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Irinotecan hydrochloride nanometer fat beam preparation and preparation method thereof

A technology of irinotecan hydrochloride and nano-lipid bundle preparation, which is applied in the field of medicine, can solve the problems of complex components, difficult to master the ratio, poor practicability, etc., and achieves the effects of simple components, simple preparation scheme and reduced toxicity.

Active Publication Date: 2014-10-08
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the composition of the lipid beam preparation of the above-mentioned patent is complex, it is difficult to grasp its proportion, it is difficult to prepare, and the practicability is poor; the particle size of the lipid beam preparation in the above-mentioned patent is about 100nm, and according to literature reports, only nanoparticles with a diameter of <50nm have obvious The effect of passively targeting tumors; the above-mentioned patent does not specify the encapsulation efficiency of the obtained lipid bundle preparation. It is known in the art that the greater the encapsulation efficiency, the greater the effective concentration of the drug in the blood, and the reduction of the drug concentration during the production process. investment and substantial cost savings

Method used

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  • Irinotecan hydrochloride nanometer fat beam preparation and preparation method thereof
  • Irinotecan hydrochloride nanometer fat beam preparation and preparation method thereof
  • Irinotecan hydrochloride nanometer fat beam preparation and preparation method thereof

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Effect test

Embodiment 1

[0032] 1) Preparation of Irinotecan Hydrochloride Nano Lipid Beam Preparation

[0033] a) Weigh 1 g of PLGA-PEG and 10 g of water and dissolve at room temperature to obtain a solution.

[0034] b) Add 1 g of irinotecan hydrochloride to the solution prepared in step a, dissolve at room temperature, and stir thoroughly to obtain a clear solution, then filter to obtain irinotecan hydrochloride nano-lipid bundle preparation, which is protected by nitrogen gas and sealed for storage.

[0035] 2) Preparation of Irinotecan Hydrochloride Nano-Preparation

[0036] Dilute the irinotecan hydrochloride nano-lipid formulation prepared in step 1 with 20 times the volume of glucose solution to obtain the irinotecan hydrochloride nano-formulation.

Embodiment 2

[0038] 1) Preparation of Irinotecan Hydrochloride Nano Lipid Beam Preparation

[0039] a) Weigh 2g of PLGA-PEG and 20g of water, stir and dissolve in a 40°C water bath to obtain a solution.

[0040] b) Add 1 g of irinotecan hydrochloride to the solution prepared in step a, dissolve in a water bath at 50° C., stir thoroughly to obtain a clear solution, and filter to obtain irinotecan hydrochloride nano-lipid bundle preparation, which is protected by nitrogen gas and sealed for storage.

[0041] 2) Preparation of Irinotecan Hydrochloride Nano-Preparation

[0042] Dilute the irinotecan hydrochloride nano-lipid formulation prepared in step 1 with 20 times the volume of normal saline to obtain the irinotecan hydrochloride nano-formulation.

Embodiment 3

[0044] 1) Preparation of Irinotecan Hydrochloride Nano Lipid Beam Preparation

[0045] a) Weigh 2g PLGA-PEG and 30g water, stir and dissolve at room temperature to obtain a solution.

[0046] b) Add 1 g of irinotecan hydrochloride to the solution prepared in step a, dissolve in a water bath at 50° C., stir thoroughly to obtain a clear solution, and filter to obtain irinotecan hydrochloride nano-lipid bundle preparation, which is protected by nitrogen gas and sealed for storage.

[0047] 2) Preparation of Irinotecan Hydrochloride Nano-Preparation

[0048] Dilute the irinotecan hydrochloride nano-lipid formulation prepared in step 1 with 30 times the volume of glucose solution to obtain the irinotecan hydrochloride nano-formulation.

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Abstract

The invention discloses an irinotecan hydrochloride nanometer fat beam preparation, which comprises an entrapment material, and irinotecan hydrochloride and a water-based solvent for injection, wherein the entrapment material is one or at least two of PLGA-PEG, PGA-PEG, PCL-PEG, PEG-NH2, PEG-COOH, DSPE-PEG, Solutol HS15, and phospholipid. The invention also discloses a preparation method for the irinotecan hydrochloride nanometer fat beam preparation and irinotecan hydrochloride nanometer fat beam powder preparation prepared by the method. The encapsulation efficiency of the irinotecan hydrochloride nanometer fat beam preparation reaches up to 85%, the grain size of the irinotecan hydrochloride nanometer fat beam preparation is about 10nm, and the irinotecan hydrochloride nanometer fat beam preparation can realize passive target to tumors and can increase pharmacological function and reduce the toxic and side effects of the system. The irinotecan hydrochloride nanometer fat beam powder preparation improves the safety and compliance of the irinotecan hydrochloride preparation, lowers the toxicity of the irinotecan hydrochloride, and prolongs the circulation time in the body. The preparation method is simple and feasible, has good repeatability, and is applicable to industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a nano-lipid bundle preparation and a preparation method thereof, in particular to an irinotecan hydrochloride nano-lipid bundle preparation and a preparation method thereof. Background technique [0002] Irinotecan hydrochloride is a derivative of camptothecin. Camptothecin is a five-membered ring alkaloid extracted and isolated from the Chinese native plant Camptotheca acuminata by Wall et al. in the United States in 1966. Camptothecin has strong anticancer activity and broad antitumor spectrum. Camptothecin can specifically bind to type I topoisomerase, and inhibit related DNA replication repair, gene recombination and transcription by inhibiting topoisomerase. [0003] However, there are certain problems in the use of camptothecin as a drug. Its toxic side effects such as bone marrow suppression and hemorrhagic cystitis, and its poor water solubility limit its clinical appli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4745A61P35/00
CPCA61K9/107A61K31/4745
Inventor 梁兴杰李婵张春秋陈飞金叔宾王浩吴雁杨蓉
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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