Cabazitaxel flexible emulsion and preparation method thereof

A Cabazitaxel and Saiflexible technology, which is applied in the fields of pharmaceutical formulation, emulsion delivery, organic active ingredients, etc., can solve problems such as the permeability and drug resistance of Cabazitaxel, and achieve good anti-paclitaxel resistance, Moderate particle size and strong permeability

Active Publication Date: 2020-11-06
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the safety problems in the clinical application of cabazitaxel injection reagents in the prior art, without considering the permeability and drug resistance of cabazitaxel into cells, and to provide a flexible emulsion of cabazitaxel and the preparation method thereof, the cabazitaxel is encapsulated in a flexible emulsion, which significantly improves the pharmacokinetic behavior of the cabazitaxel, enhances the anti-drug resistance of the cabazitaxel and the permeability into cells, thereby improving the curative effect; and Avoid the side effects of allergic excipients such as polysorbate 80 and irritating solvents such as ethanol, significantly reduce the toxic and side effects of cabazitaxel, and improve safety

Method used

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  • Cabazitaxel flexible emulsion and preparation method thereof
  • Cabazitaxel flexible emulsion and preparation method thereof
  • Cabazitaxel flexible emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]A flexible emulsion of cabazitaxel, raw materials include: 0.1g / 100mL cabazitaxel, 5g / 100mL medium-chain triglycerides, 2.5g / 100mL soybean lecithin, 1g / 100mL vitamin E polyethylene glycol succinate, 2.6g / 100mL glycerin, the balance is water.

[0038] The method for preparing 100mL above-mentioned cabazitaxel flexible emulsion comprises the steps:

[0039] (1) Preparation of the oil phase: Melt medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate and cabazitaxel in a water bath at 80°C in proportion to obtain the oil phase;

[0040] (2) Water phase preparation: mix glycerin and water, heat and dissolve at 60°C to obtain a water phase;

[0041] (3) Mix and homogenize: Add the oil phase to the water phase, cut in a 60°C water bath at 15000r / min for 30min, add 0.1mol / L sodium hydroxide / 0.1mol / L hydrochloric acid to adjust the pH of the system to 6.0, add water to make it 100mL , then 15000psi homogenized 4 times, cooled to room temperature...

Embodiment 2

[0044] A flexible emulsion of cabazitaxel, raw materials include: 0.1g / 100mL cabazitaxel, 10g / 100mL medium chain triglycerides, 2.5g / 100mL soybean lecithin, 1g / 100mL vitamin E polyethylene glycol succinate, 2.6g / 100mL glycerin, the balance is water.

[0045] The method for preparing 100mL above-mentioned cabazitaxel flexible emulsion comprises the steps:

[0046] (1) Preparation of the oil phase: Melt medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate and cabazitaxel in a water bath at 80°C in proportion to obtain the oil phase;

[0047] (2) Water phase preparation: mix glycerin and water, heat and dissolve at 60°C to obtain a water phase;

[0048] (3) Mix and homogenize: add the oil phase to the water phase, cut in a 60°C water bath at 15000r / min for 30min, add water to 100mL and then homogenize at 10000psi for 6 times, after cooling to room temperature, add 0.1mol / L hydrochloric acid to adjust the pH of the system To 4.5, a translucent e...

Embodiment 3

[0051] A kind of flexible emulsion of cabazitaxel, raw materials include: 0.1g / 100mL cabazitaxel, 20g / 100mL medium chain triglyceride, 1g / 100mL soybean lecithin, 1g / 100mL vitamin E polyethylene glycol succinate, 2.6g / 100mL 100mL glycerin, the balance is water.

[0052] The method for preparing 100mL above-mentioned cabazitaxel flexible emulsion comprises the steps:

[0053] (1) Preparation of the oil phase: Melt medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate and cabazitaxel in a water bath at 80°C in proportion to obtain the oil phase;

[0054] (2) Water phase preparation: mix glycerin and water, heat and dissolve at 60°C to obtain a water phase;

[0055] (3) Mix and homogenize: add the oil phase to the water phase, cut in a water bath at 60°C at 15000r / min for 30min, add water to 100mL and then homogenize twice at 30000psi, cool to room temperature and add 0.1mol / L sodium hydroxide to adjust When the pH of the system reaches 7.0, an op...

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Abstract

The invention discloses cabazitaxel flexible emulsion and a preparation method thereof. Raw materials of the cabazitaxel flexible emulsion comprise 0.02 to 0.3g per 100mL of cabazitaxel, 2 to 25g per100mL of oil, 1 to 3g per 100mL of phospholipid and 0.3 to 4g per 100mL of polyethylene glycol derivative, and further comprise 2 to 10g per 100mL of osmotic pressure regulating agent or 10 to 20g per100mL of freeze-drying protective additive and the balance of water. The preparation method comprises the steps of: (1) fusing the oil, the phospholipid, the polyethylene glycol derivative and the cabazitaxel to obtain an oil phase; (2) mixing the osmotic pressure regulating agent and water to obtain an aqueous phase; (3) adding the oil phase into the aqueous phase, carrying out shearing, makingup to a volume, carrying out high pressure homogenization and regulating pH; and (4) carrying out subpackaging or freeze-drying. According to the invention, the cabazitaxel is encapsulated in the flexible emulsion, a pharmacokinetic behavior of the cabazitaxel is improved, and anti-drug resistance and permeability of the cabazitaxel are reinforced, so that a curative effect is improved; and toxicor side effects are reduced, and safety is improved.

Description

technical field [0001] The invention relates to the technical field of tumor chemotherapeutic drugs, in particular to a flexible emulsion of cabazitaxel and a preparation method thereof. Background technique [0002] Taxanes such as paclitaxel and docetaxel, as an important part of tumor chemotherapy drugs, have become the first-line drugs in tumor chemotherapy. However, with the widespread use of taxane drugs, the contradiction of tumor resistance to taxanes has become increasingly prominent. Cabazitaxel, a novel semi-synthetic taxane compound, the molecular formula is C 45 h 57 NO 14 , with a molecular weight of 835.94, almost insoluble in water, soluble in ethanol. Preclinical animal studies have shown that cabazitaxel has broad-spectrum anti-tumor activity, including prostate cancer, colon cancer, lung cancer, breast cancer, etc., and can overcome docetaxel resistance and penetrate the blood-brain barrier. Compared with other paclitaxel drugs, due to the introductio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K47/44A61K47/24A61K47/26A61K31/337A61P35/00
CPCA61K9/107A61K9/19A61K47/44A61K47/24A61K47/26A61K31/337A61P35/00Y02P20/55
Inventor 谢恬曾昭武曾义英曾义军隋新兵楼剑书刘水平
Owner HANGZHOU NORMAL UNIVERSITY
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