Enteric-coated pellet preparation of proton pump inhibitor and preparation method thereof

Abstract

The invention relate to an enteric-coated pellet preparation of proton pump inhibitor and a preparation method thereof. The enteric-coated pellet preparation of proton pump inhibitor provided by the invention is composed of a blank pellet core, a drug-loaded layer, isolating layers (I) and (II) and an enteric-coated layer, wherein both the drug-loaded layer and the isolating layer (I) contain water soluble inorganic bases, and the base used in the drug-loaded layer contains sodium hydroxide and another water soluble inorganic base which can form buffer with sodium hydroxide in a water solution and the pH of which is in an alkaline environment of 11-12 (excluding 11). The enteric-coated pellet of proton pump inhibitor provided by the invention successfully solves the technical problems of the existing enteric-coated pellet preparation of proton pump inhibitor, and is a superior preparation with high drug loading efficiency, good anti-acid effect, high release rate, good repeatability, high bioavailability and good stability.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for treating peptic ulcer disease and a preparation method thereof, in particular to a proton pump inhibitor enteric-coated pellet preparation and a preparation method thereof. Background technique [0002] Proton pump inhibitors (PPIs) are benzimidazole derivatives that act on H + / K-ATPase can inhibit the secretion of basic gastric acid and acid secretion caused by various stimuli such as histamine and eating. It has the characteristics of fast onset, strong effect and long duration. It is the first choice drug for the treatment of acid-related diseases Play an important role in the eradication of Helicobacter pylori (Helicobacter pylori, Hp) infection combined therapy. Currently marketed proton pump inhibitor drugs include: Omeprazole and its optically active substance esomeprazole, lansoprazole and its optically active substance dexlansoprazole (Dexlansoprazole) ), rabeprazole (rabeprazole), p...

AI Technical Summary

Problems solved by technology

Since the stability and preparation process of domestic proton pump inhibitors have not been resolved, the cost of most domestic manufacturers remains high, and proton pump inhibitors have not yet exerted their great potential in the treatment of peptic ulcer in my country (http : / / www.healthoo.com / A8 / 200410 / A8_20041025153456_184712.asp)

Since the micropill preparation of the present invention has only one isolation layer, and the pH value of the alkaline microenvironment of the active drug is only 7-10, the drug will migrate to the enteric layer in a short period of time, resulting in long-term storage stability problems of the drug

[0009] In summary, the existing technology is still unable to solve the stability problem of proton pump inhibitor enteric-coated preparations, and it is necessary to develop a kind of proton pump inhibitor enteric-coated microparticles with high drug loading efficiency, good stability and high bioavailability. pill preparation

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