Application of Picantron as Lymphatic Tracer

A tracer, the technology of Picantron, which is applied in the field of new drug indications, can solve the problems of residual preparation process at the injection site, slow tracer staining time, large diffusion of surrounding tissues, etc., and achieves low price, low toxicity, and high diffusion little effect

Active Publication Date: 2019-06-04
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to solve the problems of slow dyeing time, short maintenance time, large diffusion of surrounding tissue, serious residue at the injection site and complicated preparation process of the existing tracers, and provide picantron and its salts as lymphatic tracers. Applications

Method used

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  • Application of Picantron as Lymphatic Tracer
  • Application of Picantron as Lymphatic Tracer
  • Application of Picantron as Lymphatic Tracer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1, the preparation of picantron hydrochloride

[0042] Weigh 1 g of picantron maleate as a starting material, dissolve it with MQ ultrapure water as a solvent, and ultrasonically dissolve it fully. Next, 717-strong base anion exchange resin (200mL swelling volume) was used as the exchanger for maleate radical exchange. Shake at room temperature for 30 minutes, take the solution out of the resin, soak the resin with water several times, and take out the free picantron solution as much as possible. Freeze-drying the obtained free picantron solution to obtain free picantron powder. Take MQ ultrapure water as a solvent to dissolve, take hydrochloric acid with a concentration equal to 1M to carry out a salt-forming reaction, and keep the reaction on a shaker for 1 hour. The reaction solution was freeze-dried to obtain picantron hydrochloride powder (yield 95%). 1 H-NMR (DMSO) δ-3.10 (dd, 4H), 3.82 (dd, 4H), 7.70 (d, 2H), 8.08 (d, 1H), 8.31 (s, 6H), 9.02 (d, 1H)...

Embodiment 2

[0043] Embodiment 2, the preparation of picantron sulfate

[0044] According to the method described in Example 1, replace "1M hydrochloric acid for salt-forming reaction" with "1M sulfuric acid for salt-forming reaction" to obtain Picantron sulfate powder. 1 H-NMR (DMSO) δ-3.10 (dd, 4H), 3.79 (dd, 4H), 7.65 (d, 2H), 7.92 (d, 1H), 8.16 (s, 6H), 9.03 (d, 1H), 9.49 (s, 1H), 10.96 (d, 2H).

Embodiment 3

[0045] Embodiment 3, the preparation of picantron trifluoroacetate

[0046] According to the method described in Example 1, replace "1M hydrochloric acid for salt formation reaction" with "1M trifluoroacetic acid for salt formation reaction" to obtain picantron trifluoroacetate powder. 1 H-NMR(DMSO)δ-3.10(dd, 4H), 3.80(dd, 4H), 7.64(d, 2H), 7.8.08(s, 6H, 1H), 9.01(d, 1H), 9.45(s , 1H), 10.97(d, 2H).

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Abstract

The invention provides application of pixantrone (a compound in a formula I) and salts (such as pixantrone maleate, pixantrone hydrochloride, pixantrone sulfate, pixantrone acetate, pixantrone trifluoroacetate, pixantrone citrate, pixantrone malate and pixantrone tartrate) thereof in serving as a lymphatic tracer or in preparing the lymphatic tracer. The pixantrone and the salts thereof can be prepared into preparations such as injections, powder injections, an emulsion, lipidosome, nanoparticles, microspheres and the like, can directly exert the effect of killing malignant cells, have blue-staining characteristics, can serve as the lymphatic tracer to be applied to introoperative lymphadenectomy in a cancer operation therapy and is applicable to a stomach caner, a breast cancer, an intestinal cancer, a cervical cancer, a testicular cancer and the like.

Description

technical field [0001] The invention belongs to the field of new drug indications, and in particular relates to the application of picantron as a lymphatic tracer. Background technique [0002] Malignant tumors have become the second leading cause of death in humans after cardiovascular diseases. Every year, there are more than 12 million new patients with malignant tumors in the world, and about 7.6 million patients die of cancer. In 2010, there were 3.09 million new cancer patients in my country every year, and 1.94 million patients died of cancer, accounting for about 1 / 4 of the global cancer deaths. In the past 20 years, the cancer mortality rate in China has increased by nearly 30%, and one out of every four or five deaths is due to cancer. Early detection and diagnosis of cancer can buy time for cancer treatment, which is of special significance to the lives of patients. Timely and thorough surgery to remove cancer cells is the key to successful cancer treatment. As...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/00A61K31/473A61P35/00
Inventor 黄蔚王洪田小波蒋柏凤
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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