A kind of cabazitaxel long circulation liposome injection and preparation method thereof

A technology of long-circulating liposomes and cabazitaxel, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problem of low drug loading, poor in vitro stability and no effect. and other problems, to achieve the effect of improving bioavailability, simplifying clinical use, and using good stability.

Active Publication Date: 2018-07-03
南京西默思博检测技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The liposomes used in the prior art of the cabazitaxel composition have the disadvantages of poor stability in vitro and low drug loading: the liposomes of traditional composition leave the blood stream quickly and accumulate in the Kupffer of the liver. cells and splenic macrophages (RES)
Studies have shown that some people use polyethylene glycol or polysorbate or PEG (PEG is polyethylene glycol) cholesterol as a long-circulation material, but they have not achieved good results.

Method used

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  • A kind of cabazitaxel long circulation liposome injection and preparation method thereof
  • A kind of cabazitaxel long circulation liposome injection and preparation method thereof
  • A kind of cabazitaxel long circulation liposome injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Prescription (100ml capacity)

[0026]

[0027] Preparation Process:

[0028] The prescription amount of cabazitaxel, tocopherol polyethylene glycol 2000 succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and 1-oleoyl-2-hydroxyphosphatidylglycerol Placed in a 500ml round-bottomed flask, dissolved in 150ml of absolute ethanol, evaporate the ethanol on a rotary evaporator at a constant temperature of 55~60℃ in a water bath at 100rpm under reduced pressure, so that the composition forms a uniform type at the bottom of the flask Lipid membrane, another 6% maltodextrin aqueous solution was added to the above round bottom flask, and the membrane was washed with a rotary evaporator at 50°C until the lipid membrane was hydrated and turned into a white liposome suspension, followed by 0.45μm, 0.22μm, filter membrane sizing (3 times each), the final dispersion is divided into vials, and then freeze-dried to obtain.

Embodiment 2

[0030] Prescription (100ml capacity)

[0031]

[0032] Place the prescription amount of cabazitaxel, tocopherol polyethylene glycol succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and 1-oleoyl-2-hydroxyphosphatidylglycerol Put it in a 500ml round bottom flask and dissolve it with 150ml chloroform, then evaporate the chloroform on a rotary evaporator at a constant temperature of 55-60°C under a reduced pressure at 100rpm on a constant temperature water bath to make the composition form a uniform lipid film on the bottom of the flask. Add 10ml of deionized water, ultrasonic for 10min, 0.45μm, 0.22μm, filter membrane granulation, the long-circulating liposome containing cabazitaxel is obtained.

Embodiment 3

[0034] Prescription (100ml capacity)

[0035]

[0036] Preparation Process:

[0037] Place the prescription amount of cabazitaxel, tocopherol polyethylene glycol 2000 succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and distearoylphosphatidylglycerol After dissolving in a 500ml round bottom flask with 150ml of acetone / methanol (1:1) solvent, the solvent was evaporated on a rotary evaporator at a constant temperature of 55~60℃ in a constant temperature water bath at 100rpm under reduced pressure, so that the composition formed at the bottom of the flask. To homogenize the lipid film, add 6% maltose solution to the above round bottom flask, and wash the film with a rotary evaporator at 50°C until the lipid film is hydrated and becomes a white liposome suspension, and then passes through 0.45μm, 0.22μm, filter membrane sizing (3 times each), the final dispersion is divided into vials, and then freeze-dried to obtain.

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Abstract

The invention provides cabazitaxel long-circulation liposome injection and a preparation method thereof. The cabazitaxel long-circulation liposome injection comprises cabazitaxel or a pharmaceutically acceptable salt thereof, tocopherol polyethylene glycol succinate, distearoyl-phosphatidylethanolamine-polyethylene glycol-maleimide and phospholipid. The cabazitaxel long-circulation liposome injection is prepared by a film method. The liposome not only has the advantages of reduced toxicity, simple and convenient clinical use and improved bioavailability, but also has good stability of storage and use.

Description

Technical field [0001] The invention relates to a cabazitaxel liposome composition and a preparation method thereof, in particular to a cabazitaxel long-circulation liposome injection and a preparation method thereof. Background technique [0002] "Cabazitaxel" refers to the chemical name (2α, 5β, 7β, 10β, 13α)-4-acetoxy-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]- 2-hydroxy-3-phenylpropionyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytaxel-11-en-2-ylbenzene A drug substance of formate-propan-2-one (1:1). Cabazitaxel (currently sold by Sanofi-Aventis) is a white to off-white powder with a chemical formula of C 45 H 57 NO 14 ·C 3 H 6 O, and the molecular weight is 894.01 (acetone solvate) / 835.93 (without solvent). [0003] Cabazitaxel (cabazitaxel) is a taxane anti-tumor drug. It is a new microtubule inhibitor that can bind to tubulin, promote the assembly of microtubules and inhibit their decomposition, thereby stabilizing microtubules and inhibiting mitosis. The function of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/24A61P35/00
Inventor 包金远张孝清程晓佳蒋玉伟
Owner 南京西默思博检测技术有限公司
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