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A kind of cabazitaxel protein nano-injection and preparation method thereof

A nano-injection, cabazitaxel technology, applied in the field of pharmaceutical preparations, can solve the problems of long time, large dosage, large toxic and side effects, hypersensitivity reactions, etc.

Active Publication Date: 2021-09-07
深圳市健开医药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the embodiments of the present invention is to provide a protein nano-injection of cabazitaxel, which aims to solve the problem of the existing cabazitaxel injection, which has large toxic and side effects, is prone to cause severe hypersensitivity reactions, and has a large dosage and a long time, and The stability is relatively poor, and there is a problem of potential safety hazards in medication

Method used

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  • A kind of cabazitaxel protein nano-injection and preparation method thereof
  • A kind of cabazitaxel protein nano-injection and preparation method thereof
  • A kind of cabazitaxel protein nano-injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Cabazitaxel protein nano-injection, including the following raw materials:

[0038] Cabazitaxel 100mg; Cholesterol 150mg; Bovine serum albumin 1.5g (1.5% concentration); Sodium octanoate 12mg.

[0039] making process:

[0040]Dissolve cabazitaxel and cholesterol in an organic solvent (chloroform: absolute ethanol = 11:1, 10ml in total), and use it as an oil phase for later use; dissolve bovine serum albumin in ultrapure water, adjust the pH to 10, Standby as the water phase; add the oil phase to the water phase, and perform ultrasonication in an ice bath at 30% power for 12 minutes to form a primary emulsion; pass the primary emulsion through a high-pressure homogenizer at a pressure of 800 bar, and circulate it 8 times The treated emulsion is subjected to 35°C decompression rotary steaming process to remove the organic solvent, centrifuged at 22000r / min (34700×g) for 30min at 4°C, removes the supernatant, and adds an appropriate amount of ultrapure water to the precip...

Embodiment 2

[0042] Cabazitaxel protein nano-injection, including the following raw materials:

[0043] Cabazitaxel 150mg; Cholesterol 200mg; Bovine serum albumin 1.5g (1.5% concentration); Sodium caprylate 12mg.

[0044] making process:

[0045] Dissolve cabazitaxel and cholesterol in an organic solvent (chloroform: absolute ethanol = 11:1, 10ml in total), and use it as an oil phase for later use; dissolve bovine serum albumin in ultrapure water, adjust the pH to 8, Standby as the water phase; add the oil phase into the water phase, and perform ultrasonication in an ice bath at 40% power for 8 minutes to form a primary emulsion; pass the primary emulsion through a high-pressure homogenizer under the condition of a pressure of 500 bar, and circulate 8 times ; The processed emulsion was subjected to vacuum rotary evaporation at 35°C to remove the organic solvent, centrifuged at 22,000 r / min (34,700×g) and 4°C for 30 minutes, removed the supernatant, and reconstituted the precipitate with a...

Embodiment 3

[0047] Cabazitaxel protein nano-injection, including the following raw materials:

[0048] Cabazitaxel 100mg; Cholesterol 100mg; Human serum albumin 2.0g (2% concentration); Sodium caprylate 16mg.

[0049] making process:

[0050] Dissolve cabazitaxel and cholesterol in an organic solvent (chloroform: absolute ethanol = 11:1, 10ml in total), and use it as an oil phase for later use; dissolve human serum albumin in ultrapure water, adjust the pH to 8, Standby as the water phase; add the oil phase into the water phase, and perform ultrasonication in an ice bath at 40% power for 3 minutes to form a primary emulsion; continue stirring the primary emulsion at room temperature for 2 hours; Press and spin steam to remove the organic solvent, centrifuge at 22000r / min (34700×g) for 30min at 4°C, remove the supernatant, and redissolve the precipitate with an appropriate amount of ultrapure water to obtain the cabazitaxel protein nanomaterial; the cabazitaxel Sai protein nanomaterials ...

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Abstract

The present invention is applicable to the technical field of pharmaceutical preparations, and provides a cabazitaxel protein nano-injection and a preparation method thereof. The cabazitaxel protein nano-injection comprises the following raw materials in parts by weight: 50-150 parts of cabazitaxel; protein carrier 400-4000 parts of materials; 50-300 parts of protein nano-modified materials; 12-100 parts of freeze-drying protective agent. In the present invention, cabazitaxel is encapsulated in a spherical or ellipsoidal nanometer composed of a protein carrier material and a protein nano-modified material or attached to the surface of the nanometer, and subjected to freeze-drying treatment with a freeze-drying protective agent to obtain the cabazitaxel protein nanometer. The injection has a good sustained-release effect and a high anti-tumor effect, which effectively avoids the hypersensitivity caused by the use of co-solvents such as surfactants, reduces the toxicity of the preparation, improves bioavailability, and reduces the dosage. Prolong the administration time.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cabazitaxel protein nano-injection and a preparation method thereof. Background technique [0002] Cabazitaxel belongs to the class of taxane antineoplastic drugs, which is a semi-synthetic paclitaxel derivative derived from the compound extracted from the needles of taxus. Its mechanism of action is similar to other taxane drugs, by promoting the assembly of microtubule dimers At the same time, it prevents the depolymerization process and stabilizes the microtubules, inhibits further cell division, thereby inhibiting the mitosis and proliferation of cancer cells. [0003] The currently marketed product is cabazitaxel injection. In order to increase the solubility of cabazitaxel and the stability of the preparation, a large amount of surfactants such as polysorbate 80 and dehydrated ethanol are added to the injection prescription as co-solvents. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/42A61P35/00
CPCA61K9/0019A61K9/19A61K31/337A61K47/42A61P35/00
Inventor 邓盛齐蒋芳罗玉莹郑林陶静
Owner 深圳市健开医药有限公司
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