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O-carborane compound composition for assisting BNCT

A compound composition and o-carborane technology, which is applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., to achieve the effect of obvious enrichment effect

Pending Publication Date: 2021-03-16
南京艾斯特医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But BPA has a disadvantage: once the BPA level in tumor cells rises, it will be excreted through the "anti-transport" mechanism, which makes BNCT somewhat limited

Method used

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  • O-carborane compound composition for assisting BNCT
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  • O-carborane compound composition for assisting BNCT

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Add 10 grams of vitamin B12 crude product (content 96.512%) and 100 grams of methyl alcohol into a 500 milliliter round bottom flask, after cooling to 0-5 degrees, add 1 gram of sodium cyanoborohydride in 3 times, stir at room temperature for 1 hour, Filtration and vacuum drying at 50°C for 12 hours yielded 8.6 g of pure vitamin B12 with a yield of 86% and a purity greater than 99.674%. Chromatogram see figure 2 , see the data in the table below

[0028] Detector A214nm

[0029] Peak# Ret. Time area Height area% Conc. unit 1 3.600 44751 5051 0.180 0.180 2 3.876 3081 414 0.019 0.019 3 4.226 15886874 1606650 99.674 99.674 4 6.080 4291 385 0.027 0.027 5 6.863 3605 287 0.023 0.023 6 7.361 1221 95 0.008 0.008 7 19.341 10634 434 0.067 0.067 8 22.669 10720 467 0.067 0.067 9 22.875 3862 352 0.024 0.024 10 24.247 2392 182 0.015 0.015 11 24.49...

Embodiment 2

[0031] Add 10 grams of vitamin B12 crude product (content 96.512%) and 100 grams of ethanol into a 500 milliliter round bottom flask, after cooling down to 0-5 degrees, add 1 gram of sodium cyanoborohydride in 3 times, stir at room temperature for 2 hours, Filtration and vacuum drying at 50°C for 12 hours yielded 8.9 g of pure vitamin B12 with a yield of 89% and a purity greater than 99.464%. Chromatogram see image 3 , see the data in the table below

[0032] Detector A214nm

[0033] Peak# Ret. Time area Height area% Conc. unit 1 3.600 44751 5051 0.280 0.280 2 3.876 3081 414 0.019 0.019 3 4.226 15886874 1606650 99.464 99.464 4 6.080 4291 385 0.027 0.027 5 6.863 3605 287 0.023 0.023 6 7.361 1221 95 0.008 0.008 7 19.341 10634 434 0.067 0.067 8 22.669 10720 467 0.067 0.067 9 22.875 3862 352 0.024 0.024 10 24.247 2392 182 0.015 0.015 11 24.492 ...

Embodiment 3

[0035] (Blank experiment without adding sodium cyanoborohydride) 10 grams of vitamin B12 crude product (content 96.512%) and 100 grams of ethanol were added in a 500 ml round-bottomed flask, cooled to 0-5 degrees, and then stirred at room temperature for 2 hours. Filtration and vacuum drying at 50°C for 12 hours yielded 9.9 g of pure vitamin B12, with a yield of 99% and a purity of 96.912%. Chromatogram see Figure 4 , see the data in the table below

[0036] Detector A214nm

[0037] Peak# Ret. Time area Height area% Conc. unit 1 2.978 71287 5899 0.313 0.313 2 3.607 202610 22760 1.431 1.431 3 4.228 13668896 1410020 96.912 96.912 4 7.237 5171 332 0.037 0.037 5 16.184 148841 2561 1.051 1.051 6 19.283 7422 285 0.052 0.052 7 22.698 43870 1228 0.310 0.310 8 24.200 14838 452 0.105 0.105 total 14162934 1443537 100.000

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PUM

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Abstract

The invention discloses an o-carborane compound composition for assisting BNCT (Boron Neutron Capture Therapy), which comprises an o-carborane derivative and a refined vitamin B12 pure product in a mass ratio of 1: (8-12), and the purity of the vitamin B12 pure product is greater than 99%. As an auxiliary drug for BNCT drugs, the refined vitamin B12 and the o-carborane derivative are compounded, and the synergistic use makes the enrichment effect of BNCT drugs in tumor cells more obvious.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical auxiliary compositions, in particular to an o-carborane compound composition for assisting BNCT. Background technique [0002] Boron Neutron Capture Therapy, referred to as BNCT, is applied to thermal neutron irradiation to target boron accumulated in tumors or cancer sites. After boron captures neutrons, heavy particles α particles (helium nuclei) and high-energy Li nuclei are produced. , and then selectively kill tumor and cancer cells. Tumor radiotherapy is a treatment method that is more popular in the medical field today. Its principle is to use the biological effects of ionizing radiation to emit radiation to directly or indirectly cause tumor cell damage. Under the irradiation of large doses of ionizing radiation, biological organisms and cell macromolecules will cause damage, resulting in apoptosis or necrosis of tumor cells, which is a direct effect. The indirect effect is due to...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61P35/00A61K31/714
CPCA61K41/0095A61K31/714A61P35/00A61K2300/00
Inventor 张红夺金涛王雯王贵军金成福李仙洛
Owner 南京艾斯特医药科技有限公司
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