Esomeprazole medicated pellet and preparing method thereof

Abstract

The invention discloses an esomeprazole medicated pellet and a preparing method of the esomeprazole medicated pellet. The esomeprazole medicated pellet is mainly prepared from 25-50% of esomeprazole raw material and ramification of the esomeprazole raw material, 20-50% of mannitol and 5-30% of polyvinylpolypyrrolidone according to weight percentage; and in addition, pharmaceutic adjuvant acceptable pharmaceutically is also contained. The ingredients of the esomeprazole medicated pellet are proportioned, and the esomeprazole medicated pellet product can be prepared by virtue of an extruding-rolling preparing method. Compared with the prior art, the technical scheme provided by the invention has the advantages that the efficiency is greatly improved, and waste of a large amount of time, manpower and material resources are avoided; and the method is simple, and the midbody of the obtained product preparation has the advantages of stable medicine, high reproducibility and the like.

Description

technical field [0001] The invention relates to pharmaceutical preparation intermediates and preparation methods thereof in the field of pharmacy, in particular to a drug-containing micropill with esomeprazole as the main ingredient and a preparation method thereof, that is, a drug-containing micropill of esomeprazole Pill intermediate and preparation method thereof. Background technique [0002] Esomeprazole is the (S)-isomer of omeprazole, a newer proton pump inhibitor widely used in clinical practice, and its chemical name is 5-methoxy-2-((S )-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl)-1H-benzimidazole, the structural formula is as follows: [0003] [0004] The mechanism of action of esomeprazole is the same as that of omeprazole, that is, it is protonated under acidic conditions, and esomeprazole is transformed into an inhibitor of H + / K + -ATPase active compound sulfenamide, rapidly reacts with H + / K + - The sulfhydryl group of cysteine ​​on the ATP...

AI Technical Summary

Problems solved by technology

Compared with several commonly used methods, extrusion-spheronization has large drug loading, high hardness, good roundness, good continuity, high output and efficiency; coating pan mixing granulation has large drug loading, roundness Good wholeness and low hardness; fluidized bed and centrifugal coating granulation have good roundness, low hardness, low drug loading, and low production efficiency; extrusion-spheronization method is used in the preparation process of pellets has obvious advantages

[0007] However, the extrusion-spheronization method is often not adopted due to excipients, such as the original product Esomeprazole enteric-coated tablets NEXIUM TM Even if fluidized bed coating is used to prepare drug-containing pellet cores, domestic marketed varieties are basically prepared by fluidized bed coating to prepare drug-containing pellet cores. For this variety, the drug loading capacity is large, and fluidized bed Coating and preparing drug-containing pellet cores often requires a lot of wasted time, manpower and material resources

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