Poly (HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent and preparation method thereof

One-DOTA, nuclear magnetic resonance technology, applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agents, pharmaceutical formulations, preparations for in vivo tests, etc., can solve problems such as large dosage, short imaging window time, and low relaxation efficiency , to achieve the effect of increasing imaging effect, increasing passive targeting ability and prolonging cycle time

Inactive Publication Date: 2018-09-04
GANSU AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these small-molecule MRI contrast agents have disadvantages such

Method used

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  • Poly (HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent and preparation method thereof
  • Poly (HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent and preparation method thereof
  • Poly (HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent and preparation method thereof

Examples

Experimental program
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Example Embodiment

[0039] Example 1 Poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent, the structural formula of the contrast agent is as follows:

[0040] ;

[0041] In the formula: x = 90 mol%, y = 10 mol%.

[0042] The average molecular weight of the contrast agent is 20-40 kDa.

[0043] The preparation method of the poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent includes the following steps:

[0044] ⑴ Preparation of poly (HPMA) polymer:

[0045] will N -(2-Hydroxypropyl)methacrylamide (0.14g, 1.00 mmol) was first dissolved in 0.5 mL of DMSO at 25°C, then 0.5 mL of acetone was added, and stirred until dissolved. When cooled to room temperature, add 0.065 g ( 5%, wt) initiator azobisisobutyronitrile (AIBN), evacuated and filled with nitrogen for 3~5 cycles, sealed and reacted at 50℃ under nitrogen protection for 24 hours, precipitated and filtered through a mixture of acetone and ether, The precipitate A was obtained. After the precipitate A was dissolved in 1 mL of anhydrous...

Example Embodiment

[0060] Example 2 Poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent, the structural formula of the contrast agent is as follows:

[0061] ;

[0062] In the formula: x = 80 mol%, y = 20 mol%.

[0063] The average molecular weight of the contrast agent is 20-40kDa.

[0064] The preparation method of the poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent includes the following steps:

[0065] ⑴ Preparation of poly (HPMA) polymer:

[0066] will N -(2-Hydroxypropyl)methacrylamide (0.2 g, 1.4 mmol) was first dissolved in 1.0 mL of DMSO at 25°C, then 3.0 mL of acetone was added, and stirred until dissolved. When cooled to room temperature, add 0.016 g ( 8%, wt) initiator azobisisobutyronitrile (AIBN), evacuated and filled with nitrogen for 3~5 cycles, sealed and reacted at 55℃ under nitrogen protection for 22 h, precipitated and filtered through a mixture of acetone and ether, The precipitate A was obtained. After the precipitate A was dissolved in 1.0 mL of anhydrous met...

Example Embodiment

[0075] Example 3 Poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent, the structural formula of the contrast agent is as follows:

[0076] ;

[0077] In the formula: x = 10 mol%, y = 90 mol%.

[0078] The average molecular weight of the contrast agent is 20-40kDa.

[0079] The preparation method of the poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent includes the following steps:

[0080] ⑴ Preparation of poly (HPMA) polymer:

[0081] will N -(2-Hydroxypropyl)methacrylamide (0.4 g, 2.8 mmol) was first dissolved in 1.0 mL of DMSO at 25 ℃, then 3 mL of acetone was added, and stirred until dissolved. When cooled to room temperature, add 0.040 g ( 10 %, wt) initiator azobisisobutyronitrile (AIBN), evacuated and filled with nitrogen for 3~5 cycles, sealed and reacted at 60℃ for 20 h under nitrogen protection, precipitated and filtered through a mixture of acetone and ether, The precipitate A was obtained. After the precipitate A was dissolved in 1.0 mL of anhydrous met...

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Abstract

The invention relates to a Poly (HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent. The formula of the contrast agent is as follows (please see the specification for the formula). In the formula, x equals to 10-90 mol%, and y equals to 10-90 mol%. At the same time, the invention further discloses a preparation method of the contrast agent. The molecular weight of the contrast agent is less than a renal threshold, the molecular weight distribution is narrow, and the contrast agent can be eliminated through metabolism.

Description

technical field [0001] The invention relates to the technical field of polymer nuclear magnetic resonance contrast agents, in particular to a poly(HPMA)-DOTA-Gd nuclear magnetic resonance contrast agent and a preparation method thereof. Background technique [0002] In recent years, magnetic resonance imaging (MRI) has been widely used in clinical diagnosis. In order to improve the contrast between lesions and normal tissue signals, about 40% of diagnoses require the use of MRI contrast agents. The MRI contrast agents currently used clinically are mainly small molecule metal complexes, such as Magnevist, Dotarem, Omniscan, Gadovist, etc. However, these small-molecule MRI contrast agents have disadvantages such as low relaxation efficiency, short imaging window time, and large dosage. Macromolecules of small-molecule contrast agents can effectively overcome the above shortcomings and improve the performance of contrast agents. Therefore, the study of macromolecular contrast...

Claims

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Application Information

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IPC IPC(8): A61K49/10A61K49/08A61K47/58C08F120/58C08F8/42
CPCA61K49/108A61K47/58A61K49/085C08F8/42C08F120/58
Inventor 许卫兵龙海涛蒲陆梅
Owner GANSU AGRI UNIV
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