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Dioscorea opposita saponin liposome, method for preparing its preparations and uses thereof

A technology of diosgenin and diosgenin is applied to the application of diosgenin liposome preparation in the medicine for preventing and treating cardiovascular diseases, and the preparation field of diosgenin liposome and preparation thereof can solve the problem that phospholipids are prone to hydrolysis and oxidation reaction, Affects diosgenin lipid stability, thermodynamic instability and other issues, and achieves the effects of being beneficial to transportation and storage, good adhesion, and prolonged action time

Active Publication Date: 2008-08-20
江苏黄河药业股份有限公司
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  • Summary
  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since dioscin liposomes belong to a colloidal dispersion system and a thermodynamically unstable system, the phospholipids of its membrane material are prone to hydrolysis and oxidation reactions, and the temperature and pH value of the external environment cause changes in the liposome structure, thereby causing lipid Leakage of drugs in the body, affecting the stability of diosgenin lipids during storage
This is a technical problem that has not been well solved for a long time

Method used

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  • Dioscorea opposita saponin liposome, method for preparing its preparations and uses thereof
  • Dioscorea opposita saponin liposome, method for preparing its preparations and uses thereof
  • Dioscorea opposita saponin liposome, method for preparing its preparations and uses thereof

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Experimental program
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Effect test

Embodiment 1

[0034] Co-dissolve 500mg soybean lecithin, 100mg cholesterol and 11mg vitamin C palmitate in ethanol, and form a film by rotary evaporation in a water bath at 50°C; dissolve 300mg poloxamer in 10ml of PBS buffer at pH 6.0 , and then 100 mg of diosgenin was dissolved in the solution; the prepared solution was added to the above film, vortexed and dispersed to obtain a liposome suspension; finally adding 0.1% bisulfite in the liposome sodium.

[0035] The particle size of the obtained diosgenin liposomes was measured by a Nicomp 380ZLS (Particle Sizing Systems, USA) particle size analyzer between 200-300nm; the product was determined to have an encapsulation efficiency of 60% by ultrafiltration centrifugation.

Embodiment 2

[0037] Co-dissolve 900mg egg yolk lecithin, 90mg cholesterol and 6.3mg vitamin E in ethanol, and form a film by rotary evaporation in a water bath at 30°C; dissolve 100mg poloxamer in 5ml of pH7.3 phosphate buffer 180 mg of diosgenin was dissolved in the buffer solution; then the prepared solution was added to the above film, vortex mixed and homogenized by magnetic stirring for 1 hour to obtain a liposome suspension; weight was added to the liposome The percentage is 0.15% sodium sulfite.

[0038] The particle size of the obtained diosgenin liposome is between 80-200nm; the encapsulation efficiency of the product is determined to be 70% by an ultrafiltration centrifugation method.

Embodiment 3

[0040]A total of 5 mg of soybean lecithin and synthetic phosphatidylserine (weight ratio 20:1), 0.5 mg of cholesterol, and 2.1 mg of vitamin E were dissolved in chloroform, and a film was formed by rotary evaporation in a water bath at 40 ° C; Wen 80 was dissolved in 2 ml of phosphate buffer solution with pH 6.5, and 1 mg of diosgenin 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 a liposome mixture. Suspension; add 0.1% sodium thiosulfate in the liposome by weight.

[0041] The particle size of the obtained diosgenin liposome is between 100-300nm; the encapsulation efficiency of the product is measured to be 80% by an ultrafiltration centrifugation method.

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Abstract

The invention relates to a yam saponin liposome, a preparation method of the yam saponin liposome and the application of yam saponin liposome in preparing the medicine for prevention and treatment of cardiovascular diseases. The composition (parts by weight) of the yam saponin liposome is as follows: phospholipid 1 to 1000, cholesterol 0.5 to 100, yam saponin 1 to 200 and emulsifier 20 to 500. The yam saponin liposome has the advantages of high optical and thermal stability, ability to prolong the active time of the medicine, simple and economical process and convenient transportation and storage compared with the prior art since the yam saponin liposome can be made into coated tablet, syrup, oral liquid, drops and capsules, and obvious therapeutic effect proven by the clinical trial for the cardiovascular diseases such as coronary heart disease and hyperlipidemia.

Description

technical field [0001] The invention relates to the preparation and use of a traditional Chinese medicine liposome and its preparation, in particular to the preparation method of the diosgenin liposome and the preparation thereof, and the application of the dioscin liposome preparation in drugs for preventing and treating cardiovascular diseases. Background technique [0002] Dioscorea saponin is the extract of the rhizome of Dioscorea Nipponica Makino (Dioscorea Nipponica Makino), which has a clear chemical structure and high oral absorption and utilization. Obvious protective effect, relieve angina pectoris; regulate fat, reduce blood viscosity, inhibit platelet aggregation, improve microcirculation, prevent thrombosis; reduce artery wall lipid infiltration and plaque formation, prevent atherosclerosis; reduce heart load, reduce Myocardial oxygen consumption, improve heart function. But at present, the diosgenin raw material drug is unstable to light and heat, and is not ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61P9/00
Inventor 葛海涛张杰陶元明
Owner 江苏黄河药业股份有限公司
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