Aspirin pulsed release pellets, its preparation and preparation method thereof

Abstract

The invention discloses aspirin pulsed release pellets, its preparation and a preparation method thereof. The pellets comprise blank pellets, an aspirin-containing drug layer, an isolation layer, a regulation releasing layer and a protective layer. The regulation releasing layer contains polyprotic acid and / or its salt, anionic polymer salt, a plasticizer and an antiadherent. The anionic polymer salt is prepared by the following method: dissolving an enteric material, and using alkali to neutralize to a pH value greater than the enteric material dissolution pH value 0.1-3. The protective layer contains the enteric material, the plasticizer and the antiadherent. The enteric material is any one material selected from: an enteric material dissolved at pH value of 4.5-5.5 to prepare pellets I; an enteric material dissolved at pH value of 6.0-6.5 to prepare pellets II; or an enteric material dissolved at pH value of 7.0-8.0 to prepare pellets III. According to the preparation, local drug concentration will not be high, accumulation of the drug inside the body can be reduced, patient compliance can be improved, and stability inside the body can be raised. Therefore, bioavailability and the antithrombotic effect are raised.

Description

technical field [0001] The invention relates to an aspirin pulse release pellet, its preparation and a preparation method. Background technique [0002] Aspirin is a commonly used drug for cardiovascular diseases and has a huge consumption. At present, in our country, the incidence of cardiovascular and cerebrovascular diseases is increasing year by year. Among the drug prevention measures used, aspirin has shown excellent effects in primary and secondary prevention, which can reduce the incidence and death of myocardial infarction and stroke. risk. Aspirin not only gets attention in routine application, but also gradually expands its scope of application. On October 22, 2010, the famous medical journal "The Lancet" reported the case analysis of 18 years of British doctors, and found that long-term use of low-dose aspirin can reduce the chance of colon cancer by 24%, and the chance of dying from colon cancer by 35%; The 2006 AHA / ASA guidelines for the primary prevention o...

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is to overcome the problem that aspirin is easily hydrolyzed and unstable and causes gastrointestinal bleeding, while in the prior art, oral chewable tablets have the problem of stimulating the stomach and upper gastrointestinal tract, and enteric-coated tablets have excessive local concentration. High problem, prolonged dissolution time of sustained-release preparations in the body leads to increased acetyl hydrolysis and enzymatic hydrolysis, which reduces the antithrombotic efficacy and other defects. It provides a local drug concentration that will not be too high, can reduce the accumulation of drugs in the body, and improve the quality of patients. Compliant aspirin pulse release pellets, aspirin pulse release formulation and preparation method thereof

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