Preparation method of molecular targeted drug liposome preparation

A technology of liposome preparations and small molecules, which is applied in the field of pharmaceutical preparations to achieve the effects of not easy to degrade, simple production methods, and high stability

Active Publication Date: 2017-05-10
常州金远药业制造有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] In view of the above-mentioned problems, the purpose of the present invention is to provide a method that solves the problems that cannot be solved by conv

Method used

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  • Preparation method of molecular targeted drug liposome preparation
  • Preparation method of molecular targeted drug liposome preparation

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Experimental program
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Embodiment 1

[0022] Embodiment 1: a kind of preparation method of liposome preparation of small molecule targeting drug, described preparation method comprises the following steps:

[0023] 1) Dissolve 1.8 parts by weight of EPC, 0.2 parts by weight of DSPG and 0.65 parts by weight of cholesterol with 12 parts by weight of absolute ethanol, dissolve 4.5 parts by weight of ammonium sulfate with 100 parts by weight of water, and dissolve the The two solutions are mixed, kept warm and hydrated, and after hydration, the particle size of the blank liposome is not more than 150nm by extrusion or homogenization;

[0024] 2) Dialyze the blank liposome solution obtained in step 1 to remove ammonium sulfate ions outside the liposome, then add 357.5 parts by weight of water to dilute, adjust the pH to 3.8 after dilution, and heat for later use;

[0025] 3 Weighing 0.095 parts by weight of tinib drug CU201 and dissolving it in dimethyl sulfoxide DMSO solution, controlling the particle diameter in the ...

Embodiment 2

[0028] Embodiment 2: a kind of preparation method of small molecule targeting drug liposome preparation, described preparation method comprises the following steps:

[0029] 1) Dissolve 2.2 parts by weight of EPC, 0.25 parts by weight of DSPG and 0.70 parts by weight of cholesterol with 16 parts by weight of absolute ethanol, dissolve 5.0 parts by weight of ammonium sulfate with 100 parts by weight of water, and dissolve the The two solutions are mixed, kept warm and hydrated, and after hydration, the particle size of the blank liposome is not more than 150nm by extrusion or homogenization;

[0030] 2) Dialyzing the blank liposome solution obtained in step 1 to remove ammonium sulfate ions outside the liposome, then adding 397.3 parts by weight of water for dilution, adjusting the pH to 4.2 after dilution, and heating for later use;

[0031] 3) Weigh 0.261 parts by weight of tinib drug CU201 and dissolve it in dimethyl sulfoxide DMSO solution, and control the particle diameter...

Embodiment 3

[0034] Embodiment 3: a kind of preparation method of liposome preparation of small molecule targeting drug, described preparation method comprises the following steps:

[0035] 1) Dissolve 2.0 parts by weight of EPC, 0.21 parts by weight of DSPG and 0.67 parts by weight of cholesterol with 14 parts by weight of absolute ethanol, and dissolve 4.625 parts by weight of ammonium sulfate with 100 parts by weight of water. The two solutions are mixed, kept warm and hydrated, and after hydration, the particle size of the blank liposome is not more than 150nm by extrusion or homogenization;

[0036] 2) Dialyze the blank liposome solution obtained in step 1 to remove ammonium sulfate ions outside the liposome, then add 378.5 parts by weight of water to dilute, adjust the pH to 4.0 after dilution, and heat for later use;

[0037] 3) Weigh 0.15 parts by weight of tinib drug CU201 and dissolve it in dimethyl sulfoxide DMSO solution, and control the particle diameter in the solution to not...

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Abstract

The invention discloses a preparation method of a molecular targeted drug liposome preparation. The preparation method comprises the operating steps of blank liposome preparation, liposome preprocessing, drug preprocessing, preparation production and postprocessing, the production processes of the steps are optimized, and finally the problem that the product obtained by adopting a conventional production method is turbid and the drug encapsulation efficiency is low is solved. According to the technical scheme, the encapsulation efficiency can be improved by 95% or above, a solution is clear and transparent, and gefitinib drugs are not easy to degrade in the preparation process. The production method is simple and easy to operate and facilitates production expanding, and the finally obtained product is high in stability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparation technology, in particular to a preparation method of a small molecule compound small molecule targeting drug liposome preparation of a signal transduction pathway target in tumor cells. Background technique [0002] At present, the focus of anti-tumor drug research and development is shifting from traditional cytotoxic drugs to new anti-tumor drugs targeting intratumor signal transduction pathways. Tyrosine protein kinase is mainly related to the conduction of signal pathways and is the center of cell signal transduction mechanism. Its overexpression can induce a variety of tumors. Tyrosine protein kinase inhibitors are a new class of anti-tumor drugs developed in the past ten years. [0003] A tinib drug CU201 is not yet on the market, and its structural formula is as follows (referring to the compound structural formula): [0004] [0005] CAS Registry Number: 1012885-89-0; [000...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/506A61K47/28A61P35/00
CPCA61K47/28A61K9/127A61K9/1277A61K31/506
Inventor 马堰启周钢符俊张晓瑶岳秀芳
Owner 常州金远药业制造有限公司
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