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Slow releasing ranolazine micro pill

A technology of sustained-release pellets and ranolazine, which is applied in the field of medicine and can solve problems such as high toxicity, unsuitable formulation of sustained-release preparations, and fluctuations in blood drug concentration

Inactive Publication Date: 2007-11-07
PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] It can be known from the literature review that not all drugs are suitable for the development of sustained-release preparations, and only drugs with certain characteristics are suitable for the development of sustained-release drugs. Drugs that have no correlation with their efficacy should not be made into sustained-release preparations. Some concentration-dependent antibiotics, whose antibacterial effect depends on the peak concentration, are not suitable to be made into sustained-release preparations in principle, etc.; however, some drugs treat chronic diseases, frequently-occurring diseases, etc. It needs to maintain a relatively stable blood drug concentration for a long time, or the drug itself has the characteristics of rapid absorption and clearance, which causes unnecessary large-scale fluctuations in blood drug concentration and short action cycles, so that frequent administration is required in order to obtain appropriate treatment. Such drugs are suitable for developing into sustained-release preparations, and ranolazine belongs to the drugs with the above-mentioned characteristics. The document of Chinese Patent Application No. 99810835.9 discloses a technical scheme for developing ranolazine into sustained-release preparations. Oxyzine is the main drug, developed into sustained-release tablets, but sustained-release tablets have great defects, and may cause "burst release" of active ingredients due to small damage, which will reduce the drug safety of patients, and Sustained-release pellets can solve the problem of "drug burst release" very well. Although the above-mentioned application has some introductions to the preparation of sustained-release pellets in its priority patent, there is no in-depth study based on the characteristics of sustained-release pellets. The study simply disclosed that ranolazine can be prepared into sustained-release pellets

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Ranolazine sustained-release pellets, including ranolazine and pharmaceutical excipients, are characterized in that they are prepared from pellets prepared by wrapping an isolation layer with 5% of the core and 95% of the pellets are successively coated with an isolation layer, a sustained-release layer, and an isolation layer. Composition of micropellets, in which the pellet core includes ranolazine, methacrylic acid copolymer, hydroxypropyl cellulose phthalate, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate One or more of phthalates, polyvinyl acetate, phthalates, polyvinylpyrrolidine phthalates and hydroxypropyl methylcellulose, hydroxypropyl cellulose, One or more of polymethacrylate, polyacrylate, polyvinylpyrrolidone, the isolation layer includes hydroxypropyl methylcellulose, hydroxypropyl cellulose, polymethacrylate, polyacrylate, polyethylene One or more of pyrrolidone, wherein the slow-release layer includes methacrylic acid copolymer, hy...

Embodiment 2

[0084] Ranolazine sustained-release pellets, including ranolazine and pharmaceutical excipients, are characterized in that they are prepared from pellets prepared by 10% pellet core wrapping isolation layer and 90% pellet core wrapping isolation layer, sustained release layer, and isolation layer in turn Composition of micropellets, in which the pellet core includes ranolazine, methacrylic acid copolymer, hydroxypropyl cellulose phthalate, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate One or more of phthalates, polyvinyl acetate, phthalates, polyvinylpyrrolidine phthalates and hydroxypropyl methylcellulose, hydroxypropyl cellulose, One or more of polymethacrylate, polyacrylate, polyvinylpyrrolidone, the isolation layer includes hydroxypropyl methylcellulose, hydroxypropyl cellulose, polymethacrylate, polyacrylate, polyethylene One or more of pyrrolidone, wherein the slow-release layer includes methacrylic acid copolymer, hydroxypropyl cellulose phthalate...

Embodiment 3

[0086] Ranolazine sustained-release pellets, including ranolazine and pharmaceutical excipients, are characterized in that they are prepared from pellets prepared by 15% pellet core wrapping isolation layer and 85% pellet core wrapping isolation layer, sustained release layer, and isolation layer in turn Composition of micropellets, in which the pellet core includes ranolazine, methacrylic acid copolymer, hydroxypropyl cellulose phthalate, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate One or more of phthalates, polyvinyl acetate, phthalates, polyvinylpyrrolidine phthalates and hydroxypropyl methylcellulose, hydroxypropyl cellulose, One or more of polymethacrylate, polyacrylate, polyvinylpyrrolidone, the isolation layer includes hydroxypropyl methylcellulose, hydroxypropyl cellulose, polymethacrylate, polyacrylate, polyethylene One or more of pyrrolidone, wherein the slow-release layer includes methacrylic acid copolymer, hydroxypropyl cellulose phthalate...

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PUM

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Abstract

The present invention discloses one kind of slow releasing ranolazine micro pill including ranolazine and supplementary material. It consists of coating and isolating layer in 5-30 %, preferably in 10 % and pill core in 70-95 %, preferably in 90 %. The slow releasing ranolazine micro pill is tested to have release amount of 20-40 % within 2 hr, 50-80 % within 6 hr, and 80-100 % within 12 hr.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to ranolazine sustained-release pellets. Background technique [0002] Sustained-release preparations are one of the fastest-growing preparations in recent years. Sustained-release preparations can release drugs slowly according to certain rules, and maintain effective drug concentrations in the body for a long time, so as to improve curative effect, prolong drug action time and reduce drug exposure. The purpose of adverse reactions, specifically, has three advantages: (1) For patients, drug sustained release technology can increase the efficacy of drugs, reduce adverse reactions, increase patient compliance and comfort, especially for the elderly, For children and patients who need long-term medication, sustained-release preparations can improve their medication compliance; (2) Drug sustained-release technology can improve drug compliance and treatment convenience, greatly reducin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/30A61K31/495A61K47/32A61K47/14A61K47/34A61K47/38A61K47/02A61P9/10A61P9/04A61K47/10
Inventor 顾群金治刚米长江赵丽云
Owner PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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