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Cabazitaxel long-circulation liposome injection and preparation method thereof

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

Active Publication Date: 2015-04-01
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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  • Cabazitaxel long-circulation liposome injection and preparation method thereof
  • Cabazitaxel long-circulation liposome injection and preparation method thereof
  • 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 prescribed amount of cabazitaxel, tocopheryl macrogol 2000 succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and 1-oleoyl-2-hydroxyphosphatidylglycerol Place in a 500ml round-bottomed flask, dissolve with 150ml of absolute ethanol, evaporate the ethanol on a rotary evaporator on a constant temperature water bath at 55-60°C at 100rpm and reduce pressure, so that the composition forms a uniform type at the bottom of the flask. Lipid film, add 6% maltodextrin aqueous solution into the above-mentioned 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. 0.22 μm, membrane sizing (3 times each), the final dispersion was divided into vials, and then freeze-dried to obtain.

Embodiment 2

[0030] Prescription (100ml capacity)

[0031]

[0032] Prescribed amounts of cabazitaxel, tocopheryl polyethylene glycol succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and 1-oleoyl-2-hydroxyphosphatidylglycerol were placed in Put it in a 500ml round bottom flask, dissolve it with 150ml chloroform, evaporate the chloroform on a rotary evaporator on a constant temperature water bath at 55-60°C at 100rpm and reduce pressure, so that the composition forms a uniform lipid film at the bottom of the flask, Add 10ml of deionized water, sonicate for 10min, 0.45μm, 0.22μm, and filter the membrane to complete the particle, and the long-circulating liposome containing cabazitaxel is obtained.

Embodiment 3

[0034] Prescription (100ml capacity)

[0035]

[0036] Preparation Process:

[0037] Prescribed amounts of cabazitaxel, tocopheryl macrogol 2000 succinate, distearoylphosphatidylethanolamine-polyethylene glycol 1200-maleimide and distearoylphosphatidylglycerol were placed in the In a 500ml round bottom flask, after dissolving with 150ml of acetone / methanol (1:1) solvent, evaporate the solvent on a rotary evaporator on a constant temperature water bath at 55 to 60°C at 100rpm and under reduced pressure, so that the composition forms a mixture at the bottom of the flask. Homogenize the lipid film, and add 6% maltose solution into the above-mentioned 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. 0.22 μm, membrane sizing (3 times each), the final dispersion was 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-epoxytaxane-11-en-2-ylbenzene Drug substance of formic acid-propan-2-one (1:1). Cabazitaxel (currently marketed by Sanofi-Aventis) is a white to off-white powder with the formula C 45 h 57 NO 14 ·C 3 h 6 O, and a molecular weight of 894.01 (acetone solvate) / 835.93 (without solvent). [0003] Cabazitaxel is a taxane antineoplastic drug and a new microtubule inhibitor that can bind to tubulin, promote the assembly of microtubules and inhibit its decomposition, thereby stabilizing microtubules and inhibiting mitosis. It plays an anti-tumor r...

Claims

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Application Information

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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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