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Matrine elaioplast drop ball and its preparation

A technology of ginseng fat and matrine, applied in the field of matrine preparations and preparation thereof, can solve the problems of poor stability of injections, affecting the application of drug carriers, restricting the use of stability, and the like, and solve the problem of instability , Complete absorption, solve the targeted effect

Inactive Publication Date: 2007-01-17
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the commonly used dosage form of matrine is injection. Considering that the method of injection administration is complicated, it is necessary to go to the hospital for medication, which is not very convenient for patients. At the same time, injections generally have the problem of poor stability.
Preparation of matrine into liposomes can achieve targeted drug delivery. However, traditional liposomes composed of lecithin and cholesterol are thermodynamically unstable systems, and their weak stability in vivo and in vitro limits their use. Great influence on its application as a drug carrier

Method used

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  • Matrine elaioplast drop ball and its preparation
  • Matrine elaioplast drop ball and its preparation
  • Matrine elaioplast drop ball and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] One, preparation of matrine liposomes with ether injection method

[0029] (1) prepare matrine liposome

[0030] Prepare 1% matrine solution with pH 6.8 phosphate buffer solution as solvent, take 120ml in a conical flask, dissolve 1.2g of soybean lecithin and 0.6mg of cholesterol in 60ml of ether. Slowly inject the ether solution into the matrine solution with a No. 5 needle (the needle tip is under the liquid surface) under electromagnetic stirring, stir evenly, heat to 65°C, remove the ether by volatilization, and obtain matrine liposomes.

[0031] The prepared liposome is added with a cryoprotectant and placed in a lyophilizer to freeze-dry to form a white powdery substance, which can be hydrated by adding water before use.

[0032] (2) Determination of Encapsulation Efficiency

[0033] ① Separation conditions

[0034] Separation voltage: 20KV, detection wavelength: 196-400 full-wavelength scanning; measurement wavelength: 206nm Sampling method: pressure injection...

Embodiment 2

[0069] One, reverse evaporation method prepares matrine liposome

[0070] Take 1.2g of soybean lecithin and 0.6g of cholesterol, dissolve them in 200ml of ether, and place them in a conical flask. Prepare 1% matrine solution with pH 7.4 phosphate buffer solution, under electromagnetic stirring, slowly drop 120ml of 1% matrine solution into the Erlenmeyer flask, stir to form an emulsion with ether, decompress Ether was distilled off for 1 h to obtain matrine liposomes.

[0071] Two, preparation of matrine liposome dripping pills

[0072] Weigh 10g of polyethylene glycol (6000) and 5g of polyethylene glycol (4000) into a beaker, heat and melt on a water bath at 90°C, add 3g of matrine liposome, stir evenly, and keep warm for later use. Preheat the dropping pill machine to keep the temperature of the liquid storage chamber at 90±1°C, use soybean oil as the coolant, pre-cool to 5°C, adjust the distance between the drip nozzle and the cooling liquid surface, pour the liquid medic...

Embodiment 3

[0074] One, film method prepares matrine liposome

[0075] Soybean lecithin 1.2g, cholesterol 0.6g, dissolve in 200ml ether, remove the organic solvent under reduced pressure with a rotary evaporator, form a uniform phospholipid film in a pear-shaped bottle, add 120ml of matrine 1% pH7.4 Phosphate buffer solution, soaking, stirring and eluting the lipid film to obtain matrine liposomes.

[0076] Two, preparation of matrine liposome dripping pills

[0077] Weigh 10 g of glycerin and 6 g of poloxamer into a beaker, heat and melt on a water bath at 88° C., add 3 g of matrine liposomes, stir evenly, and keep warm for later use. Preheat the dropping pill machine to keep the temperature of the liquid storage chamber at 88±1°C, use liquid paraffin as the coolant, pre-cool to 5°C, adjust the distance between the drip nozzle and the cooling liquid surface, pour the liquid medicine into the liquid storage chamber, and start the valve , be 60 drop / min drop system with dropping speed, c...

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Abstract

A dripping pill of matrine liposome with high stability and disintegrating speed is prepared from the matrine liposome prepared from matrine, soybean lecithin and cholesterol, and water-soluble matrix through proportional mixing, and dripping in cooling liquid.

Description

technical field [0001] The invention relates to a matrine preparation and a preparation method thereof. Background technique [0002] Matrine (MAT) is derived from Sophora flavescens Ait, S.alopecuroides L. and S.subprostrata Chun et T.Chen of the leguminous plant Sophora flavescens Ait. It has various pharmacological effects and clinical functions. Such as anti-tumor, anti-bacterial, anti-parasitic, anti-viral, anti-arrhythmia, swelling and diuretic, anti-allergic and alleviating leukopenia caused by cyclophosphamide. The anti-cancer mechanism of matrine shows that matrine not only has a direct killing effect on tumor cells, but also induces some tumor cells to differentiate into normal cells and promote apoptosis. In addition, while matrine is anti-tumor, it does not have a destructive effect on normal cells, and it can also increase white blood cells and improve the immune function of the body. [0003] As a new dosage form, liposome has many unique characteristics in t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/127A61K47/28A61K31/4375A61K36/489A61P7/10A61P9/06A61P31/04A61P31/12A61P33/00A61P35/00
Inventor 刘小平王静王莹秦磊周园沈亮
Owner WUHAN UNIV OF TECH