Preparing method of taxanes substance preparation with nanostructure

A nanostructure and paclitaxel technology, which is applied in the directions of medical preparations, drug combinations, and pharmaceutical formulations containing active ingredients, can solve the problems of hemolysis and easy precipitation of paclitaxel.

Inactive Publication Date: 2010-03-17
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Prepare cyclodextrin compounded paclitaxel preparations, although it is widely used, paclitaxel is easy to precipitate at low concentrations, and may cause hemolysis at high concentrations

Method used

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  • Preparing method of taxanes substance preparation with nanostructure
  • Preparing method of taxanes substance preparation with nanostructure
  • Preparing method of taxanes substance preparation with nanostructure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Dissolve 0.25g of dextran-65 and 0.25g of poloxamer-188 in 25ml of deionized water, adjust the pH=3.0, adjust the speed to 800rpm, and dropwise add 0.25g of α-cyanide at -5°C A mixed solution of n-butyl acrylate, 0.015g of natural paclitaxel and 5ml of ethanol was stirred at room temperature for 6 hours, adjusted to pH 7, and separated with a 0.45μm membrane to obtain a nanostructured natural paclitaxel preparation. The test results are shown in figure 1 , 4 , 7.

[0030] From figure 1 It can be seen that the preparation in this example is a solid nano particle, and the particle is complete, from Figure 4 It can be seen that the average particle size is 302nm, Figure 7 It shows that the content of natural paclitaxel in this preparation is lower compared with other examples.

Embodiment 2

[0031] Example 2: Dissolve 0.5g of dextran-65 in 25ml of deionized water, stir well to dissolve. Adjust the pH to 2.9, adjust the speed to 800rpm, add 0.25g n-butyl α-cyanoacrylate dropwise at room temperature 20°C, react for 6 hours, adjust the pH to 7, separate with a 0.45μm membrane, then add 0.015g natural paclitaxel, 5ml ethanol , and reacted for 4 hours to obtain a nanostructured natural paclitaxel preparation, the test results are shown in figure 2 , 5 ,8.

[0032] From figure 2 It can be seen that the preparation is a nano hollow particle, from Figure 5 Obtain its average particle diameter to be 231nm, by Figure 8 It can be seen that the natural paclitaxel content of this preparation is the highest compared to other examples.

Embodiment 3

[0033]Example 3: Dissolve 0.5g of Dextran-65 and 0.25g of Poloxamer-188 in 50ml of deionized water, adjust the pH to 3.0, adjust the speed to 800rpm, and add 0.25g of α-cyano group dropwise at room temperature 28°C n-butyl acrylate, reacted for 6 hours, adjusted the pH to 7, separated with a 0.45 μm membrane, then added 0.010 g of natural paclitaxel and 5 ml of ethanol, and reacted for 4 hours to obtain a nanostructured natural paclitaxel preparation. See the test results image 3 , 6 , 9, the test results show that its encapsulation rate is 98.16%.

[0034] From image 3 It can be seen that the preparation is also a hollow nano particle, and the particle is uniform and complete, and the plane is closely arranged. Figure 6 It can be seen that the average particle diameter of the preparation is 234nm, by Figure 9 It can be seen that the natural paclitaxel content of this preparation is moderate compared to other examples.

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Abstract

The invention discloses a preparing method of taxanes substance preparation with nanostructure. Taxanes substance is dissolved in organic solvent and then dispersed in alpha-PBCA, and taxanes substance is highly-dispersed aqueous emulsion under the action of other auxiliary agents to form taxanes substance preparation with nanostructure. The taxanes substance preparation with nanostructure has stable performance and particle size distribution of 50-500nm, is round without adhesion, has the slow release function, can biologically degrade and has no toxic and side effect. The invention has simple technology, environment-friendly preparing process and easy industrialization.

Description

Technical field: [0001] The invention relates to a preparation method of an anticancer drug preparation, in particular to a preparation method of a paclitaxel substance preparation with a nanostructure. Background technique: [0002] Paclitaxel substances mainly include natural paclitaxel (referred to as paclitaxel), docetaxel, paclitaxel prodrugs and various compounds modified based on the structure of paclitaxel. Paclitaxel is a diterpenoid compound extracted from Taxus chinensis, which was officially approved by the FDA in 1992 as an anticancer drug. Its main mechanism of action is that paclitaxel acts as a microtubule stabilizer, acts on the M phase of mitosis, and inhibits normal mitosis of cells by inhibiting microtubule depolymerization. It has been clinically proven that paclitaxel has a good curative effect on various cancers such as breast cancer and ovarian cancer. However, due to its extremely poor water solubility (0.25 μg / ml), the current clinical paclitaxel ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61P35/00
Inventor 孙汉雄孙国明周长江李吟之
Owner SHANGHAI JIAO TONG UNIV
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