Compound oral solid preparation containing clopidogrel and preparation method thereof

Abstract

The invention relates to a compound oral solid preparation containing clopidogrel. The compound oral solid preparation comprises a sheet core and an outer layer, wherein the sheet core contains acetylsalicylic acid and includes two coating layers, the two coating layers are an internal gastric juice soluble coating layer and an external enteric coating layer, and the outer layer contains clopidogrel and its officinal salt and contains KG1000OR KG802 microcrystalline cellulose. The compound oral solid preparation can achieve the advantages that the outer layer containing the clopidogrel and its officinal salt is rapidly released in the stomach and the sheet core containing acetylsalicylic acid can be released in the intestinal tract. The compound oral solid preparation has the advantages that a production process of the preparation includes few steps, a tableting process is larger in parameter range and is easy to control, the production efficiency is high, few degradation impurities after long-term storage are produced, the stability is better, and the safety in clinic use is better.

Description

technical field [0001] The invention relates to a solid preparation and a preparation method thereof, which contains acetylsalicylic acid or a medicinal salt thereof and clopidogrel or a medicinal salt thereof, and belongs to the technical field of medicine. Background technique [0002] Cardiovascular disease is the main cause of human death. Cardiovascular disease has been the leading cause of death among residents since 1990 in my country. The 2008 "Statistical Bulletin on China's Health Development" shows that the number of deaths caused by cardiovascular diseases has accounted for 40.27% of the total number of deaths in the country, and the number of deaths among young adults aged 35 to 54 has increased most rapidly. Therefore, controlling the spread of cardiovascular diseases has become the top priority for improving people's health in the 21st century. [0003] Thromboembolic diseases are very common clinically. Atherosclerosis is a common and frequently-occurring...

AI Technical Summary

Problems solved by technology

Once the sticky punch occurs, the weight of the tablet will drop, and the loading and appearance of the solid preparation will be unqualified.

The sticking problem of clopidogrel solid preparation tableting step has been documented in the literature. The literature shows that clopidogrel has strong static electricity and is easy to be adsorbed on the punch, causing sticking.

Clopidogrel has poor compatibility with commonly used lubricants (such as magnesium stearate) with less dosage and better lubricating effect (magnesium stearate will cause the degradation of clopidogrel), so we can only choose lubricants with relatively good lubricating effect Weak but compatible other lubricants (such as hydrogenated castor oil)

Lubricants have a great influence on the dissolution rate of clopidogrel, and the dissolution rate decreases significantly when the dosage is high. Therefore, in order to reduce the impact on the dissolution rate, the amount of lubricant added should be reduced as much as possible, and insufficient lubricants often lead to sticking.

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