Preparation method for nano-sized zirconium-based cation metal organic framework (Zr-MOFs) materials carrying anionic medicine

A metal-organic framework and anionic technology, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of small loading, micron-level size, uncontrolled release, etc. Problems, to achieve the effect of large drug loading and increase loading

CN105999280AActive Publication Date: 2016-10-12ZHEJIANG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Publication Date
2016-10-12

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Abstract

The invention discloses a preparation method for nano-sized zirconium-based cation metal organic framework (Zr-MOFs) materials carrying an anionic medicine. According to the method, firstly, cation functionalized Zr-MOFs are obtained, then, the anionic medicine is loaded to the Zr-MOFs, and the releasing effect of the Zr-MOFs is controlled through pH. After an n-donor ligand of the synthesized Zr-MOFs materials is subjected to cationization, due to the coulomb force, very strong acting force is exerted to the anionic medicine, a large loading capacity can be reached, and the nano-sized Zr-MOFs materials carrying the anionic medicine have a pH controlled-release effect in the medicine slow-release process. Thus, the materials have potential application prospects in the aspects of anionic medicine loading and controlled releasing.
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Description

technical field

[0001] The invention belongs to the field of preparation and application of drug loading and controlled release systems, in particular to a method for preparing nanoscale zirconium-based cationic metal organic framework materials Drug@Zr-MOFs loaded with anionic drugs, which can be used for anionic drugs loading and controlled release. Background technique

[0002] In the field of pharmacy, diclofenac sodium is a non-steroidal anti-inflammatory analgesic with excellent efficacy, and is often used to treat postoperative infection. However, the half-life of diclofenac sodium in the body is only 1 to 2 hours, and the extremely high blood concentration will cause many adverse reactions in the human body, such as gastrointestinal ulcers, renal failure and dermatitis. There are many other drugs that have problems such as too short half-life, instability in the body, and excessive blood drug concentration can cause adverse reactions in the body. Therefore, the deve...

Examples

Embodiment 1

[0030] (1) ZrCl is mixed with a reactor 4 (11.7mg, 0.05mmol) and N-containing organic ligand pyridine-2,5-dicarboxylic acid (8.35mg, 0.05mmol) were uniformly dissolved in N,N-dimethylformamide (DMF, 18mL), and then added A small amount of glacial acetic acid (2mL, 35mmol), ultrasonically oscillated for 10min, and placed in an oven at 120°C for 24h;

[0031] (2) Centrifuge after cooling at room temperature, disperse the precipitate in DMF (10mL), repeat centrifugal washing 3 times, after centrifugation, disperse the sample evenly in acetone (10mL), let stand for 24h, add acetone (10mL) again after centrifugation ), repeating for three days, the obtained precipitate is a Zr-MOFs material that has not been cationized;

[0032] (3) Take the Zr-MOFs material synthesized above and dry it in a vacuum oven at 60°C for 12 hours;

[0033] (4) Use a glass bottle to disperse the dried Zr-MOFs material (700mg) in CHCl 3 (15mL), then added dropwise methyl trifluoromethanesulfonate (4.44m...

Embodiment 2

[0040] (1) ZrCl is mixed with a reactor 4 (11.7mg, 0.05mmol) and N-containing organic ligand 2,2'-bipyridine-5,5'-dicarboxylic acid (24.4mg, 0.1mmol) were uniformly dissolved in N,N-dimethylformamide (DMF , 18mL), a small amount of glacial acetic acid (2.29mL, 40mmol) was added, ultrasonically oscillated for 10min, and placed in an oven at 120°C for 24h;

[0041] (2) Centrifuge after cooling at room temperature, disperse the precipitate in DMF (10mL), repeat centrifugal washing 3 times, after centrifugation, disperse the sample evenly in acetone (10mL), let stand for 24h, add acetone (10mL) again after centrifugation ), repeating for three days, the obtained precipitate is a Zr-MOFs material that has not been cationized;

[0042] (3) Take the Zr-MOFs material synthesized above and dry it in a vacuum oven at 60°C for 12 hours;

[0043] (4) Use a glass bottle to disperse the dried Zr-MOFs material (700mg) in CHCl 3 (15mL), then added dropwise methyl trifluoromethanesulfonate ...

Embodiment 3

[0048] (1) ZrCl is mixed with a reactor 4 (11.7mg, 0.05mmol) and N-containing organic ligand 4,4'-(pyridine-2,5-ylidene)benzoic acid (44.3mg, 0.15mmol) were uniformly dissolved in N,N-dimethylformamide ( DMF, 18mL), then add a small amount of glacial acetic acid (2.86mL, 50mmol), ultrasonically oscillate for 10min, and put it in an oven at 120°C for 24h;

[0049] (2) Centrifuge after cooling at room temperature, disperse the precipitate in DMF (10mL), repeat centrifugal washing 5 times, after centrifugation, disperse the sample evenly in acetone (10mL), let stand for 24h, add acetone (10mL) again after centrifugation ), repeated for three days, and the obtained precipitate was a Zr-MOFs material that had not been cationized;

[0050] (3) Take the Zr-MOFs material synthesized above and dry it in a vacuum oven at 60°C for 12 hours;

[0051] (4) Use a glass bottle to disperse the dried Zr-MOFs material (700mg) in CHCl 3 (15mL), then added dropwise methyl trifluoromethanesulfon...