Tablet containing sacubitril valsartan sodium and preparation method thereof

A technology of sacubitrilvaler and sartan sodium, which is applied in the direction of medical preparations containing active ingredients, medical preparations without active ingredients, pill delivery, etc., which can solve the problems of easy weathering and deliquescence, stickiness without inspection, and personnel Large damage and other problems, achieve the effect of one-sided smoothness and non-sticky flushing, ensure bioavailability, and solve the problem of sticky flushing

Active Publication Date: 2021-11-16
NANJING HEALTHNICE MEDICAL TECH +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Sacubitril valsartan sodium is an angiotensin receptor antagonist (valsartan ARB) combined with a neutral endopeptidase inhibitor (sacubitril NEPi) with a non-covalent bond (hydrogen bond, ionic bond) The supramolecular complex, the therapeutic effect of this supramolecular complex in vivo is far greater than the simple sum of the two, but this structure is unstable to humidity and heat, and the raw material drug has a special The surface properties are easy to aggregate, adsorb, and adhere, which brings great challenges to the preparation process.
[0007] Chinese patent CN103251587A discloses an oral tablet of sacubitril-valsartan sodium, pointing out that the existing preparation method may have negative effects on the raw drug, for example, resulting in an amorphous increase of the dual-action complex and / or its components Therefore, the formulation of dual-action complexes (such as supramolecular complexes) is important
[0008] Chinese patent CN111358783A discloses a pharmaceutical preparation of sacubitril-valsartan sodium. In order to solve the problem of moisture absorption of raw materials, a large amount of dipotassium hydrogen phosphate / disodium hydrogen phosphate, disintegrant, and a large amount of inorganic salts are added to the formula. The use of the drug can easily cause electrolyte imbalance in the human body, which will bring great risks to clinical medication.
As we all know, dipotassium hydrogen phosphate or disodium hydrogen phosphate is easy to weather and deliquescence, which will bring a series of problems to the quality of the product in the later stage, and it does not effectively solve the sticking problem of the tablet
[0009] Chinese patent CN109464442A discloses a kind of sacubitril-valsartan sodium pharmaceutical composition, adopts acetone as the solvent of raw material and auxiliary material, then mixes granulation, tabletting, coating, has adopted organic solvent in the preparation process, to Personnel injury is greater, the preparation process is more cumbersome, and the problem of sticking and punching has not been investigated

Method used

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  • Tablet containing sacubitril valsartan sodium and preparation method thereof
  • Tablet containing sacubitril valsartan sodium and preparation method thereof
  • Tablet containing sacubitril valsartan sodium and preparation method thereof

Examples

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Effect test

Embodiment 1

[0042] A tablet containing sacubitril-valsartan sodium, wherein the formula composition and mass percentage of the tablet core are shown in Table 1 below, wherein the mass ratio of xylitol to silicified microcrystalline cellulose is 3.0:1.

[0043] Formula composition and mass percent of table 1 tablet core

[0044] formula Dosage (g) Mass percentage (%) Sacubitril Valsartan Sodium 100 50 Xylitol 23 11.5 Silicified microcrystalline cellulose 70 35 Croscarmellose Sodium 6 3 Magnesium stearate 1 0.5

[0045] The preparation method is as follows:

[0046] (1) Sacubitril-valsartan sodium and silicified microcrystalline cellulose (D90=70 μm) were put into the hopper mixer, and mixed for 20 minutes at a speed of 15 rpm to make them uniformly dispersed;

[0047] (2) add xylitol in the mixture that obtains in step (1), with the rotating speed of 15 revs / min, mix 15 minutes, make it disperse;

[0048] (3) Add croscarmellose sodium a...

Embodiment 2

[0051] A tablet containing sacubitril-valsartan sodium, wherein the formula composition and mass percentage of the tablet core are shown in Table 2 below, wherein the mass ratio of xylitol to silicified microcrystalline cellulose is 1.8:1.

[0052] Formula composition and mass percent of table 2 tablet core

[0053] formula Dosage (g) Mass percentage (%) Sacubitril Valsartan Sodium 100 50 Xylitol 33 16.5 Silicified microcrystalline cellulose 60 30 Croscarmellose Sodium 6 3 Magnesium stearate 1 0.5

[0054] The preparation method is as follows:

[0055] (1) Put sacubitril-valsartan sodium and silicified microcrystalline cellulose (D90=120 μm) into the hopper mixer, and mix for 20 minutes at a speed of 15 rpm to make them uniformly dispersed;

[0056] (2) add xylitol in the mixture that obtains in step (1), with the rotating speed of 15 revs / min, mix 15 minutes, make it disperse;

[0057] (3) Add croscarmellose sodium and mag...

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Abstract

The invention relates to a tablet containing sacubitril valsartan sodium and a preparation method of the tablet. The sacubitril valsartan sodium tablet or tablet core is prepared from the following components in parts by weight: 40-60 parts of sacubitril valsartan sodium, 5-25 parts of xylitol, 20-50 parts of silicified microcrystalline cellulose, 1-5 parts of a disintegrating agent and 0.25-0.75 part of a lubricating agent, wherein the particle size D90 of the silicified microcrystalline cellulose is 65-125 microns, and the mass ratio of the xylitol to the silicified microcrystalline cellulose is (1.5-4.5) : 1. According to the tablet provided by the invention, xylitol and silicified microcrystalline cellulose are used as filling agents, specific auxiliary materials are screened out, and the ratio of the auxiliary materials is controlled. The formula solves the sticking problem of the tablet in the preparation process. The medicine has the advantages of simple preparation method, low cost, quick dissolution, good friability, smooth and stickless tablet surface, good stability and the like. The method is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a tablet containing sacubitril-valsartan sodium and a preparation method thereof. Background technique [0002] Sacubitril valsartan sodium was developed by Novartis Pharmaceuticals Co., Ltd. for the treatment of chronic heart failure or hypertension. It is a dual-acting molecule that simultaneously inhibits neprilysin and angiotensin receptors, simultaneously acts on the renin-angiotensin system and promotes brain natriuretic peptide circulation, and acts on cardiac neuroendocrine in multiple ways system, blocking receptors that exert deleterious effects while promoting protective mechanisms. Clinical studies have shown that sacubitril-valsartan sodium has a significant effect in the treatment of chronic heart failure and hypertension with good safety. It was approved for marketing in the United States in July 2015. The product name is ENTRESTO, and the dosage forms ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/26A61K31/41A61K31/216A61P9/04A61P9/12
CPCA61K9/2054A61K9/2018A61K9/2095A61K31/41A61K31/216A61P9/04A61P9/12A61K2300/00
Inventor 陈长德圣晨丁佳伟孙莉莉王华娟
Owner NANJING HEALTHNICE MEDICAL TECH
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