Edoxaban-containing sustained release preparation and preparation method thereof

A technology for edoxaban and sustained-release preparations, applied in the field of edoxaban-containing sustained-release preparations and its preparation

Active Publication Date: 2021-05-14
齐飞
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] To overcome the deficiencies in the prior art, the first object of the present invention is to provide a sustained-release preparation containing edoxaban with high dissolution rate and good stability, which avoids or reduces the peak-valley phenomenon of blood drug concentration, so that Edoxaban can achieve rapid onset and sustained release, solve the problem of low dissolution rate, and improve the safety and effectiveness of the drug

Method used

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  • Edoxaban-containing sustained release preparation and preparation method thereof
  • Edoxaban-containing sustained release preparation and preparation method thereof
  • Edoxaban-containing sustained release preparation and preparation method thereof

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Embodiment 1-11

[0032]

[0033]

[0034]

[0035]

[0036] Embodiment 1-11 preparation technology:

[0037] (a) Preparation of edoxaban solid dispersion: the weight component ratio of edoxaban tosylate, poloxamer and sodium lauryl sulfate is 1:1.5:0.5. Take edoxaban toluenesulfonate, add 10 times the amount of ethanol with a mass fraction of 80%, and ultrasonically assist in dissolving to obtain a homogeneous solution; take another poloxamer in an evaporating dish, heat it in a water bath, and pour it into toluene after it is completely melted Add edoxaban sulfonic acid solution, add sodium lauryl sulfate, stir evenly, evaporate the solvent, condense and stir the resulting mixture to solidify, dry, pulverize, and sieve;

[0038] (b) Preparation of the immediate-release layer: pass the edoxaban toluenesulfonate solid dispersion, the disintegrating agent and the filler in the prescribed amount through an 80-mesh sieve and mix uniformly, add magnesium stearate and mix uniformly to ob...

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Abstract

The invention belongs to the technical field of drug sustained release preparations, and particularly relates to an edoxaban-containing sustained release preparation and a preparation method thereof. The sustained release preparation consists of a quick release layer and a sustained release layer, wherein the quick release layer mainly consists of an edoxaban solid dispersion, a disintegrating agent, a filling agent and a lubricating agent; the sustained release layer is mainly composed of an edoxaban bulk drug, a sustained-release material, a filler, a lubricant and an adhesive. The sustained release preparation containing edoxaban, which is excellent in controlled release effect and high in dissolution stability, is provided by optimizing the types, the proportion and the dosage of the filling agent and the sustained release material and optimizing the preparation method of the edoxaban solid dispersion in the process, and the problems that a sustained release preparation containing edoxaban is poor in release effect, low in dissolution rate and the like are solved.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to a sustained-release preparation containing edoxaban and a preparation method thereof. Background technique [0002] Thrombosis has gradually become a common disease that threatens human health, especially in patients with cardiovascular and cerebrovascular thrombosis, its morbidity, disability and mortality are high. Thrombosis can cause stenosis and occlusion of the vascular lumen, leading to ischemia and infarction of major organs, thereby causing various diseases, such as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. [0003] The chemical name of Edoxaban is N-(5-chloro-2-pyridyl)-N'-[(1S,2R,4S)-4-[(dimethylamino)formyl]-2-[[4, 5,6,7-Tetrahydro-5-methylthiazolo[5,4-C]pyridin-2-yl)formyl]amino]cyclohexyl]oxalamide p-toluenesulfonate monohydrate, structural formula as follows: [0004] [0005] Edox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K31/444A61P7/02A61K47/02A61K47/38A61K47/10A61K47/32A61K47/36A61K47/26A61K47/20
CPCA61K31/444A61K9/2095A61P7/02A61K9/209A61K9/2009A61K9/2054A61K9/2018A61K9/2027A61K9/205A61K9/2013
Inventor 齐飞
Owner 齐飞
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