Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Felodipine sustained-release tablet and preparation method thereof

A felodipine and gentle technology, applied in the direction of medical preparations with non-active ingredients, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of cumbersome process, poor curative effect, complicated process, etc., and achieve the solution of preparation The effect of cumbersome process, low requirements for production equipment, and simple preparation process

Active Publication Date: 2011-09-21
山东威高药业有限公司
View PDF12 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method process is more complicated, and the use cost of crospovidone is high
Cross-linked povidone is used as a super disintegrant. This method is effective in preparing fast-dissolving preparations, but the preparation of sustained-release preparations leads to difficulty in controlling the release rate, large amount of sustained-release matrix materials, obvious burst release phenomenon, and difficult to guarantee safety.
[0006] The preparation methods of the above-mentioned prior art are complicated, the process is cumbersome, the energy consumption is high, and industrialized production is very difficult, which has seriously affected the production and application of felodipine sustained-release preparations
There are also some companies that have not solubilized felodipine, but directly prepared sustained-release preparations, resulting in poor curative effect of some felodipine sustained-release preparations, affecting the healing of patients.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0020] The preparation method of felodipine slow-release tablet of the present invention, it comprises the following steps: first, add povidone K30 or povidone K25 in ethanol and dissolve, wherein the weight ratio of ethanol and povidone K30 or povidone K25 is 3~10:1; Second, add felodipine into the ethanol solvent dissolved with povidone K30 or povidone K25, the weight ratio of ethanol to povidone K30 or povidone K25 is 3~10:1 , to obtain a mixed solution after completely dissolving; thirdly, adding the prepared mixed solution to the slow-release material for direct adsorption, mixing, and granulation, and the weight ratio of the slow-release material to ethanol is 0.1~2.5:1; fourthly, the The granules are dried under normal pressure to obtain dry granules containing the solid dispersion of felodipine and povidone, and then granulated and tableted to obtain plain tablets or coated with plain tablets to obtain coated tablets.

[0021] Excipients are also added to the sustained...

Embodiment 1

[0022] Embodiment 1: a kind of felodipine sustained-release tablet, its raw material consists of:

[0023] Felodipine 2.5mg

[0024] Povidone K30 30mg

[0025] Hydroxypropyl Methyl Cellulose K4M 20mg

[0026] Hydroxypropyl Methyl Cellulose K100 25mg

[0027] Lactose 6.5mg

[0028] Microcrystalline Cellulose 15mg

[0029] Ethanol 90mg

[0030] Sodium stearyl fumarate 1mg

[0031] Mix the hypromellose K4M, K100, lactose, and microcrystalline cellulose of the prescribed amount evenly to prepare the auxiliary material mixture; add povidone K30 to ethanol to dissolve completely, then add felodipine to dissolve completely and Mix evenly, add directly to the prepared auxiliary material mixture, pass through a 20-mesh sieve to granulate after stirring evenly, and dry in a 50°C oven under normal pressure for 2 hours to obtain sustained-release granules containing solubilized felodipine, granulate, and then add stearin-rich Sodium maleate is mixed evenly and compressed into table...

Embodiment 2

[0032] Embodiment 2: a kind of felodipine slow-release tablet, its raw material consists of:

[0033] Felodipine 2.5mg

[0034] Povidone K30 7.5mg

[0035] Hydroxypropyl Methyl Cellulose K100 50mg

[0036] Lactose 24mg

[0037] Microcrystalline Cellulose 15mg

[0038] Ethanol 75mg

[0039] Sodium stearyl fumarate 1mg

[0040] Mix the hypromellose K100, lactose and microcrystalline cellulose in the prescribed amount evenly to prepare a mixture of auxiliary materials; add povidone K30 to ethanol to dissolve completely, then add felodipine to dissolve completely and mix evenly , directly added to the prepared auxiliary material mixture, stirred evenly, passed through a 20-mesh sieve to granulate, dried in an oven at 50°C under normal pressure for 2 hours, and obtained slow-release granules containing solubilized felodipine, granulated, and then added stearyl fumaric acid The sodium is mixed evenly, pressed into tablets, and then the obtained plain tablets are film-coated to...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a felodipine sustained-release tablet and a preparation method thereof. The sustained-release tablet contains an effective amount of felodipine, polyvinylpyrrolidone K30 or polyvinylpyrrolidone K25, wherein the ratio of the polyvinylpyrrolidone K30 or polyvinylpyrrolidone K25 to the felodipine is 3 to 12 : 1, sustained-release materials and the like. The preparation method of the felodipine sustained-release tablet comprises the following steps: adding a solubiliser into an organic good solvent of felodipine for dissolution, and then adding the felodipine for completedissolution of the solubiliser; adding a prepared solution into a adsorbent mixture, and performing sieving and granulating; and then carrying out drying under a normal pressure to obtain sustained-release dry particles containing solubilized felodipine, and then carrying out granulating, tabletting, and coating to obtain a felodipine sustained-release tablet. According to the invention, the felodipine is solubilized, which enables the curative effect to be enhanced. Besides, a traditional hard-soluble medicament sustained-release tablet has complicated preparation process with high energy consumption, and is not easy to produce and uncontrollable in quality; however, the above problems are solved by the preparation method provided in the invention. Therefore, the simple, low-energy, and high-efficient industrialized production is allowed according to the invention.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a felodipine sustained-release tablet and a preparation method thereof. Background technique [0002] Felodipine is a new generation of DHPs calcium antagonist with high selectivity to blood vessels, which lowers blood pressure by reducing peripheral vascular resistance. The half-life of felodipine sustained-release tablets is as long as 25 hours, and it is taken once a day. It is convenient to use and has good patient compliance. It can be used as an effective drug for the long-term treatment of essential hypertension and is suitable for the treatment of all stages of hypertension. [0003] Scientific research has found that simple high blood pressure can cause damage to organs, but blood pressure fluctuations are especially serious. Felodipine ordinary tablets need to be taken 2-3 times a day. Although this preparation can achieve blood pressure lowering However, d...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/32A61K9/36A61K31/4422A61K47/32A61P9/12
Inventor 王俊锋毕建伟左永昌张辉王翠娜
Owner 山东威高药业有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products