Enteric-coated micropellet containing esomeprazole magnesium

Abstract

The invention relates to an enteric-coated micropellet containing esomeprazole magnesium. The enteric-coated micropellet comprises an inert pellet core, a medicament-loaded layer, an isolation layer and an enteric-coated layer, wherein the enteric-coated layer contains a methacrylic acid / ethyl acrylate 1: 1 copolymer, glyceryl monostearate, Tween 80 and talcum powder, wherein the methacrylic acid / ethyl acrylate 1: 1 copolymer is preferably Eudragit L30D-55. The enteric-coated micropellet containing esomeprazole magnesium, provided by the invention, can give consideration to acid resistance, release rate and stability of a product for a long time in the placement process, can meet or exceed existing preparation quality standards; and furthermore, the enteric-coated micropellet is prepared by simple process steps, is suitable for a relatively large pellet core (0.3mm-1mm), has the characteristic of low production cost, and is more suitable for large-scale industrialized production.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to an enteric-coated pellet containing esomeprazole magnesium. Background technique [0002] Esomeprazole (Esomeprazole, 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl-1H -benzimidazole) is a new generation of proton pump inhibitors (PPIs) that inhibit H + / K + -ATPase to reduce gastric acid secretion and prevent the formation of gastric acid. Esomeprazole is the L-isomer of the first generation PPI omeprazole. The effect is better, there is no obvious acid breakthrough phenomenon at night, 24 hours of continuous acid suppression, less individual differences, less interaction with other drugs and other advantages, it is the current treatment of acid-related diseases, such as peptic ulcer, gastroesophageal reflux disease , Zollinger-Ellison syndrome and other drugs of choice. [0003] The original manufacturer of esomeprazole magnesium salt is AstraZeneca, a Br...

AI Technical Summary

Problems solved by technology

Some of the methods disclosed in the prior art, such as the method disclosed in the above-mentioned Chinese patent application CN103127026A, can achieve a loss of less than 10% in the acid for 2 hours in long-term placement, and a release rate higher than 75% in the buffer for 30 minutes, and Esomeprazole magnesium enteric-coated pellets with a total impurity content of less than 2%, but because its acid resistance, release rate and other indicators are far lower than the measured values ​​of the original research product, its onset time and clinical efficacy are different from those of the original research product. Compared with listed products, there is still a certain gap

However, the prescription of the original product on the market is only suitable for smaller pellet cores (0.1mm to 0.3mm). Compared with large pellet cores, the liquid droplets of small pellet cores are not easy to spread during coating spraying, which may easily lead to pill adhesion, making production difficult; at the same time , the specific surface area of ​​the small pellet core is large, and it is easy to cause problems such as large amount of coating material and high production cost.

[0010] In view of the fact that it is difficult for the existing technology to provide esomeprazole magnesium enteric-coated pellet capsules that can meet the loss of less than 10% in 2h in acid, the release rate of buffer solution is higher than 75% in 30min, and the impurity content is lower than 2%; or prepare Although the prepared preparations can meet the above-mentioned quality standards, they cannot maintain this characteristic during the storage period; or although they can meet the above-mentioned quality standards during the storage period, there are problems such as the production process is too complicated, the production cycle is long, and the cost is too high. It is very necessary to develop a kind of esomeprazole magnesium enteric-coated pellet capsule that can take into account product acid resistance, release degree and stability for a long time in the placing process, and reach high-quality standards as far as possible, and the capsule can meet and It is superior to the existing preparation quality standards, and the process is simple, and it can be applied to larger pellet cores (0.3mm-1mm), which makes the pellets less likely to stick when coating, and is more suitable for large-scale industrial production; at the same time, the amount of coating material less, less expensive to produce

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