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Functionalization mesoporous molecular sieve used in adsorption and sustained-release alkaline drug method

A technology of mesoporous molecular sieves and basic drugs, applied in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve problems such as few reports on research, and achieve the effect of slowing down the release rate

Inactive Publication Date: 2008-09-10
SHANXI INST OF COAL CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, in the research on mesoporous molecular sieves, a new type of drug carrier, people mostly focus on acidic drugs such as ibuprofen, captopril, and bovine serum albumin, while famotidine, citrate, etc. There are few reports on commonly used basic drugs such as metidine

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Synthesis of carboxyl-functionalized mesoporous molecular sieves: according to the method described in the literature Phys.Chem.Chem.Phys. (Physical Chemistry Chemical Physics) 2004, 6, 2461-2467. First, add 4.0g of surfactant P123 to 120mL of 2.0M HCl in 2.0M, stir until P123 is completely dissolved, then add 6.0mL of inorganic silicon source tetraethyl orthosilicate and 4.0mL of organosilane containing cyano groups such as (CH 3 CH 2 O) 3 SiCH 2 CH 2 CN, aged at 40°C after stirring for 24h. After filtering, the obtained solid was treated with dilute sulfuric acid solution to obtain a functionalized mesoporous molecular sieve with a carboxyl content of 40.0% (mole percent, the same below). The specific surface of the obtained molecular sieve is 430m 2 / g, the pore size is 4.3nm.

[0022] Drug adsorption: Add 1.0 g of amoxicillin to 200 mL of water to make the concentration of amoxicillin 5.0 mg / mL to obtain solution A1. Take 0.5 g of a functionalized molecular s...

Embodiment 2

[0026] Synthesis of carboxyl-functionalized mesoporous molecular sieves: according to the method described in the literature Chem. Mater. (Chemical Materials) 1999, 11, 3285-3295. First, add 2.0g surfactant CTAB to 240mL water, add 1.0g NaOH at the same time, stir until CTAB is completely dissolved, then add 9.5mL inorganic silicon source such as ethyl orthosilicate and 0.5mL organosilane containing cyano group such as (CH 3 CH 2 O) 3 SiCH 2 CH 2 CN, aged after stirring at room temperature for 24h. After filtering, the obtained solid was treated with dilute sulfuric acid solution to obtain a functionalized mesoporous molecular sieve with a carboxyl content of 5.0%. The specific surface of the obtained molecular sieve is 1250m 2 / g, the pore size is 3.0nm.

[0027] Drug adsorption: add 10.0 g of purified urea into 100 mL of chloroform, so that the concentration of the purified urea is 100.0 mg / mL, and obtain solution A2. Take 2.0 g of a functionalized molecular sieve sam...

Embodiment 3

[0031]Synthesis of carboxyl-functionalized mesoporous molecular sieves: according to the method described in the document Micropor.Mesopor.Mat. (microporous mesoporous material) 2004,72,33-42, get 2.0g MCM-48 sample and 3.0mL (CH 3 O) 3 SiCH 2 CH 2 CH 2 CH 2 CN was added to 100mL toluene and refluxed for 12.0h. The resulting solid was filtered and treated with dilute sulfuric acid to give carboxyl functionalized MCM-41. The carboxyl content in the sample is 21.0%, and the specific surface of the molecular sieve is 1100m 2 / g, the pore size is 3.1nm.

[0032] Drug adsorption: Add 10.0 g of cyanamide to 100 mL of water to make the concentration of cyanamide to 100.0 mg / mL to obtain solution A3. Take 2.0 g of a functionalized molecular sieve sample with a carboxyl content of 21.0%, add it to solution A3, and seal it. After stirring at room temperature for 3 days, it was filtered, and the solid obtained by filtration was dried at room temperature. That is, sample B3 was o...

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Abstract

The invention relates to a functionalized mesoporous molecular sieve and a method to use the functionalized mesoporous molecular sieve for adsorption and controlled release of alkaline drugs, namely, an alkaline drug is added to water or organic solution to obtain solution A, ensuring that the concentration of the alkaline drug is 1.0-100.0 mg / mL; the functionalized mesoporous molecular sieve is added to the solution A, ensuring that the functionalized mesoporous molecular sieve / solution A is equal to 0.1-0.5g / 10.0-500.0 mL, stirred for 0.5 to 3 days and then filtered, the obtained solid is dried, thus obtaining functionalized mesoporous molecular sieve B capable of absorbing drugs; -CH3 group is grafted on the surface of the unctionalized mesoporous molecular sieve B capable of absorbing drugs by adopting a post-processing method, so as to obtain double-functionalized solid pulvis with absorbed alkaline drug. The functionalized mesoporous molecular sieve of the invention has the advantages of well-distributed drug, large drug loading capacity, availability for convenient adjusting and long time of drug release.

Description

technical field [0001] The invention relates to the application of an organic functionalized mesoporous molecular sieve in the adsorption and sustained release of basic drugs. technical background [0002] Compared with the traditional drug delivery technology, drug sustained release technology has the advantages of reducing the toxic and side effects of drugs on the human body, improving the efficacy of drugs, and increasing the comfort of patients when taking medication. Therefore, the research on drug sustained release technology not only has important therapeutic value, but also has great Has commercial potential. Silicon-based mesoporous molecular sieves have become a new type of carrier in the field of drug sustained release because of their high specific surface area, large pore volume, uniform distribution and continuously adjustable pore structure within a certain range, and good biocompatibility. [M. Vallet-Regí, A. Rámila, R.P. del Real, J. Pérez-Pariente, Chem. ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/22A61K47/02A61K47/12A61K47/20A61K31/426A61K31/43A61K31/44A61K31/635A61P31/04A61P31/06A61P1/04
Inventor 孙予罕徐武军徐耀吴东
Owner SHANXI INST OF COAL CHEM CHINESE ACAD OF SCI
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