Magnetic resonance imaging contrast using arabinogalactan as carrier
A technology of arabinogalactan and magnetic resonance imaging, which is applied in preparations for in vivo tests and pharmaceutical formulations, can solve problems such as easy hydrolysis of ester bonds, reduced relaxation efficiency of contrast agents, and increased toxicity
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Embodiment 1
[0053] Preparation of arabinogalactan by ethylenediamine-modified gadolinium diethylenetriaminepentaacetate complex (Gd-DTPA-CMAGA) contrast agent for magnetic resonance imaging
[0054] a) 1g of DTPA was dissolved in a mixed solution of 4.8ml of acetonitrile and 5.4ml of triethylamine, and the temperature was raised to 55°C. After DTPA was completely dissolved, 0.371g of DCC and 0.207g of HONSu were added at the same time, stirred at room temperature for 1.5h, and filtered to obtain DTPA- ONSu solution.
[0055] b) Dissolve 6g of arabinogalactan in 50ml of 6mol / L NaOH solution at 0°C, then add 12.3g of monochloroacetic acid, stir at 60°C for 50min, precipitate with methanol, filter, and dry in vacuo to obtain carboxymethyl sylated arabinogalactan.
[0056] c) Dissolve 6 g of carboxymethylated arabinogalactan in deionized water, adjust the pH to 3 with 1 mol / L HCl, add 9.3 g of EEDQ methanol solution dropwise, and add 12.5 ml of ethylenediamine dropwise while stirring, Stir ...
Embodiment 2
[0060] Preparation of Arabinogalactan as a Contrast Agent for Magnetic Resonance Imaging via Manganese Diethylenetriaminepentaacetate Complex Modified with Ethylenediamine
[0061] a) Step a) in the same example 1.
[0062] b) Same as step b) in Example 1.
[0063] c) Same as step c) in Example 1.
[0064] d) Same as step d) in Example 1.
[0065] e) Dissolve 0.5g of the DTPA macromolecule ligand modified by arabinogalactan in d in 10ml of deionized water, add 3ml of 0.2mol / L MnCl 2 Solution (more than 20% of the ratio), adjust the pH value to 5.7 with 1mol / L NaOH, stir overnight at room temperature, dialyze, exchange the aqueous solution outside the dialysis bag until its longitudinal relaxation time T 1 More than 3000ms, lyophilized to obtain arabinogalactan modified by ethylenediamine diethylenetriaminepentaacetic acid manganese complex magnetic resonance imaging contrast agent.
Embodiment 3
[0067] Preparation of arabinogalactan as a contrast agent for magnetic resonance imaging via ethylenediamine-modified gadolinium ethylenediaminetetraacetate complexes
[0068] a) Dissolve 0.743g EDTA in a mixed solution of 4.8ml acetonitrile and 5.4ml triethylamine, raise the temperature to 55°C, after EDTA is completely dissolved, add 0.371g DCC and 0.207g HONSu at the same time, stir at room temperature for 1.5h, filter to obtain EDTA- ONSu solution.
[0069] b) Same as step b) in Example 1.
[0070] c) Same as step c) in Example 1.
[0071]d) Dissolve 1 g of the aminated arabinogalactan in c in 25 ml of deionized water, add 10 ml of the EDTA-ONSu solution in step a, adjust the pH to 10 with 6 mol / L NaOH, stir at room temperature for 24 hours, and pump under reduced pressure Acetonitrile was removed, dialyzed for 5 days, the solution in the osmotic bag was rotary evaporated at 55°C to a small volume, and freeze-dried to obtain the arabinogalactan-modified EDTA macromolecul...
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