Cardiac failure resisting medicine LCZ696 oral sustained-release pellets and preparation method thereof

A technology of slow-release pellets and heart failure, applied in the field of medicine, can solve the problems of peak and valley blood drug concentration, easy adhesion to the mouth and throat, adverse drug side effects, etc., achieve low production cost, simple operation, and reduce drug toxicity side effects

Inactive Publication Date: 2016-12-07
TAILITE MEDICINE HUBEI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, the ordinary immediate-release preparation of LCZ696 developed by Novartis abroad needs to be taken orally twice a day, which has the following disadvantages: the number of times of taking the medicine is relatively large, which increases the difficulty of medication for people, especially the elderly and those with dysphagia; There are obvious peak and valley phenomena in the blood concentration, which is not conducive to reducing the side effects of the drug
Chinese invention patent CN 105748420A discloses a sustained-release matrix tablet containing the active pharmaceutical ingredient LCZ696, which overcomes the above-mentioned shortcomings to a certain extent, but the matrix tablet obtained is not coated, and the sustained-release effect is not good. At the same time, it is made of powder Compressed into tablets, it is easy to stick to the mouth and throat when taking it, and it is inconvenient to swallow

Method used

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  • Cardiac failure resisting medicine LCZ696 oral sustained-release pellets and preparation method thereof
  • Cardiac failure resisting medicine LCZ696 oral sustained-release pellets and preparation method thereof
  • Cardiac failure resisting medicine LCZ696 oral sustained-release pellets and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] An anti-heart failure drug LCZ696 oral sustained-release pellets:

[0032] Including the core and the coating outside the core, the core ingredients are: LCZ696 2g, microcrystalline cellulose 10g, lactose 5g, hydroxypropyl methylcellulose 1g; the coating ingredients are: Eudragit RS100 2g, PEG4000 0.8g , triethyl citrate 1g, talc powder 1g, titanium dioxide 0.2g.

[0033] The preparation method of the above-mentioned anti-heart failure drug LCZ696 oral sustained-release pellets: take the materials according to the quality of the above-mentioned raw materials, first mix LCZ696 with microcrystalline cellulose and lactose, and use hydroxypropyl methylcellulose as a binder , the centrifugal-fluidization method is used in the centrifugal coating granulator to make the pellet core, and then the pellet core is coated with the coating ingredients in the same way, and after the coating is completed, it is obtained.

Embodiment 2

[0035] An anti-heart failure drug LCZ696 oral sustained-release pellets:

[0036]Including the ball core and the coating outside the ball core. The core ingredients are: LCZ696 15g, microcrystalline cellulose 15g, mannitol 5g, ethyl cellulose 8g; the coating ingredients are: polyvinylpyrrolidone 5g, Eudragit RL100 3g, PEG4000 0.1g, dimethyl phthalate 0.1g, talc powder 0.1g.

[0037] The preparation method of the above-mentioned anti-heart failure drug LCZ696 oral sustained-release pellets: take the materials according to the quality of the above-mentioned raw materials, first mix LCZ696 with microcrystalline cellulose and mannitol evenly, and use ethyl cellulose as a binder. Roll in a coating pan to form a ball core, then add coating ingredients and continue rolling to coat the ball core. After the coating is completed, it is ready.

Embodiment 3

[0039] An anti-heart failure drug LCZ696 oral sustained-release pellets:

[0040] Including the core and the coating outside the core, the core ingredients are: LCZ696 35g, sucrose powder 30g, compressible starch 30g, medicinal calcium carbonate 10g, methyl cellulose 6g; the coating ingredients are: Eudragit NE30D 25g , PEG4000 3g. Triethyl citrate 3g, talcum powder 10g, sodium lauryl sulfate 5g.

[0041] The preparation method of the above-mentioned anti-heart failure drug LCZ696 oral sustained-release pellets: take materials according to the quality of the above-mentioned raw materials, first mix LCZ696 with sucrose powder, compressible starch and medicinal calcium carbonate, and methyl cellulose is The binder is made into pellet cores in a extrusion-pellet pellet machine, and then the pellet cores are coated with coating ingredients. After the coating is completed, it is ready to be obtained.

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Abstract

The invention belongs to the field of medicine, and particularly relates to cardiac failure resisting medicine LCZ696 oral sustained-release pellets and a preparation method thereof. The sustained-release pellets comprise pellet cores prepared from, by weight, 2-55 parts of LCZ696 medicine, 15-90 parts of diluent and 1-15 parts of adhesive and a coating prepared from, by weight, 1-35 parts of sustained-release materials, 0.1-5 parts of pore-foaming agent, 0.1-5 parts of plasticizer and 0.1-25 parts of antisticking agent on the outer portions of the pellet cores. The cardiac failure resisting medicine LCZ696 oral sustained-release pellets have the advantages that LCZ696 can be slowly released in the body by means of the sustained-release pellets, the plasma concentration is more stable, and clinical effectiveness and safety are effectively improved. The cardiac failure resisting medicine LCZ696 oral sustained-release pellets are suitable for symptoms caused by the cardiac failure, medicine release is stable, the effect is good, irritation to the gastrointestinal tract is small, and absorption is good after oral medication. The preparation method of the sustained-release pellets is easy to operate, the production cost is low, efficiency is high, and the sustained-release pellets are suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an anti-heart failure drug LCZ696 oral sustained-release pellets and a preparation method thereof. Background technique [0002] LCZ 696 (foreign name is Entresto, CAS number is 936623-90-4, molecular formula is (C24H29N5O3) (C24H29NO5) 2.5(H2O) 3Na + ) is a dual-acting angiotensin receptor and neprilysin inhibitor with a unique mode of action thought to reduce strain in failing hearts. LCZ 696 combines the hypertension drug valsartan, which improves vasodilation and stimulates the body to excrete sodium and water, with the experimental drug AHU-377, which blocks the mechanism of action of two polypeptides that threaten to lower blood pressure. LCZ696 is a combination of two components, valsartan and AHU-377, which are: N-valeryl-N-[[2'-(1H-tetrazol-5-yl)[1 ,1'-biphenyl]-4-yl]methyl]-L-valine (valsartan, CAS: 137862-87-4) and 4-(((2S,4R)-1-([1 ,1'-biphenyl]-4-yl)-5-ethoxy-4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/41A61K31/216A61P9/04
CPCA61K9/5026A61K9/0002A61K9/5015A61K9/5031A61K31/216A61K31/41A61K2300/00
Inventor 刘明星童庆吴建宏
Owner TAILITE MEDICINE HUBEI
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