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Esomeprazole medicated pellet and preparing method thereof

A technology of esomeprazole and esomeprazole magnesium, which is applied in the field of esomeprazole drug-containing pellet intermediates and its preparation, can solve the problem of large drug loading and waste in the mixing and granulation of coating pans Time, manpower and material resources, low production efficiency and other issues, to achieve significant economic benefits, improve efficiency, and high production efficiency

Active Publication Date: 2014-07-02
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Esomeprazole medicated pellet and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The esomeprazole drug-containing pellets of the present invention are mainly composed of 175g (mass percentage of 41.7%) of raw materials esomeprazole, 145g of mannitol (34.5% of mass percentage) and 100g of crospovidone (mass percentage is 23.8%); in addition, 150g of binder purified water (accounting for 35.7% of the total weight of the three main raw materials) is added.

[0031] Explanation: The purified water added in this example goes through the preparation method and is finally dried to obtain the product, and all the added purified water evaporates; therefore, the main raw materials in this example are composed of esomeprazole, mannitol and crospovidone.

[0032] The preparation method of esomeprazole drug-containing pellet of the present invention, its detailed steps are as follows:

[0033] a. First, the raw materials esomeprazole, crospovidone and mannitol are crushed through a 80-mesh sieve, sieved and placed in a stirring mixer to mix evenly. After mixing ...

Embodiment 2

[0035] Embodiment 2: basically the same as Embodiment 1, the difference is:

[0036]The esomeprazole drug-containing pellets of the present invention mainly consist of raw materials esomeprazole 145g (mass percentage is 34.5%), mannitol 173g (mass percentage is 41.2%) and crospovidone 102g (mass percentage is 24.3%); in addition, 165g of binder purified water (accounting for 39.3% of the total weight of the three main raw materials) is added.

[0037] Explanation: The purified water added in this example goes through the preparation method and is finally dried to obtain the product, and all the added purified water evaporates; therefore, the main raw materials in this example are composed of esomeprazole, mannitol and crospovidone.

[0038] The preparation method of the esomeprazole drug-containing pellets of the present invention is the same as in Example 1.

Embodiment 3

[0039] Embodiment 3: basically the same as Embodiment 1, the difference is:

[0040] The esomeprazole drug-containing pellets of the present invention mainly consist of raw materials esomeprazole 110g (mass percentage is 26.2%), mannitol 210g (mass percentage is 50%) and crospovidone 100g (mass percentage is 23.8%); in addition, 146g of binder purified water (accounting for 34.8% of the total weight of the three main raw materials) is added.

[0041] Explanation: The purified water added in this example goes through the preparation method and is finally dried to obtain the product, and all the added purified water evaporates; therefore, the main raw materials in this example are composed of esomeprazole, mannitol and crospovidone.

[0042] The preparation method of the esomeprazole drug-containing pellets of the present invention is the same as in Example 1.

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Abstract

The invention discloses a drug-containing esomeprazole pellet and a preparation method thereof. Expressed in percent by weight, the esomeprazole drug-containing pellets mainly consist of 25-50% of raw materials esomeprazole and its derivatives, 20-50% of mannitol and 5-30% of crospovidone. % composition; In addition, it also contains pharmaceutically acceptable pharmaceutical excipients. The invention carries out proportioning according to the raw material composition of the esomeprazole drug-containing pellets, and utilizes an extrusion-spheronization preparation method to produce the product of the invention, the esomeprazole drug-containing pellets. Compared with the prior art, the technical scheme of the present invention is used to prepare esomeprazole drug-containing pellets, which improves efficiency and avoids wasting a lot of time, manpower and material resources; and the method is simple, and the obtained product preparation intermediate has the The advantages of stability and high reproducibility.

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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4439A61K47/32A61K47/36A61K47/38A61P1/04
Inventor 任逢晓张胜华邬向东
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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