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Elemene cabazitaxel compound flexible emulsion and preparation method thereof

A flexible technology of cabazitaxel and compound formula, which is applied in the fields of pharmaceutical formulation, emulsion delivery, organic active ingredients, etc., can solve problems such as drug penetration into cells, drug resistance, safety, and problems, and achieve remarkable results. Prospect of clinical transformation application, reduction of toxicity and irritation, and effect of enhancing curative effect

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 large irritation of the cabazitaxel-elemene compound preparation in the prior art, and the safety problem in clinical application, and the problem of the permeability and drug resistance of the drug entering the cell is not considered. , to provide a kind of elemene-cabazitaxel compound flexible emulsion and its preparation method, encapsulating elemene and cabazitaxel in the flexible emulsion at the same time can make the two drugs synergistically act on tumor cells, after adding a certain amount When elemene is improved into a flexible emulsion, the pharmacokinetic behavior of the drug is significantly improved, the drug resistance effect and the penetration into cells are enhanced, the curative effect is enhanced, the dosage of cabazitaxel is reduced, and the dosage of cabazitaxel is reduced. The toxic side effects of taxel and the irritation of elemene significantly improve the safety of the drug

Method used

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  • Elemene cabazitaxel compound flexible emulsion and preparation method thereof
  • Elemene cabazitaxel compound flexible emulsion and preparation method thereof
  • Elemene cabazitaxel compound flexible emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A kind of elemene-cabazitaxel compound flexible emulsion, calculated in 100mL, raw materials include: 0.5g elemene, 0.1g cabazitaxel, 5g medium-chain triglycerides, 2.5g soybean lecithin, 1g vitamin E polyethylene glycol Succinate, 2.6g glycerin, balance water.

[0040] The preparation method of above-mentioned elemene cabazitaxel compound flexible emulsion comprises the following steps:

[0041] (1) Preparation of the oil phase: melting medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate, elemene and cabazitaxel in a water bath at 80°C in proportion to obtain the oil phase;

[0042] (2) Water phase preparation: mix glycerin and water, heat and dissolve at 60°C to obtain a water phase;

[0043] (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 15...

Embodiment 2

[0045] A kind of elemene-cabazitaxel compound flexible emulsion, calculated in 100mL, raw materials include: 0.1g elemene, 0.1g cabazitaxel, 5g medium-chain triglycerides, 2.5g soybean lecithin, 1g vitamin E polyethylene glycol Succinate, 2.6g glycerin, balance water.

[0046] The preparation method of above-mentioned elemene cabazitaxel compound flexible emulsion comprises the following steps:

[0047] (1) Preparation of the oil phase: melting medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate, elemene and cabazitaxel in a water bath at 80°C in proportion to obtain the oil phase;

[0048] (2) Water phase preparation: mix glycerin and water, heat and dissolve at 60°C to obtain a water phase;

[0049] (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 hydrochloric acid to adjust the pH of the system to 4.5, add water to 100mL, and then homogenize twice at 25000psi, Coo...

Embodiment 3

[0051] A kind of elemene-cabazitaxel compound flexible emulsion, calculated in 100mL, raw materials include: 2g elemene, 0.1g cabazitaxel, 5g medium-chain triglycerides, 2.5g soybean lecithin, 1g vitamin E polyethylene glycol succinate Ester, 2.6g glycerin, the balance is water.

[0052] The preparation method of above-mentioned elemene cabazitaxel compound flexible emulsion comprises the following steps:

[0053] (1) Oil phase preparation: melt medium-chain triglycerides, soybean lecithin, vitamin E polyethylene glycol succinate, elemene and cabazitaxel in a water bath at 70°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 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 , homoge...

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Abstract

The invention discloses an elemene cabazitaxel compound flexible emulsion and a preparation method thereof. The emulsion is prepared from the following raw materials: 0.1-2g / 100mL elemene, 0.05-0.3 g / 100mL cabazitaxel, 2-20g / 100mL oil, 1-3g / 100mL phospholipid, 0.3-4g / 100mL polyethylene glycol derivative, 2-10g / mL osmotic pressure regulator and the balance of water. The preparation method comprisesthe following steps: (1) melting the oil, the phospholipid, the polyethylene glycol derivative, the elemene and the cabazitaxel to obtain an oil phase; (2) mixing the osmotic pressure regulator withthe water to obtain a water phase; and (3) adding the oil phase into the water phase, performing shearing and homogenizing under high pressure, adjusting the pH value, and performing sub-packaging. The elemene and the cabazitaxel are encapsulated in the flexible emulsion at the same time, so that the pharmacokinetic behavior of medicines is remarkably improved, the anti-drug-resistance effect of the medicines and the permeability of the medicines entering cells are improved, the curative effect is enhanced, and the safety of the medicines is remarkably improved.

Description

technical field [0001] The invention relates to the technical field of tumor chemotherapeutic drugs, in particular to a compound flexible emulsion of elemene-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. The progression of many life-threatening diseases such as cancer is influenced by multiple mechanisms. Due to this complexity, success with single-drug therapy is limited, so drug combinations are often used to fight cancer and enhance efficacy. [0003] 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 sho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/14A61K47/24A61K47/22A61K31/015A61K31/337A61P35/00
CPCA61K9/107A61K47/14A61K47/24A61K47/22A61K31/015A61K31/337A61P35/00A61K2300/00Y02P20/55
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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