A sacubitril valsartan sustained-release agent and preparation method thereof

A technology of sacubi and sustained-release agent, which is applied in the directions of pill delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the peak-to-valley fluctuation of blood drug concentration, easy to produce adverse reactions, and can not achieve the purpose of treatment, etc. problems, to achieve the effect of prolonging the efficacy time, reducing toxicity and adverse reactions, and facilitating medication

Active Publication Date: 2019-06-07
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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  • A sacubitril valsartan sustained-release agent and preparation method thereof
  • A sacubitril valsartan sustained-release agent and preparation method thereof
  • A sacubitril valsartan sustained-release agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

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

[0048] The sacubitril valsartan co-crystal, the hydrophilic gel matrix material, the diluent, the first lubricant are mixed, dry granulated, and then the second lubricant is added for mixing and tableting to obtain the sacubitril valsartan Sartan sustained-release agent;

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

[0050] The material obtained above is the core material of sacubitril and valsartan sustained-release tablet.

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

[0052] When the sacubitril and valsartan sustained-release preparation has a c...

Embodiment 1～3

[0057] According to the ratio in Table 1, the sustained-release formulation of sacubitril and valsartan was prepared:

[0058] Table 1 The ratio of raw materials in Examples 1 to 3

[0059]

[0060]

[0061] among them,

[0062] 49 / 51mg / tablet: refers to the said sacubitril and valsartan sustained-release formulation, the content of sacubitril is 49mg / tablet, and the content of valsartan is 51mg / tablet. The rest can be deduced by analogy.

[0063] Preparation:

[0064] Combine sacubitril valsartan co-crystal, hypromellose K15M, lactose and talc powder in a three-dimensional motion mixer and mix them evenly, then add magnesium stearate to mix, and use the dry granulator to obtain the mixed powder The pressure roller of about 30KN is pressed into strips, and then pulverized and granulated by a granulator to obtain internal phase particles; the internal phase particles and the external part of talcum powder and magnesium stearate are mixed evenly in a three-dimensional motion mixer, and ...

Embodiment 4～6

[0066] According to the ratio of Table 2, the sustained-release formulation of sacubitril and valsartan was prepared:

[0067] Table 2 The ratio of raw materials in Examples 4-6

[0068]

[0069] Preparation:

[0070] Combine sacubitril and valsartan co-crystal, hypromellose K100M and talc powder in a three-dimensional motion mixer and mix them evenly, then add magnesium stearate to mix, and use a dry granulator to use about 30KN for the resulting mixed powder The pressure roller is pressed into strips, and then pulverized and granulated by a granulator to obtain internal phase particles; the internal phase particles, added part of talc and magnesium stearate are placed in a three-dimensional motion mixer and mixed uniformly, and then high-speed rotary press The tablet machine compresses the final mixture 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 preparation and a preparation method thereof. Background technique [0002] Sacubitril / valsartan co-crystal (sacubitril / valsartan, formerly known as LCZ696) was developed by Swiss Novartis Pharmaceuticals, and was launched in the United States under the trade name "Entresto" in July 2015. The marketed dosage form is non-moisture-proof coated immediate release tablet. [0003] Entresto is used for heart failure patients with reduced ejection fraction to reduce the risk of cardiovascular death and heart failure hospitalization. Heart failure is a life-threatening heart disease. The patient's heart cannot pump enough blood, and therefore faces a high risk of death, repeated hospitalizations and other symptoms (such as dyspnea, fatigue, fluid retention). The disease can seriously affect the patient Life span and quality of life....

Claims

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Application Information

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Patent Type & Authority Patents(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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