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High-purity multi-arm anticancer conjugate

A high-purity, high-purity technology, applied in the field of medicine, can solve the problems of heptanesulfonic acid replacement, affecting the purity of medicines into medicinal salts, and the inability to remove heptanesulfonic acid.

Active Publication Date: 2019-09-20
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since sodium heptanesulfonate is converted into heptanesulfonic acid after preparation and purification by HPLC, heptanesulfonic acid is a strong acid and will form a salt with BGC0222, and heptanesulfonic acid cannot be completely replaced by weak acid, so that desalination in subsequent purification During the process, the heptanesulfonic acid cannot be completely removed, and more heptanesulfonic acid and BGC0222 are salted, which directly affects the purity of the drug and the stability of the subsequent medicinal salt

Method used

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  • High-purity multi-arm anticancer conjugate

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Experimental program
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Effect test

Embodiment 1

[0028] The first step of purification:

[0029] Preparation column: 300DAC 300×250mm, filler: Unisil 10-300C18, mobile phase water phase: 0.02M sodium dihydrogen phosphate + 0.0075M sodium heptanesulfonate aqueous solution, mobile phase organic phase: acetonitrile, detection wavelength: 220nm;

[0030] BGC0222 crude product 200g, after dissolving with 10% (V / V) acetonitrile / water, load the sample, prepare and purify by HPLC, gradient elution (time: 0~100min; mobile phase organic phase concentration: 20%~60%), the collected purity is greater than 95% % of the components as the product of the first step of purification.

Embodiment 2

[0032] Pre-desalination:

[0033] Preparation column: 300DAC, filler: Unisil 10-300C18, mobile phase aqueous phase: 5‰ acetic acid aqueous solution, mobile phase organic phase: acetonitrile, detection wavelength: 220nm;

[0034] The pure products collected in the first step of purification were mixed, injected, gradient eluted (time: 0-80 min; mobile phase organic phase concentration: 5%-80%), and samples were collected.

Embodiment 3

[0036] Equilibrate and proceed to the second purification step:

[0037] Packing: anion exchange packing, model: UniGel-80Q, quantity: 2L, column: glass column (10*110cm), after the regeneration of ion exchange packing, the mobile phase washes the ion exchange column, and the mobile phase water phase is 5‰ (v / v) Acetic acid aqueous solution, mobile phase organic phase is acetonitrile, and the volume ratio of acetic acid aqueous solution and acetonitrile is 3:2, after equilibrating, load sample, use identical mobile phase ion exchange desalination, elute and collect product, obtain purity greater than 99% BGC0222.

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Abstract

The invention discloses a compound represented by the formula (I) and having a purity of more than 99%. The high-purity medicinal compound is obtained by the following method: (1) carrying out primary purification on a crude product of the compound represented by the formula (I) by ion pair chromatography with reversed-phase high performance liquid chromatography (RP-HPLC), and carrying out gradient elution with a mobile phase; (2) after primary purification, carrying out pre-desalination treatment, and carrying out gradient elution with a mobile phase; (3) after completion of pre-desalination treatment, swashing an ion exchange column by a mobile phase to achieve the purpose of balance; and (4) carrying out ion exchange by ion exchange chromatography, carrying out secondary purification, removing remaining heptane sulfonic acid, and thus obtaining the pure compound represented by the formula (I).

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a medicinal compound, in particular to a high-purity multi-arm anticancer conjugate. Background technique [0002] Chinese patent application 201710263114.9 discloses a multi-arm anti-cancer conjugate BGC0222, the structure of which is shown in formula (I): [0003] [0004] The compound is a multi-arm conjugate compound, and the basic structure of its drug carrier is four-arm polyethylene glycol, which is called 4ARM-PEG-20K, and its molecular weight is about 20kDa, which is large. complex structure. In the process of preparing BGC0222, the crude product of BGC0222 contains more impurities, and these impurities are mainly compounds that have not been fully coupled, and the existence of these impurities directly affects the drug loading capacity of the drug. In order to increase the drug loading capacity of the drug, the only way is to remove these uncoupled compounds to improve ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64C07K1/20C07K1/18A61P35/00
CPCC07K7/64A61K47/60A61K47/64A61P35/00
Inventor 袁建栋黄仰青宋云松
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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