidation index was 0.08.

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PUM

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Abstract

The invention discloses a secretio bufonis nano liposome which comprises the following constituents (by weight portions): 0.01-1 part of toad venoms extract, 0.1-20 of phospholipids, 0.05-10 parts of cholesterin, and 0.1-10 parts of emulsifying agent. The invention also discloses the process for preparation through film membrane dispersion method. The secretio bufonis nano liposome has a grain size between 10-100nm and the advantages of high medicinal encapsulation efficiency, low medicinal percolation ratio and oxidation index, and better constancy.

Description

technical field [0001] The invention relates to a nano-liposome and a preparation method thereof, in particular to a toad venom nano-liposome and a preparation method thereof. Background technique [0002] The active ingredients of the traditional Chinese medicine Bufonis Bufonis (classified name Venenum Bufonis) mainly include bufonisin, cinobufonitoxin base, bufonisin and other fat-soluble ingredients. The existing Chansu injection is an aqueous preparation of Chansu extract, which has the functions of anti-tumor, anti-virus, and improving immune function. It has been widely used clinically in patients with middle and advanced tumors and chronic hepatitis B. However, in the course of clinical application, vascular irritating adverse reactions such as poor intravenous infusion, redness and swelling at the infusion site, and intravenous pain often occur; and fat-soluble drugs often have disadvantages such as low bioavailability and unstable absorption after administration. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K35/56A61K9/127A61P35/00A61P31/12A61P37/04A61K35/65
Inventor 奉建芳杨勇芦洁
Owner SHANGHAI INST OF PHARMA IND CO LTD
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