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Cis-platinum microparticle system composition, preparation method and application

A system composition and microparticle technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of poor tumor efficacy and achieve high drug loading, high yield, and low cost effect

Active Publication Date: 2020-12-25
SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Kataoka and colleagues reported that particles larger than 30 nm have poor efficacy on poorly permeable tumors (Nat Nanotechnol, 2011), and Jain et al. also confirmed that nanoformulations with a particle size of 12 nm have better penetration on poorly permeable tumors Sex (Nat Nanotechnol, 2012)

Method used

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  • Cis-platinum microparticle system composition, preparation method and application
  • Cis-platinum microparticle system composition, preparation method and application
  • Cis-platinum microparticle system composition, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Weigh MPEG 2000 -P(GluNa) 2000 About 38.85mg, 48mg of silver nitrate, put in a 100m round bottom flask, add 30ml of distilled water, shake in a water bath at 40°C for 10 hours; centrifuge to remove the supernatant, collect the precipitate, then disperse the precipitate with 30ml of purified water, add cisplatin 45 mg of the raw material was placed in a 40°C water bath for 96 hours of shaking reaction; after the precipitate was completely dissolved, the solution was concentrated by 10KDa ultrafiltration and centrifugation, and the concentrated liquid was combined, passed through a 0.22 μm filter membrane, and then freeze-dried.

Embodiment 2

[0034] Weigh 45mg of cisplatin raw material, 48mg of silver nitrate, add 30ml of distilled water, shake and react in a water bath at 37°C for 4 hours; centrifuge to take the supernatant, and then add MPEG 2000 -P(GluNa) 2000 About 38.85mg, put it in a round bottom flask, shake it to dissolve, put it in a water bath at 37°C and shake it for 72 hours; then 10KDa ultrafiltration and centrifugation, concentrate, wash the concentrated solution several times, combine the concentrated liquids, pass through 0.22μm Filtered and freeze-dried.

Embodiment 3

[0036]Weigh 149mg of cisplatin raw material, 161.5mg of silver nitrate, MPEG 2000 -P(GluNa) 2000 Put 298mg in a 100m round-bottomed flask, add 50ml of distilled water, and shake in a water bath at 37°C for 4-10 hours; filter to remove silver chloride, take the subsequent filtrate and concentrate it by ultrafiltration and centrifugation at 10KDa; divide the concentrated liquid into freeze-dry.

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Abstract

The invention relates to a cis-platinum microparticle system composition which is lower in cost but has higher cis-platinum drug loading capacity and a macrophage phagocytosis shielding effect, and apreparation method. Cis-platinum nanoparticles prepared from a methoxy polyethylene glycol 2000-sodium polyglutamate copolymer (MPEG2000-P(GluNa)2000) as a carrier and cis-platinum under the preparation method conditions required by the patent have higher drug loading capacity, can better shield phagocytosis of macrophages in an in-vivo blood circulation process, and have better tumor tissue distribution.

Description

[0001] field of invention [0002] The invention belongs to the technical field of medicines, and specifically relates to the composition and preparation method of a microparticle system with lower cost but higher cisplatin drug load and shielding macrophage phagocytosis effect. Background technique [0003] Cisplatin (cis-dichlorodiammine platinum, CISP) is the first metal complex with anticancer activity discovered by American scientists Rosenborg et al. in 1965, and belongs to cell non-specific drugs. As a broad-spectrum anti-cancer drug, cisplatin has clinical curative effect and high anti-cancer activity on many cancers, such as breast cancer, ovarian cancer, cervical cancer, esophageal cancer, non-small spherical cell lung cancer and gastric cancer. However, its severe nephrotoxicity, auditory attenuation and other side effects limit the wide application of cisplatin and its platinum compounds in clinical practice. The human kidney’s clearance threshold for foreign matt...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/60A61K33/243A61P35/00
CPCA61K47/6935A61K47/60A61K33/243A61P35/00
Inventor 张震李军王维剑牛冲董朋伟
Owner SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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