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Cabazitaxel liposome injection and preparation method thereof

A cabazitaxel and injection technology, which is applied in the field of liposome compositions and their preparation, can solve the problems of leakage of encapsulated substances, liposome fusion, complicated steps, etc., and achieves reduced toxicity, improved bioavailability, and prolonged circulation. effect of time

Inactive Publication Date: 2014-05-07
NANJING LUYE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (2) Before clinical use, two-step dilution is required, that is, first dilute with 13% ethanol, then dilute with glucose, and need to be filtered. The clinical use steps are cumbersome, and there are potential safety hazards in medication
Because liposomes may undergo various changes during placement, such as phospholipids can be oxidized and hydrolyzed, liposomes may undergo changes such as aggregation and fusion, thereby causing leakage of packaged substances, the present invention overcomes the above-mentioned problems of liposomes. Deficiencies, providing a liposome of cabazitaxel with good stability and sufficient stability during storage

Method used

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  • Cabazitaxel liposome injection and preparation method thereof
  • Cabazitaxel liposome injection and preparation method thereof
  • Cabazitaxel liposome injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Put 40mg of cabazitaxel, 500mg of egg yolk lecithin, 200mg of hydrogenated soybean lecithin, 100mg of mPEG2000 modified bis-stearylphosphatidylethanolamine (DSPE-mPEG2000), 10mg of cholesterol in a 500ml round-bottomed flask, dissolve in 200ml of absolute ethanol, Rotary evaporator on a constant temperature water bath at 55-60°C evaporates ethanol at 100rpm and reduced pressure, so that phospholipids and drugs form a uniform lipid film at the bottom of the flask, and add 8ml of 5% mannitol aqueous solution to the above-mentioned round bottom flask Wash the membrane with a rotary evaporator at 50°C until the lipid film is hydrated and turns into a white liposome suspension, and extrude the whole particle through 0.4, 0.2, and 0.1 μm in sequence (3 times each) to obtain the product. Dissolve 8000 mg of sucrose in liposomes, after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion is divided into vials, and then freeze-dried.

[0021] After the fre...

Embodiment 2

[0023] Weigh 10mg of cabazitaxel, 335mg of soybean lecithin, 5mg of cholesterol and 15mg of mPEG2000 modified distearoylphosphatidylethanolamine (DSPE-mPEG2000) into a 100ml round-bottomed flask and dissolve in 50ml of chloroform / methanol (1:1) mixed solvent , on a constant temperature water bath at 55-60°C with a rotary evaporator at 100rpm and under reduced pressure to evaporate the mixed solvent, so that the phospholipids and drugs form a uniform lipid film at the bottom of the flask, and add 3.5ml of 5% glucose aqueous solution to the above In a round-bottomed flask, rotate 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 extrude the whole particle through 0.4, 0.2, and 0.1 μm in sequence (3 times each), that is, have to. Dissolve 700 mg of glucose in liposomes, after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion is divided into vials, and then freeze-dried. ...

Embodiment 3

[0026] Weigh 10mg of cabazitaxel, 400mg of soybean lecithin, 50mg of double myristyl phosphatidylglycerol (DMPG) and 7.5mg of cholesterol into a 100ml round bottom flask, dissolve in 50ml of chloroform / methanol (1:1) mixed solvent, and place at 55~ Rotary evaporator on a constant temperature water bath at 60°C evaporates the mixed solvent under the condition of 100rpm and reduced pressure, so that phospholipids and drugs form a uniform lipid film at the bottom of the flask, and add 3.5ml 5% glucose aqueous solution to the above round bottom flask , rotate and wash the membrane with a rotary evaporator at 50°C until the lipid film is hydrated and becomes a white liposome suspension, and then extrude the whole pellet through 0.4, 0.2, and 0.1 μm in turn (3 times each), that is, 450mg Mannitol was dissolved in liposomes, and after sterile filtration (membrane filter pore size 0.2 μm), the final dispersion was dispensed into vials and freeze-dried.

[0027] After the freeze-dried ...

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Abstract

The invention provides a cabazitaxel liposome injection and a preparation method thereof. The cabazitaxel liposome injection comprises cabazitaxel, phosphatide, cholesterol, and mannitol or glucose, and can be prepared through the vacuum film condensation method, the rotary evaporation method, reverse evaporation method, high-pressure homogenization method, and pH gradient method. The cabazitaxel liposome injection has the advantages of reduced toxicity, convenience in clinic, and improved biological availability, and furthermore avoids the a plurality of changes of liposome during the storage process, such as oxidation and hydrolysis of phosphatide, agglomeration and fusion of liposome, and the like, wherein the changes can cause the leakage of coated substance. The invention provides a cabazitaxel liposome which has a good stability and is enough stable in the storage period.

Description

technical field [0001] The invention relates to a liposome composition and a preparation method thereof, in particular to a cabazitaxel liposome injection and a preparation method thereof. Background technique [0002] Cabazitaxel is a taxane antineoplastic drug and a new microtubule inhibitor that can bind to tubulin, promote the assembly of microtubules and inhibit their disassembly, thereby stabilizing microtubules and inhibiting mitosis. It plays an anti-tumor role in the function of tumor cells in phase and interphase. The drug was effective not only against docetaxel-sensitive tumors, but also in tumor models insensitive to other chemotherapy drugs, including docetaxel. [0003] Currently, the only Cabazitaxel preparations on the market are Cabazitaxel injection (trade name: Jevtan) developed by Sanofi-Aventis, France. The injection is firstly dissolved in Tween-80 (Tween-80), diluted with 13% ethanol to 10 mg / ml before clinical use, and further diluted with 5% gluco...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/337A61K47/28A61P35/00
Inventor 李锦陈文忠程光柯志意翁帼英程培元
Owner NANJING LUYE PHARMA
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