Preparation method of aspirin/chitosan modified carbon nanotube administration system

A carbon nanotube and aspirin technology, which is applied in the field of preparation of aspirin/chitosan modified carbon nanotube drug delivery system, can solve the problem of not completely inhibiting thromboxane platelet aggregation, hindering the wide application of aspirin, reducing the incidence of gastrointestinal bleeding, etc. problems, to achieve good research and development application prospects, good economic development potential, and the effect of a dense drug delivery system

Inactive Publication Date: 2019-07-30
QINGDAO UNIV OF SCI & TECH
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  • Summary
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  • Claims
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Problems solved by technology

Since the discovery in the 1960s that the aromatic compound Aspirin (Asp) has a significant anti-platelet aggregation effect, it was used in the treatment and prevention of AMI in the 1970s. Evidence-based medical research has proved that aspirin is effective in the prevention and treatment of stroke, angina pectoris, and myocardial infarction. It is an effective drug for diseases such as senile dementia and migraine, which can reduce thrombosis and embolism events in the heart, brain and peripheral blood vessels by 25%. It has a stimulating effect on the gastrointestinal mucosa, especially for patients who need to take medicine for a long time. widely used
In addition, many experimental studies in recent years have found that some patients cannot completely inhibit the generation of thromboxane and platelet aggregation even though they take conventional doses or even larger doses of aspirin, especially for patients with symptomatic arterial thrombosis, aspirin cannot prevent at least 75% The occurrence of serious vascular events, that is, the phenomenon known as aspirin resistance (aspirin resistance, AR) or aspirin failure (aspirin failure), for this reason, a lot of research work has been tried at home and abroad, aiming at improving the properties of aspirin, especially in this aspect in recent years There are many research reports, the basic point of which is to focus on the release characteristics of aspirin under the traditional slow-release materials or the formation of aspirin and small molecular substances into salts and esters, but most of them are limited to in vitro studies, and the clinical data are insufficient. The effect is inconclusive
For the countermeasures of AR, it has been reported in the literature that increasing the dose of aspirin can reduce the occurrence of some AR, but due to secondary bleeding and gastrointestinal reactions, the treatment is often discontinued

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  • Preparation method of aspirin/chitosan modified carbon nanotube administration system
  • Preparation method of aspirin/chitosan modified carbon nanotube administration system
  • Preparation method of aspirin/chitosan modified carbon nanotube administration system

Examples

Experimental program
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Effect test

Embodiment 1

[0032]First mix concentrated sulfuric acid and concentrated nitric acid in a volume ratio of 1:3, and then add multi-walled carbon nanotubes to the mixed acid with a mass / volume ratio of 5:1 under ultrasonic conditions. In the process, by controlling the ultrasonic parameters (ultrasonic power is 10w, ultrasonic time is 2s, interval time is 4s, and the number of ultrasonic waves is 60 times), the reaction temperature is 20°C, and the reaction time is 1h, the carboxylated multi-walled carbon nanotubes, concentrated sulfuric acid and concentrated Mixed acid of nitric acid, washed with water, filtered, and freeze-dried at -20°C for 24 hours, the product obtained is the active intermediate of multi-walled carbon nanotubes. Under the condition of ultrasound (ultrasonic power is 10w, ultrasonic time is 2s, interval time is 4s, and the number of ultrasonic waves is 60 times), the active intermediate of multi-walled carbon nanotubes is dissolved in deionized water containing catalyst E...

Embodiment 2

[0040] First mix concentrated sulfuric acid and concentrated nitric acid in a volume ratio of 3:1, and then add single-walled carbon nanotubes to the mixed acid with a mass / volume ratio of 1:5 under ultrasonic conditions. In the process, by controlling the ultrasonic parameters (ultrasonic power is 50w, ultrasonic time is 4s, interval time is 7s, and the number of ultrasonic waves is 60 times), the reaction temperature is 50°C, and the reaction time is 1h, the carboxylated single-walled carbon nanotubes, concentrated sulfuric acid and concentrated Mixed acid of nitric acid, washed with water, filtered, and freeze-dried at -30°C for 36 hours, the product obtained is the active intermediate of single-walled carbon nanotubes. Under the condition of ultrasound (ultrasonic power is 50w, ultrasonic time 4s, interval time 7s, ultrasonic times 60 times), the single-walled carbon nanotube active intermediate is dissolved in deionized water containing catalyst DCC and HOBt with a mass ra...

Embodiment 3

[0042] First mix concentrated sulfuric acid and concentrated nitric acid in a volume ratio of 1:1, and then add multi-walled carbon nanotubes to the mixed acid with a mass / volume ratio of 2:3 under ultrasonic conditions. Among them, by controlling the ultrasonic parameters (ultrasonic power 100w, ultrasonic time 8S, interval time 10S, ultrasonic frequency 100 times), reaction temperature 100°C, and reaction time 5h, carboxylated multi-walled carbon nanotubes, concentrated sulfuric acid and concentrated nitric acid were obtained. The mixed acid was washed with water, filtered, and freeze-dried at -40°C for 48 hours to obtain the product, which is the active intermediate of multi-walled carbon nanotubes. Under the condition of ultrasonic ((ultrasonic power 100w, ultrasonic time 8S, interval time 10S, ultrasonic times 100 times), the active intermediate of multi-walled carbon nanotubes was dissolved in deionized water containing catalyst DIC and DMAP with a mass ratio of 1:3, Pre...

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Abstract

The invention discloses a preparation method of an aspirin/chitosan modified carbon nanotube administration system, which specifically comprises the following steps of: (1) pre-fabricating a carboxylic carbon nanotube, concentrated sulfuric acid and concentrated nitric acid mixed acid, and washing, filtering and freeze-drying to prepare a carbon nanotube active intermediate; (2) prefabricating a mixed solution of the chitosan/carbon nanotube and a catalyst, adding absolute ethyl alcohol, centrifuging and freeze-drying to obtain chitosan/carbon nanotube freeze-dried powder; (3) dissolving the chitosan/carbon nanotube freeze-dried powder in deionized water solution, adding aspirin for reaction, adding absolute ethyl alcohol, centrifuging, and freeze-drying to obtain an aspirin-chitosan/carbon nanotube solid product. A chemical modification/non-covalent modification/pi-pi conjugate adsorption method is used, as a result, the administration system is more compact and the performance is more stable. The preparation method has the advantages of simple and stable operation, low manufacturing cost and the like, and has good research, development and application prospects.

Description

technical field [0001] The invention belongs to the technical field of new drug research and development, and in particular relates to a preparation method of an aspirin / chitosan modified carbon nanotube drug delivery system. Background technique [0002] The morbidity and mortality of acute myocardial infarction (AMI) and thromboembolic diseases are very high, and the research on drugs to prevent and treat these diseases has attracted worldwide attention. Since the discovery in the 1960s that the aromatic compound Aspirin (Asp) has a significant anti-platelet aggregation effect, it was used in the treatment and prevention of AMI in the 1970s. Evidence-based medical research has proved that aspirin is effective in the prevention and treatment of stroke, angina pectoris, and myocardial infarction. It is an effective drug for diseases such as senile dementia and migraine, which can reduce thrombosis and embolism events in the heart, brain and peripheral blood vessels by 25%. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/61A61K47/52A61K31/616A61P9/10
CPCA61K31/616A61K47/61A61K47/6923A61P9/10
Inventor 宋益民罗尚满华潘爱红贾喜乐李媛媛张航王慧茹周莉
Owner QINGDAO UNIV OF SCI & TECH
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