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Cabazitaxel albumin nanoparticle preparation for injection and preparation method thereof

A technology of albumin nanoparticles and cabazitaxel, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of poor stability of preparations, increased toxicity and side effects, poor water solubility, etc., and achieve stability Improving, enhancing efficacy of medication safety and patient compliance

Inactive Publication Date: 2014-12-24
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the listed Cabazitaxel injection has its outstanding anti-tumor effect, there are also some unresolved problems: (1) Poor water solubility leads to the need to use surfactants to aid dissolution, while the Tween- 80, prone to allergic reactions
(2) Two dilutions are required clinically, which is time-consuming and laborious
(3) The resulting formulation has poor stability and must be used within 24 hours once diluted
(4) The tissue is widely distributed and has no targeting to the tumor site, which weakens its anti-tumor effect to a certain extent and increases systemic side effects
Chinese patents CN102415999 A, CN103495179 A, ​​CN103768024 A, etc. disclose that albumin is used to prepare nanoparticles, but in the preparation process, either chemical methods are used to prepare albumin nanoparticles, or a large amount of organic solvents are used, which is highly toxic

Method used

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  • Cabazitaxel albumin nanoparticle preparation for injection and preparation method thereof
  • Cabazitaxel albumin nanoparticle preparation for injection and preparation method thereof
  • Cabazitaxel albumin nanoparticle preparation for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031]Dissolve the prescribed amount of cabazitaxel in a mixed solvent of dichloromethane and absolute ethanol (9:1), add a certain volume of cottonseed oil, and ultrasonically make the mixture uniform as the organic phase. Take 10mg of human serum albumin dissolved in 10ml of deionized water as the water phase, at room temperature or in an ice-water bath, add the organic phase to the water phase drop by drop under high-speed shear, and continue shearing for a certain period of time to make colostrum , and further use a high-pressure homogenizer to homogenize, and then remove the organic solvent by rotary evaporation in a water bath at 40° C. to obtain cabazitaxel albumin nanoparticles.

Embodiment 2

[0033] Dissolve the prescribed amount of cabazitaxel in a mixed solvent of dichloromethane and absolute ethanol (1:3), add a certain volume of soybean oil, and ultrasonically make the mixture uniform as the organic phase. Take 100mg of bovine serum albumin dissolved in 10ml of deionized water as the water phase, at room temperature or in an ice-water bath, add the organic phase to the water phase drop by drop under high-speed shear, and continue shearing for a certain period of time to make colostrum , and further use a high-pressure homogenizer to homogenize, and then remove the organic solvent by rotary evaporation in a water bath at 40° C. to obtain cabazitaxel albumin nanoparticles.

Embodiment 3

[0035] Dissolve the prescribed amount of cabazitaxel in a mixed solvent of dichloromethane and absolute ethanol (1:9), add a certain volume of sesame oil, and ultrasonically make the mixture uniform as the organic phase. Dissolve 100mg of ovalbumin in 10ml of deionized water as the water phase, add the organic phase dropwise to the water phase at room temperature or in an ice-water bath under high-speed shearing, and continue shearing for a certain period of time to make colostrum. Further use a high-pressure homogenizer for homogenization, and then remove the organic solvent by rotary evaporation in a water bath at 40°C to obtain cabazitaxel albumin nanoparticles.

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Abstract

The invention provides a cabazitaxel albumin nanoparticle preparation and a preparation method thereof. The cabazitaxel albumin nanoparticle preparation comprises cabazitaxel, albumin and pharmaceutically necessary auxiliary materials and can be prepared with a high-pressure homogenization method, a film shearing method, a solvent evaporation method and the like. According to the cabazitaxel albumin nanoparticle preparation and the preparation method thereof, problems of the drug loading capacity and the stability of existing albumin nanoparticles are solved; a low-toxicity organic solvent is adopted, so that highly allergic reactions due to the fact that Tween-80 is adopted in a cabazitaxel injection liquid can be avoided; by the aid of the high permeability and the retention effect of the nanoparticle on tumors, more drugs can be targeted passively to be concentrated in tumor tissue, so that the anti-tumor effect is improved; the preparation method is simple and suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to preparation of insoluble drug cabazitaxel into soluble albumin nanoparticle preparation for injection and a preparation method thereof. The cabazitaxel albumin nano-preparation includes cabazitaxel, albumin and pharmaceutically necessary auxiliary materials, and can be prepared by methods such as high-pressure milk homogenization, film shearing, and solvent evaporation. The present invention can make use of the high permeability and retention effect of nanoparticles on tumors, enable more drugs to be passively targeted and concentrated in tumor tissues, and improve the anti-tumor effect; -80 (Tween-80) produced hypersensitivity reactions. The preparation method of the preparation is simple and suitable for large-scale industrial production. Background technique [0002] Cabazitaxel is a broad-spectrum anti-tumor drug, which mainly forms stable non-functional microtubule...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/337A61K47/42A61P35/00
Inventor 何勤高会乐邰晓伟
Owner SICHUAN UNIV
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