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Ancitabine dimyristate acid ester liposome and preparation method thereof

A technology of myristate and cyclocytidine, applied in the field of medicine, can solve the problems of poor water solubility, difficult administration, difficult absorption, etc., and achieves the effects of high encapsulation rate, improved absorption, and improved curative effect.

Inactive Publication Date: 2010-09-08
QINGDAO UNIV
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Problems solved by technology

Since two fatty chains of myristic acid are linked to the pentose ring of cyclocytidine, the molecule of cyclocytidine dimyristate has poor water solubility, which causes difficulty in administration and absorption

Method used

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  • Ancitabine dimyristate acid ester liposome and preparation method thereof
  • Ancitabine dimyristate acid ester liposome and preparation method thereof
  • Ancitabine dimyristate acid ester liposome and preparation method thereof

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Embodiment

[0010] (1) Preparation

[0011] Cyclocytidine dimyristate liposomes were prepared by reverse-phase evaporation. Natural lecithin is separated by alumina column chromatography to obtain pure product, lecithin: cholesterol: distearoyl phosphatidylcholine is placed in a chicken heart bottle according to the molar ratio of 1:1:0.5, and an appropriate amount of chloroform is added to dissolve it . Accurately weigh the required amount of cyclocytidine dimyristate, add it into the same chicken heart bottle to dissolve it, remove chloroform by rotary evaporation under reduced pressure in a nitrogen atmosphere at 45°C, and form a dry film on the inner wall of the chicken heart bottle, diethyl ether and pH A phosphate buffer solution with a value of 7.15 was added in a volume ratio of 3:1 (add ether first to dissolve the lipid film, and then add a phosphate buffer solution), and after 20 minutes of ultrasonic dispersion by an ultrasonic cleaner, the resulting mixture was evaporated in ...

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Abstract

The invention relates to an ancitabine dimyristate acid ester liposome and a preparation method thereof, belonging to the technical field of medicines. The invention overcomes the defects of difficult administration and absorption, caused by the poor water solubility of ancitabine dimyristate acid ester, and improves the treatment effect of the ancitabine dimyristate acid ester. In the invention, the liposome is prepared from 3',5'-ancitabine dimyristate acid ester which is an esterified derivative of ancitabine and auxiliary materials comprising natural adjunct lecithin, cholesterol and a stabilizer which is 2-octadecanoyl phosphatidylcholine by using a reverse phase evaporation method. The prepared liposome is an innovated novel ancitabine derivative slow-release targeting preparation and has the advantages of high encapsulation efficiency of (82.5 + / -3.2)%, even size distribution and high stability. The invention has the advantages of simple preparation process, easily controlled main process parameters and moderate operation condition and is suitable for industrialized production. The invention can be used for treating leukemia, lymphoma and certain solid tumors.

Description

technical field [0001] The invention belongs to the technical field of medicine. Specifically, it is a cyclocytidine dimyristate liposome and a preparation method thereof. Background technique [0002] Cyclocitidine is a commonly used anti-leukemia drug in clinical practice. However, cyclocitidine is easily deaminated by cytosine deaminase in the liver and loses its anticancer activity. In order to maintain an effective blood drug concentration, it is necessary to continuously administer multiple doses to the patient, resulting in myelosuppression and patient emaciation. In order to improve the curative effect of cyclocytidine and overcome its shortcoming of easy deamination and degradation in vivo, the inventors modified the molecular structure of cyclocytidine, and connected two fatty chains of myristic acid to its pentose ring to synthesize 3',5'-Cyclocytidine dimyristate, its molecular structure is shown in the attached figure 1. [0003] Experiments have proved that...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7064A61K47/28A61K47/24A61P35/02
Inventor 王继波石振燕孙衍增张丽
Owner QINGDAO UNIV
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