Cabazitaxel protein nanometer injection and preparation method thereof

A nano-injection, cabazitaxel technology, applied in the field of pharmaceutical preparations, can solve the problems of hypersensitivity reactions with large toxic and side effects, hidden dangers of drug safety, large dosage, etc. release effect

Active Publication Date: 2019-08-02
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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  • Cabazitaxel protein nanometer injection and preparation method thereof
  • Cabazitaxel protein nanometer injection and preparation method thereof
  • Cabazitaxel protein nanometer injection and preparation method thereof

Examples

Experimental program
Comparison scheme
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 invention is applicable to the technical field of medicinal preparations, and provides a cabazitaxel protein nanometer injection and a preparation method thereof. The cabazitaxel protein nanometerinjection is prepared from the following raw materials in parts by weight: 50-150 parts of cabazitaxel, 400-4000 parts of a protein carrier material, 50-300 parts of a protein nanometer modified material, and 12-100 parts of a freeze-drying protective agent. According to the cabazitaxel protein nanometer injection and the preparation method thereof, the cabazitaxel is encapsulated into a spherical or ellipsoidal nanometer material formed by the protein carrier material and the protein nanometer modified material or is attached to the surface of the spherical or ellipsoidal nanometer material,and freeze-drying treatment is performed by using the freeze-drying protective agent; the obtained cabazitaxel protein nanometer injection has a relatively good slow-release effect, and has a relatively good anti-tumor effect at the same time, hypersensitivity caused by the use of cosolvents such as surfactants is effectively avoided, toxicity of the preparations is reduced, the bioavailability is improved, administration dosage is reduced, and administration time is prolonged.

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 Applications(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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