Preparation of Sorafenib Nanomedicine Based on Small Molecular Chaperones

A sorafenib nanometer and nanomedicine technology, which is applied in the field of preparation of sorafenib nanometer medicine, can solve the problems of high production cost, complicated preparation process and poor reproducibility

Active Publication Date: 2020-10-23
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above methods all involve the use of a large number of excipients, low drug loading, complex preparation process, poor reproducibility, and high production cost.

Method used

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  • Preparation of Sorafenib Nanomedicine Based on Small Molecular Chaperones
  • Preparation of Sorafenib Nanomedicine Based on Small Molecular Chaperones
  • Preparation of Sorafenib Nanomedicine Based on Small Molecular Chaperones

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Preparation of Sorafenib Nanomedicine Based on Small Molecular Chaperone 6

[0049]

[0050] Dissolve sorafenib and small molecule chaperone 6 (molar ratio 1:1) in DMF (sorafenib 25mg / ml), and add 40ul DMF solution to 1000ul water for injection at room temperature with a dropping rate of 1mL / min, vortex stirring at high speed (2000r / min), and remove the organic solvent after dialysis to obtain sorafenib nanomedicine. Analysis and determination by transmission electron microscopy (TEM) and dynamic light scattering particle size analyzer (DLS). It is found that the nanoparticles formed by sorafenib under the action of 6 are 80-100nm, with round shape and good dispersion. figure 1 As shown, the dispersion coefficient PDI is 0.1~0.2, and the potential is -30~-40mV, such as figure 2 Shown.

Embodiment 2-7

[0052] According to the method in Example 1 and the same conditions as in Example 1, sorafenib nanomedicines with different small molecular chaperones were prepared respectively, and the results are shown in Table 1.

[0053] Table 1

[0054]

[0055]

Embodiment 8-11

[0057] Taking small molecular chaperone 6 as an example, in this example, a sorafenib nanomedicine based on small molecular chaperone 6 was prepared according to the method of Example 1, and different molar ratios of sorafenib and small molecular chaperone were prepared. The effects of sorafenib nano-drugs are shown in Table 2.

[0058] Table 2

[0059]

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PUM

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Abstract

The invention provides a preparation method of Sorafenib nanometer medicines based on a micromolecule partner. The method based on the micromolecule partner comprises the following steps of mixing themicromolecule partner with Sorafenib, and preparing the Sorafenib nanometer medicines by a nanometer precipitation method, wherein the micromolecule partner is amphipathic fat acid or salts. The preparation method is simple, extra-high in the medicine carrying quantity, good in repeatability, environment-friendly, and suitable for industrial mass production. The obtained Sorafenib nanometer medicines are good in solubility, and high in stability.

Description

Technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of sorafenib nano-medicine based on small molecular chaperones. Background technique [0002] Sorafenib is a new type of multi-target anti-tumor drug, which can simultaneously inhibit multiple kinases and exert multiple anti-tumor effects. Sorafenib has poor solubility and strong hydrophobicity. In order to improve its solubility in water, it is clinically made into tosylate. The commercial preparation of sorafenib is The generic name is sorafenib tosylate tablets, the English product name is However, its water solubility is still poor, its oral bioavailability is low, its clinical application dose is large, and its obvious side effects (including hypertension, hand-foot skin reactions and gastrointestinal reactions including gastric bleeding) restrict its clinical application. [0003] The currently reported sorafenib delivery systems mainly ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/69A61K31/44A61P35/00
Inventor 张娜韩雷强刘永军
Owner SHANDONG UNIV
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