Cabazitaxel protein nanomaterial and preparation method thereof

A technology of cabazitaxel and nanomaterials, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve toxic and side effects, hypersensitivity reactions, hidden dangers of drug safety, and dosage Large and other problems, to achieve the effect of prolonging the administration time, reducing the administration dose, and high encapsulation efficiency

Inactive Publication Date: 2019-08-16
深圳市健开医药有限公司 +1
View PDF7 Cites 3 Cited by
  • 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 nanomaterial 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cabazitaxel protein nanomaterial and preparation method thereof
  • Cabazitaxel protein nanomaterial and preparation method thereof
  • Cabazitaxel protein nanomaterial and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Cabazitaxel protein nanomaterials, including the following raw materials:

[0035] Cabazitaxel 50mg; Cholesterol 100mg; Bovine serum albumin 0.5g (0.5% concentration).

[0036] Preparation Process:

[0037] 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 (oil-water ratio 1:10); Add the oil phase into the water phase, and perform ultrasonication in an ice bath at 40% power for 8 min to form a primary emulsion; pass the primary emulsion through a high-pressure homogenizer at a pressure of Under the condition of 500bar, cycle 8 times; the treated emulsion was subjected to vacuum rotary evaporation at 35°C to remove the organic solvent, and centrifuged at 22000r / min (34700×g) for 30min at 4°C to remove the supernatant and precipitate Add proper amount of ultrapure water t...

Embodiment 2

[0039] Cabazitaxel protein nanomaterials, including the following raw materials:

[0040] Cabazitaxel 100mg; cholesterol 150mg; bovine serum albumin 1.5g (1.5%).

[0041] Preparation Process:

[0042] 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 precipitate for redissolution. have t...

Embodiment 3

[0044] Cabazitaxel protein nanomaterials, including the following raw materials:

[0045]Cabazitaxel 150mg; cholesterol 200mg; bovine serum albumin 1.5g (1.5%).

[0046] Preparation Process:

[0047] 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 an appropriate amount of ultrapure ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
encapsulation rateaaaaaaaaaa
Login to view more

Abstract

The invention is applicable to the technical field of pharmaceutical preparations, and provides a cabazitaxel protein nanomaterial and a preparation method thereof. The cabazitaxel protein nanomaterial comprises, by weight, 50-150 parts of cabazitaxel, 400-4000 parts of protein carrier materials and 50-300 parts of protein nano modifying materials. The cabazitaxel protein nanomaterial and the preparation method thereof have the advantages that the cabazitaxel is encapsulated in a spherical or ellipsoidal nano composed of the protein carrier materials and the protein nano modifying materials, or adhered to the surface of the nano, and the obtained cabazitaxel protein nanomaterial has uniform particle size, high encapsulation rate, and good sustained release effect and anti-tumor effect, sothat hypersensitive reactions caused by the use of co-solvents such as surfactants are effectively avoided, the toxicity of the preparations is reduced, the bioavailability is improved, the dosage isdecreased, and the medication 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 nanomaterial 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. Cl...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/337A61K47/42A61K47/24A61P35/00
CPCA61K9/5123A61K9/5169A61K31/337A61K47/24A61K47/42A61P35/00
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap