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Lisinopril sustained release tablet and preparation method thereof

A technology for sustained-release tablets and tablet cores, which is applied in the field of lisinopril sustained-release tablets and their preparation, can solve the problems that blood pressure of hypertensive patients cannot be controlled relatively smoothly, the release speed is unstable, and the process is complicated, and the reduction of Cardiovascular and cerebrovascular incidence rate, improving bioavailability, and the effects of wide source of raw materials

Inactive Publication Date: 2017-10-24
江苏黄河药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The current lisinopril preparations are ordinary tablets and capsules, and its blood pressure control depends on the blood drug concentration, but the blood drug concentration has peaks and troughs. It is too low, and after the effect of the drug, the blood pressure of the patient rebounds, often exceeding the normal blood pressure, which directly leads to the inability to control the blood pressure of the hypertensive patient more smoothly, and the purpose of drug administration cannot be achieved according to the rhythm of the blood pressure of the human body. , and some shapes are complicated in composition, although they have a certain comprehensive curative effect, they are not conducive to industrial production
In order to solve the above technical problems, the patent No. 201210585996.8 discloses a lisinopril sustained-release tablet and its preparation method. After the porogen in the coating layer is gradually dissolved in the present invention to form drug release channels, the Drugs pass through these channels to achieve the effect of release, so as to achieve the effect of delayed release and slow release of drugs; the release rate is determined by the characteristics of the tablet core and the characteristics of the coating layer. Due to the complicated process, the process conditions and technical parameters are not easy to control. Poor reproducibility, resulting in unstable release rate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The invention provides a lisinopril sustained-release tablet, which consists of a tablet core containing lisinopril and a coating layer wrapped outside the tablet core, the coating layer is made of ethyl cellulose, the The tablet core includes the following substances in parts by weight: 5.0 parts of lisinopril and 40 parts of porous carbon material.

[0037] The preparation method of described lisinopril sustained-release tablet, comprises the following steps:

[0038] (1) Soak the fungus with salt water for 10 minutes, after drying, carbonize in an inert gas to obtain a porous carbon material, the concentration of the salt water is 5g / mL, the carbonization temperature is 900°C, and the carbonization time is 1 hour;

[0039] (2) After mixing lisinopril, porous carbon material, polyethylene glycol, magnesium stearate, and microcrystalline cellulose uniformly, granulate, dry, and compress tablets to make a tablet core containing lisinopril;

[0040] (3) Ethyl cellulose...

Embodiment 2

[0042] The invention provides a lisinopril sustained-release tablet, which consists of a tablet core containing lisinopril and a coating layer wrapped outside the tablet core, the coating layer is made of ethyl cellulose, the The tablet core includes the following substances in parts by weight: 10 parts of lisinopril and 70 parts of porous carbon material.

[0043] The preparation method of described lisinopril sustained-release tablet, comprises the following steps:

[0044] (1) Soak sphagnum moss in salt water for 60 minutes, after drying, carbonize in an inert gas to obtain a porous carbon material, the concentration of the salt water is 15g / mL, the carbonization temperature is 200°C, and the carbonization time is 10 hours;

[0045] (2) Lisinopril, porous carbon material, polyethylene glycol, glycerin, talcum powder, sucrose, dextrin, polyvinylpyrrolidone, propyl gallate, sodium diacetate are mixed evenly, granulated, dried, pressed Tablets made into tablet cores containi...

Embodiment 3

[0048] The invention provides a lisinopril sustained-release tablet, which consists of a tablet core containing lisinopril and a coating layer wrapped outside the tablet core, the coating layer is made of ethyl cellulose, the The tablet core includes the following substances in parts by weight: 6 parts of lisinopril and 50 parts of porous carbon material.

[0049] The lisinopril sustained-release tablet also contains the following substances:

[0050] The preparation method of described lisinopril sustained-release tablet, comprises the following steps:

[0051] (1) Soak Lisa fern in salt water for 40 minutes, dry it, and carbonize it in an inert gas to obtain a porous carbon material. The concentration of the brine is 2g / mL, the carbonization temperature is 400°C, and the carbonization time for 5 hours;

[0052] (2) Mix lisinopril, porous carbon material, polyvinylpyrrolidone, castor oil, magnesium stearate, talcum powder, precrossed starch, starch, dibutylhydroxytoluene, a...

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Abstract

The invention relates to the technical fields of sustained release tablets and preparation thereof and particularly relates to a lisinopril sustained release tablet and a preparation method thereof. The lisinopril sustained release tablet is formed by a tablet core containing lisinopril and a coating layer packaging the tablet core, wherein the coating layer is prepared from non-water-soluble coating materials. The lisinopril sustained release tablet is characterized in that the tablet core contains the following substances in parts by weight: 5.0%-10 parts of lisinopril and 40-70 parts of a porous carbon material. The lisinopril sustained release tablet has a release delaying effect and a sustained release effect; and the preparation method is simple in process, wide in raw material source and beneficial to industrial production.

Description

technical field [0001] The invention relates to the technical field of sustained-release tablets and preparation thereof, in particular to a lisinopril sustained-release tablet and a preparation method thereof. Background technique [0002] Lisinopril is a lysine derivative of enalaprilat, which belongs to the third generation of angiotensin-converting enzyme inhibitors. Lisinopril can inhibit the activity of angiotensin-converting enzymes, making angiotensin II and The concentration of aldosterone decreases, the activity of plasma renin increases, and the expansion of peripheral blood vessels and the decrease of vascular resistance result in an antihypertensive effect. It is mainly suitable for the treatment of essential hypertension. [0003] However, the onset of hypertensive diseases has the characteristics of a circadian rhythm. The blood pressure of the human body presents rhythmic changes within 24 hours. One of two important features. Understanding the rhythmic cha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K9/22A61K9/36A61K9/32A61K47/46A61K47/38A61K47/10A61P9/12A61P9/00
Inventor 朱正标陶元明张汉华李苗苗范小雪
Owner 江苏黄河药业股份有限公司
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