A kind of montelukast sodium granule composition and preparation method thereof

Abstract

The invention provides a montelukast sodium particle composition and a preparing method thereof. The particles are prepared from montelukast sodium, a filling agent, cross-linked polyvinylpolypyrrolidone, copovidone, magnesium stearate and purified water; with combination of self properties of montelukast sodium and the characteristics of the preparation, the synergistic effect of cross-linked polyvinylpolypyrrolidone and copovidone is fully utilized, a dissolution release behavior is effectively guaranteed with hydrogen-bond interaction in vitro and in vivo, the bioavailability is guaranteed,and the taking safety is increased. At the same time, the invention also discloses a preparing process of the montelukast sodium particles; the preparation process is simple and easy to operate, andis suitable for industrialized production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a montelukast sodium granule composition and a preparation method thereof. Background technique [0002] Montelukast (Montelukast) is an anti-asthma drug developed by Merck of the United States. It is a selective leukotriene receptor antagonist. It was approved by the U.S. FDA in February 1998. Its trade name is "Singulair", and its formulations include: Film-coated tablets, chewable tablets and granules, with specifications of 10mg, 5mg and 4mg respectively, were subsequently launched in 71 countries including Canada, Italy, Spain, Sweden, Switzerland, Germany and France. In the late 1990s, Merck’s montelukast tablets began to enter the Chinese market, with the trade name “Singulair”, and then its oral granules (Guoyao Zhunzi J20120044) and chewable tablets were also listed in my country one after another. Kastina granules are suitable for the prevention and ...

AI Technical Summary

Problems solved by technology

[0005] Patent WO2003035036A1 discloses the prescription and preparation process of commercially available montelukast sodium granules. The fluidized bed granulation method is adopted, and the prepared granules are loose to further improve the dissolution rate of montelukast sodium and ensure the bioavailability in vivo. However, montelukast sodium easily reacts with oxygen under high temperature conditions, and the oxidized impurities (sulfoxide) increase significantly; in order to reduce the oxidized impurities, patent WO2009153305A2 uses nitrogen as the carrier gas of the fluidized bed to avoid contact between particles and oxygen. Fewer oxidized impurities, but higher requirements for equipment, difficult to achieve with domestic existing technology

[0006] Patent CN201510747141.4 discloses a montelukast sodium granule composition and its preparation method, using lauryl dimethyl amine oxide and ammonium glycyrrhizinate as protective agents, although lauryl dimethyl amine oxide It can solubilize the main drug and has low physiological toxicity, but as a synthetic surfactant, it still has potential safety hazards for the human body, especially the gastrointestinal tract of children

[0007] Patent CN201310598573.4 discloses a montelukast sodium granule composition and its preparation method. Hypromellose and hypromellose are used as binders. Through verification, it can be known that hypromellose can make montelukast Unknown impurities are introduced into the special sodium particles, which vary with the preparation process and are highly dependent on the process

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