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Sacubitril / valsartan sustained release agent and preparation method thereof

A technology of Shakubi and sustained-release preparations, which is applied in pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve peak and valley fluctuations in blood drug concentration, easy adverse reactions, and failure to achieve therapeutic purposes, etc. problems, to achieve the effect of prolonging the drug effect time, reducing toxicity and adverse reactions, and facilitating drug use

Active Publication Date: 2016-09-14
LIANGJIANG MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Immediate-release tablets need to be administered twice or more times a day, so it often leads to missed doses, and some patients even change the dosage regimen without authorization, thus failing to achieve the expected therapeutic purpose; The way of administration is prone to large peak-to-valley fluctuations in blood drug concentration. Adverse reactions or even poisoning are likely to occur when the blood drug concentration peaks.

Method used

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  • Sacubitril / valsartan sustained release agent and preparation method thereof
  • Sacubitril / valsartan sustained release agent and preparation method thereof
  • Sacubitril / valsartan sustained release agent and preparation method thereof

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Experimental program
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Effect test

preparation example Construction

[0047] The present invention also provides a preparation method of sacubitril-valsartan sustained-release agent, comprising:

[0048] Sacubitril-valsartan co-crystal, hydrophilic gel skeleton material, diluent, first lubricant are mixed, dry granulated, and then the second lubricant is added to mix and tabletted to obtain the sacubitril-valsartan Sartan sustained-release agent;

[0049] The mass ratio of the sacubitril-valsartan co-crystal, skeleton material, diluent to the total amount of the first lubricant and the second lubricant is (10-70): (10-50): (0-80 ): (0.1~10).

[0050] Above-mentioned obtained is sacubitril valsartan sustained-release tablet core material.

[0051] The first lubricant and the second lubricant are added in batches, and the proportion of the lubricant is not particularly limited in the present invention, and can be added according to actual conditions.

[0052] When the sacubitril-valsartan slow-release agent has a coating, the steps also include...

Embodiment 1～3

[0057] According to the proportioning in Table 1, sacubitril valsartan sustained-release preparation is prepared:

[0058] Table 1 Embodiment 1~3 raw material ratio

[0059]

[0060]

[0061] in,

[0062] 49 / 51mg / tablet: refers to that in the sacubitril / valsartan sustained-release preparation, the sacubitril content is 49 mg / tablet, and the valsartan content is 51 mg / tablet. And so on for the rest.

[0063] Preparation:

[0064] Mix sacubitril valsartan co-crystal, hypromellose K15M, lactose and talc powder in a three-dimensional kinematic mixer evenly, then add magnesium stearate and mix, and use the obtained mixed powder with a dry granulator The pressure roller of about 30KN is pressed into strips, and then crushed and granulated by a granulator to obtain the internal phase particles; the internal phase particles, the added part of talc powder and magnesium stearate are placed in a three-dimensional motion mixer and mixed evenly, and then use a high-speed A rotary...

Embodiment 4～6

[0066] According to the proportioning in Table 2, sacubitril valsartan sustained-release preparation is prepared:

[0067] Table 2 Embodiment 4~6 raw material ratio

[0068]

[0069] Preparation:

[0070] Mix sacubitril, trivalsartan co-crystal, hypromellose K100M and talcum powder in a three-dimensional motion mixer evenly, then add magnesium stearate and mix, and use a dry granulator to obtain the mixed powder with a pressure of about 30KN The pressure roller is pressed into strips, and then crushed and granulated by a granulator to obtain the internal phase granules; the internal phase granules, the added part of talcum powder and magnesium stearate are placed in a three-dimensional motion mixer and mixed evenly, and then the high-speed rotary press is used to Tablet machines compress the final blend into tablets. Opadry AMB type moisture-proof coating material is used for coating to obtain moisture-proof coated sustained-release tablets.

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Abstract

The invention provides a sacubitril / valsartan sustained release agent, including 10wt%-70wt% of sacubitril / valsartan, 10wt%-50wt% of hydrophilic gel framework material, 0-80 wt% of a diluent and 0.1wt%-10wt% of a lubricant, wherein the total content of the above components is 100%. In the study of in vitro releasing rate of intestinal juice, the sacubitril / valsartan sustained release tablet reaches release of sacubitril about 80% to 12 h, release of valsartan about 80% to 8, achieves slow release of the two active ingredients, and shows slow release characteristics in vitro test.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a sacubitril-valsartan sustained-release agent and a preparation method thereof. Background technique [0002] Sacubitril / valsartan co-crystal (sacubitril / valsartan, formerly known as LCZ696) was developed by Novartis Pharmaceuticals, Switzerland, and was launched in the United States under the trade name "Entresto" in July 2015. The marketed dosage form is immediate release with non-moisture-proof coating tablet. [0003] Entresto is used in patients with heart failure with reduced ejection fraction to reduce the risk of cardiovascular death and hospitalization for heart failure. Heart failure is a life-threatening heart condition in which the heart cannot pump enough blood and is at high risk of death, repeated hospitalization and other symptoms (such as difficulty breathing, fatigue, fluid retention) that can seriously affect the patient longevity and qua...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/41A61K31/216A61K9/22A61K9/36A61K47/38A61P9/04
CPCA61K9/2013A61K9/286A61K31/216A61K31/41A61K47/38A61K2300/00
Inventor 陈海军彭佳乐贺耘
Owner LIANGJIANG MEDICINE CO LTD
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