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Nanoparticles preparation encapsulated with carfilzomib, and preparation method thereof

A carfilzomib and nanoparticle technology, which is applied in the field of carfilzomib-encapsulated nanoparticle preparations and the preparation thereof, can solve the problems of poor water solubility, increased toxic and side effects, and is difficult to prepare, and achieves uniform particle size and impurity content. Low and high water solubility

Inactive Publication Date: 2016-09-07
LIANGJIANG MEDICINE CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, due to its poor water solubility, it is difficult to prepare a composition with a high enough concentration to produce the required pharmacological effects. Currently, the substituted cyclodextrin inclusion technology is used, which requires the addition of a large amount of cyclodextrin. The preparation process needs to be in weak acidity. environment, it is easy to produce new impurities in the preparation process, which will inevitably increase the toxicity and side effects and affect its clinical application

Method used

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  • Nanoparticles preparation encapsulated with carfilzomib, and preparation method thereof
  • Nanoparticles preparation encapsulated with carfilzomib, and preparation method thereof
  • Nanoparticles preparation encapsulated with carfilzomib, and preparation method thereof

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specific Embodiment approach

[0027] The invention provides a nanoparticle preparation loaded with carfilzomib, comprising:

[0028] Carfilzomib 1~20 parts by weight;

[0029] 0.5-10 parts by weight of lecithin;

[0030] 10~100 parts by weight of polyethylene glycol block copolymer;

[0031] The polyethylene glycol block copolymer is a PEG-PLGA-PEG triblock copolymer with a number average molecular weight of 5000-50000 and / or a PEG-PLGA block copolymer with a number average molecular weight of 5000-50000.

[0032] The present invention selects specific polyethylene glycol block copolymers, and uses lecithin as a surfactant, and the water solubility of the prepared carfilzomib nanoparticles is better than that of cyclodextrin inclusion carfilzomib. Higher water solubility and lower impurity content in the preparation.

[0033] In the nanoparticle preparation carrying carfilzomib provided by the present invention, the content of the carfilzomib is preferably 1-20 parts by weight, more preferably 5-15 part...

Embodiment 1

[0061] Dissolve 5 mg of carfilzomib, 2.5 mg of lecithin, 50 mg of mPEG-PLGA in 5 mL of dichloromethane as an organic phase, dissolve poloxamer at a concentration of 2 mg / mL, and dissolve hypromellose at a concentration of 0.4 mg / mL in 50 mL of purified water was added to obtain the aqueous phase. After the organic phase was added to the water phase, it was sheared at 15,000 rpm for 3 minutes with a high-speed emulsification shearer to obtain a carfilzomib nanoemulsion. The emulsion was placed in a fume hood overnight and stirred to remove the organic phase to obtain carfilzomib nanoparticle suspension. After the suspension was removed by centrifugation to remove free drug and surfactant, a nanoparticle preparation loaded with carfilzomib was obtained, which was stored in a refrigerator at 4°C. Gained nanoparticle mean particle size is 265nm, and its particle size distribution figure is shown in attached figure 1 ; The drug loading capacity is 11.08%, and the encapsulation ef...

Embodiment 2

[0073] Dissolve 5 mg of carfilzomib and 50 mg of PEG-PLGA-PEG triblock copolymer in 5 mL of dichloromethane as an organic phase, and dissolve poloxamer in purified water at a concentration of 2 mg / mL to obtain an aqueous phase. After the organic phase was added to the water phase, it was sheared at 15,000 rpm for 3 minutes with a high-speed emulsification shearer to obtain a carfilzomib nanoemulsion. The emulsion was placed in a fume hood overnight and stirred to remove the organic phase to obtain carfilzomib nanoparticle suspension. The suspension was centrifuged to remove free drug and surfactant, and stored in a refrigerator at 4°C. The average particle diameter of the obtained nanoparticles is 180nm, the drug loading capacity is 10.32%, and the encapsulation efficiency is 85.35%.

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Abstract

The invention provides a nanoparticles preparation loaded with carfilzomib. The preparation includes, by weight, 1-20 parts of carfilzomib, 0.5-10 parts of lecithin, 10-100 parts of polyethylene glycol copolymer, which is a PEG-PLGA-PEG triblock copolymer with number-average molecular weight of 5000-50000 and / or a PEG-PLGA block copolymer with the number-average molecular weight of 5000-50000. The invention selects the specific polyethylene glycol copolymer, and uses lecithin as a surfactant. The prepared nanoparticles encapsulated with carfilzomib have water solubility better than carfilzomib encapsulated with cyclodextrin, have high water solubility, uniform particle size, and lower impurity content.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a nanoparticle preparation loaded with carfilzomib and a preparation method thereof. Background technique [0002] Carfilzomib is an intravenously administered tetrapeptide epoxyketone skeleton proteasome inhibitor for the treatment of recurrent multiple It was approved for marketing by the US Food and Drug Administration (FDA) on July 20, 2012. [0003] However, due to its poor water solubility, it is difficult to prepare a composition with a high enough concentration to produce the required pharmacological effects. Currently, the substituted cyclodextrin inclusion technology is used, which requires the addition of a large amount of cyclodextrin, and the preparation process needs to be in weak acidity. It is easy to produce new impurities during the preparation process of the preparation, which will inevitably increase the toxic and side effects and affect i...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/19A61K38/08A61K47/24
CPCA61K9/19A61K9/5146A61K38/08A61K47/24
Inventor 余灏贺耘其他发明人请求不公开姓名
Owner LIANGJIANG MEDICINE CO LTD
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