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Preparation methods of methotrexate and lecithin compound, nano-particles of methotrexate and lecithin compound as well as targeted sustained release preparation of methotrexate and lecithin compound

A technology of methotrexate phospholipid and aminopterate phospholipid, which is applied in the direction of anti-inflammatory agents, drug combinations, pharmaceutical formulations, etc., can solve the problems of high cost, long cycle for new drug application, complicated preparation process, etc., and achieve good stability, Low toxicity therapeutic effect, good tumor targeting and sustained release properties

Inactive Publication Date: 2015-11-18
XIAMEN CHITOSAN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The MTX in the above two related patents is a polymer compound prepared by chemical bonding with the carrier material. The preparation process is complicated and the cost is high. The cycle of new drugs is also very long

Method used

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  • Preparation methods of methotrexate and lecithin compound, nano-particles of methotrexate and lecithin compound as well as targeted sustained release preparation of methotrexate and lecithin compound
  • Preparation methods of methotrexate and lecithin compound, nano-particles of methotrexate and lecithin compound as well as targeted sustained release preparation of methotrexate and lecithin compound
  • Preparation methods of methotrexate and lecithin compound, nano-particles of methotrexate and lecithin compound as well as targeted sustained release preparation of methotrexate and lecithin compound

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Embodiment 1

[0047] In the preparation method of the methotrexate phospholipid complex in this embodiment, methotrexate and lecithin are dissolved in the organic solvent A, and the mixing reaction is carried out at 20° C. The mixing reaction time is 12 hours. The organic solvent A in the resulting mixed solution is removed by vacuum rotary evaporation, and then the dried product after removing the organic solvent A is purified and further dried by using organic solvent B to obtain the methotrexate phospholipid complex, the organic solvent A It is one or more of tetrahydrofuran, dimethylformamide and acetone, and the organic solvent B is one or two mixtures of dichloromethane and chloroform. The mixing reaction is carried out in a water bath mode. The obtained methotrexate phospholipid complex was sequentially purified and dried. The molar ratio of methotrexate to lecithin is 1:1. The lecithin is egg yolk lecithin or soybean lecithin.

[0048] In the method for preparing methotrexate pho...

Embodiment 2

[0051] In the preparation method of the methotrexate phospholipid complex in this embodiment, methotrexate and lecithin are dissolved in the organic solvent A, and the mixing reaction is carried out at 40° C. The mixing reaction time is 12 hours. The organic solvent A in the mixed solution is removed by vacuum rotary evaporation, and then the dried product after removing the organic solvent A is purified and further dried by using the organic solvent B to obtain the methotrexate phospholipid complex, the organic solvent A is one or more of tetrahydrofuran, dimethylformamide and acetone, and the organic solvent B is one or more of chloroform and dichloromethane. The mixing reaction is carried out in a water bath mode. The obtained methotrexate phospholipid complex was sequentially purified and dried. The molar ratio of methotrexate to lecithin is 1:4. The lecithin is egg yolk lecithin or soybean lecithin.

[0052] In the method for preparing methotrexate phospholipid complex...

Embodiment 3

[0055] In the preparation method of the methotrexate phospholipid complex in this embodiment, methotrexate and lecithin are dissolved in the organic solvent A, and the mixing reaction is carried out at 30° C. The mixing reaction time is 24 hours. The organic solvent A in the resulting mixed solution is removed by vacuum rotary evaporation, and then the dried product after removing the organic solvent A is purified and dried by using organic solvent B to obtain the methotrexate phospholipid complex, the organic solvent A It is one or more of tetrahydrofuran, dimethylformamide and acetone, and the organic solvent B is one or more of chloroform and dichloromethane. The mixing reaction is carried out in a water bath mode. The obtained methotrexate phospholipid complex was sequentially purified and dried. The molar ratio of methotrexate to lecithin is 1:2. The lecithin is egg yolk lecithin or soybean lecithin.

[0056] In the method for preparing methotrexate phospholipid comple...

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Abstract

The invention relates to a preparation method of a methotrexate and lecithin compound, which comprises the following steps: dissolving methotrexate and lecithin in an organic solvent A, carrying out mixed reaction at 20-40 DEG C for 12-24h, removing the organic solvent A in the mixed liquor after mixed reaction to obtain a dried product, and then purifying the dried product in which the organic solvent A is removed by adopting an organic solvent B, so as to obtain the methotrexate and lecithin compound. The invention also relates to a preparation method of nano-particles of the methotrexate and lecithin compound as well as a preparation method of a targeted sustained release preparation of the methotrexate and lecithin compound. The nano-particles of the methotrexate and lecithin compound, prepared by the method provided by the invention, have particle sizes of 100-500nm, good stability and better tumor targeting and sustained release characteristics. The targeted sustained release preparation of the methotrexate and lecithin compound, prepared by the method provided by the invention, has the advantages of targeting property, long circulation, low toxicity and good curative effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical antitumor drug preparations and antirheumatic drugs, in particular to a preparation method of a methotrexate phospholipid complex, its nanoparticle and its targeted sustained-release preparation. Background technique [0002] Methotrexate (MTX) is a folate antimetabolite that can bind to folate receptors on the surface of tumor cells and play a good targeting role. It is often used in the treatment of various malignant tumors and is also a commonly used antirheumatic drug. , MTX also has many disadvantages in medicinal use. When treating brain tumors, a small amount can pass through the blood-brain barrier. This product can increase the toxicity of liver and kidney function. Because the mechanism of action of the drug is through the inhibition of dihydrofolate reductase. It can hinder the synthesis of tumor cell DNA, so it also has a drug effect on normal biological cells, and the toxicity is relativ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/19A61K47/24A61K31/519A61P35/00A61P29/00
Inventor 侯振清李岩秀蔺金燕侯鲁
Owner XIAMEN CHITOSAN BIO TECH
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