Tamoxifen citrate liposome and preparation method thereof

A technology of tamoxifen and citric acid, which is applied in the field of medicine, can solve the problems of failing to reduce toxic and side effects, achieve the effects of improving solubility and bioavailability, reducing drug toxicity, and prolonging drug action time

Active Publication Date: 2019-07-23
北京斯利安药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the existing dosage forms of tamoxifen citrate are difficult to solve the problems of its dissolution rate and bioavailability, and fail to reduce its toxic and side effects

Method used

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  • Tamoxifen citrate liposome and preparation method thereof
  • Tamoxifen citrate liposome and preparation method thereof
  • Tamoxifen citrate liposome and preparation method thereof

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preparation example Construction

[0025] The invention provides a kind of preparation method of tamoxifen citrate liposome, comprising:

[0026] Tamoxifen citrate, phospholipids and cholesterol are dissolved in a solvent, and a liposome film is prepared by gradient vacuum evaporation; the gradient vacuum evaporation is specifically:

[0027] -0.01~-0.02Mpa rotary evaporation for 20~40min; -0.04~-0.05Mpa rotary evaporation for 20~30min; -0.06~-0.07Mpa rotary evaporation for 10~20min; -0.08~-0.1Mpa rotary evaporation for 3~5min;

[0028] The liposome film is hydrated and filtered to obtain tamoxifen citrate liposome.

[0029] The preparation method of the tamoxifen citrate liposome provided by the invention first dissolves tamoxifen citrate, phospholipid and cholesterol in a solvent.

[0030] According to the present invention, the phospholipid is preferably soybean lecithin.

[0031] The present invention does not limit the sources of tamoxifen citrate, phospholipids and cholesterol, which can be purchased co...

Embodiment 1

[0071] A tamoxifen citrate liposome.

[0072] Recipe: Formula No. 1 is used.

[0073] Preparation:

[0074] (1) Weigh soybean lecithin, cholesterol and tamoxifen citrate according to the formula dosage and add them to an eggplant-shaped bottle, add a mixture of methylene chloride and methanol with a volume ratio of 2:1, soybean lecithin and the added dichloromethane The ratio of the methyl chloride-methanol mixture is 8mg:6ml. After ultrasonic dissolution, the organic solvent is removed by gradient vacuum evaporation. The gradient vacuum evaporation process is as follows: -0.01Mpa for 30min; -0.04Mpa for 30min; -0.06Mpa for 20min; -0.1Mpa for 3min. The temperature of the evaporation process is 39°C, and the rotation speed is 85 / min. After the evaporation is complete, blow nitrogen gas for about 5-10 minutes to remove the residual organic solvent. A lipid film is obtained.

[0075] (2) Add ultrapure water with a ratio of 1ml to 4mg of soybean lecithin to 68°C, slowly add t...

Embodiment 2

[0078] A tamoxifen citrate liposome.

[0079] Formula: No. 2 formula is adopted.

[0080] Preparation:

[0081] (1) Weigh soybean lecithin, cholesterol and tamoxifen citrate according to the formula dosage and add them to an eggplant-shaped bottle, add a mixture of methylene chloride and methanol with a volume ratio of 1.8:1, soybean lecithin and the added dichloromethane The ratio of methyl chloride to methanol mixture is 8mg:8ml. After ultrasonic dissolution, the organic solvent is removed by gradient vacuum evaporation. The gradient vacuum evaporation process is as follows: -0.02Mpa for 40min; -0.05Mpa for 25min; -0.065Mpa for 15min; -0.09Mpa for 4min. The temperature of the evaporation process is 40°C, and the rotation speed is 88r / min. After the evaporation is complete, blow nitrogen gas for about 5-10 minutes to remove the residual organic solvent. A lipid film is obtained.

[0082] (2) Add ultrapure water with a ratio of 1ml to 6mg of soybean lecithin to 65°C, slow...

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Abstract

The invention provides a preparation method of a tamoxifen citrate liposome. The preparation method comprises the steps of enabling tamoxifen citrate, phospholipid and cholesterol to dissolve in a solvent, and performing treatment by a gradient vacuum evaporation method to obtain a liposome film; and performing hydration on the liposome film, and performing filtration so as to obtain the tamoxifencitrate liposome. According to the preparation method, tamoxifen citrate is wrapped with phospholipid and cholesterol mediums to obtain the tamoxifen citrate liposome, so that the toxicity of medicines can be notably reduced, the solubility and the biological availability of the medicines can be improved, and the medicine action time can be prolonged; and besides, the tamoxifen citrate liposome which is obtained by a method for preparing the liposome film through gradient vacuum evaporation of the solvent is better in filming properties, moderate (150-200nm) and uniform in particle diameter,higher in entrapment efficiency (80% or above) and better in stability.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a tamoxifen citrate liposome and a preparation method thereof. Background technique [0002] Tamoxifen citrate is a non-steroidal anti-estrogen drug, its structure is similar to estrogen, and there are two isomers, Z-type and E-type. Among them, the Z-type isomer enters breast cancer cells, can compete with estrogen receptor (ER), forms a receptor complex, prevents the function of estrogen, and thus inhibits the proliferation of breast cancer cells, so it is widely used in breast cancer cells. Treatment of various types of breast cancer, especially suitable for postmenopausal women with breast cancer who are positive for estrogen receptors and progesterone receptors and have low levels of prostate specific antigen. [0003] Tamoxifen citrate is a fat-soluble drug, almost insoluble in water, so its bioavailability is low. Tamoxifen citrate has certain toxic and side effects, wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/138A61K47/28A61K47/24A61P35/00
CPCA61K9/127A61K9/1277A61K31/138A61K47/24A61K47/28
Inventor 张海朝易斌王曙宾罗丽莲肖艳皎蔡正军马克阳
Owner 北京斯利安药业有限公司
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