A kind of roxithromycin sustained and controlled release preparation

A technology of roxithromycin and controlled-release preparations, which is applied in the field of medicine, can solve problems such as the core material sticking to the surface of microcapsule particles, high one-time investment in equipment, and affecting product quality, so as to achieve good floating performance and improve biological Utilization and the effect of prolonging the residence time

Active Publication Date: 2018-08-28
西安远大德天药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the embedding rate of the spray drying method is low, and the core material may adhere to the surface of the microcapsule particles, thereby affecting the quality of the product. The size of the equipment is large, the cost is high, the thermal efficiency is relatively low by 30%-40%, and the energy consumption is large.
[0010] In the research on the preparation of active substance complexes by supercritical carbon dioxide injection method in the literature, Shen Peiqiong used mesoporous silica as the carrier and A-tocopherol as the model drug, and prepared A-tocopherol / mesoporous silica by supercritical carbon dioxide injection method Compound, but the disadvantage of supercritical carbon dioxide is that the equipment and operation are carried out under high pressure, and the one-time investment of equipment is relatively high

Method used

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  • A kind of roxithromycin sustained and controlled release preparation
  • A kind of roxithromycin sustained and controlled release preparation

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Experimental program
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Effect test

Embodiment 1

[0029] The roxithromycin sustained-release preparation of the present embodiment is mainly made of roxithromycin and mesoporous silicon dioxide, and the mass ratio of said roxithromycin and mesoporous silicon dioxide is 1:1, and said The mesoporous silica was MCM-48 mesoporous silica.

[0030] The preparation method of the roxithromycin sustained-release preparation of the present embodiment may further comprise the steps:

[0031] Step 1, wet grinding roxithromycin and mesoporous silica together for 3 hours, the grinding medium is water, to obtain drug-loaded silica suspension;

[0032] Step 2, wrapping the drug-loaded silicon dioxide suspension described in step 1 on the microcrystalline cellulose ball core to make micropills by using the liquid phase layering method, and then packing the micropills into capsules to make capsules, Each capsule contains roxithromycin 150mg.

Embodiment 2

[0034] The roxithromycin sustained-release preparation of the present embodiment is mainly made of roxithromycin and mesoporous silicon dioxide, and the mass ratio of said roxithromycin and mesoporous silicon dioxide is 6:1, and said The mesoporous silica was MCM-48 mesoporous silica.

[0035] The preparation method of the roxithromycin sustained-release preparation of the present embodiment may further comprise the steps:

[0036] Step 1, wet-grinding roxithromycin and mesoporous silica for 24 hours, and the grinding medium is water, to obtain a drug-loaded silica suspension;

[0037] Step 2, adding microcrystalline cellulose and lactose to the drug-loaded silicon dioxide suspension described in step 1, mixing uniformly, extruding and spheronizing to make pellets, and then packing the pellets into capsules to make capsules, Each capsule contains roxithromycin 150mg; the quality of microcrystalline cellulose is 30% of the quality of roxithromycin, and the quality of lactose i...

Embodiment 3

[0039] The roxithromycin sustained-release preparation of the present embodiment is mainly made of roxithromycin and mesoporous silicon dioxide, and the mass ratio of said roxithromycin and mesoporous silicon dioxide is 6:1, and said The mesoporous silica was MCM-48 mesoporous silica.

[0040] The preparation method of the roxithromycin sustained-release preparation of the present embodiment may further comprise the steps:

[0041] Step 1, wet grinding roxithromycin and mesoporous silica together for 20 hours, the grinding medium is water, to obtain drug-loaded silica suspension;

[0042] Step 2, adding microcrystalline cellulose and lactose to the drug-loaded silicon dioxide suspension described in step 1, mixing uniformly, extruding and spheronizing to make pellets, and then packing the pellets into capsules to make capsules, Each capsule contains roxithromycin 150mg; the quality of microcrystalline cellulose is 30% of the quality of roxithromycin, and the quality of lactos...

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Abstract

The invention discloses a roxithromycin controlled-release preparation. The roxithromycin controlled-release preparation is mainly prepared from roxithromycin and mesoporous silica, and the mass ratio of roxithromycin to mesoporous silica is (1-10):1. Mesoporous silica is adopted as a controlled-release material. Roxithromycin has high hydrophobicity and is fast dissolved out in the stomach, which is a key feature for guaranteeing the bioavailability of the preparation, after medicine is loaded in mesoporous silica,a crystalline structure is lost, an amorphous or molecular state emerges, the medicine is free of lattice constraint, free energy is large, and the medicine can be more easily dissolved in media; secondarily, a large specific surface of mesoporous silica is favorable for dissolution of the medicine; besides, adsorption of mesoporous silica on roxithromycin is physical adsorption, no chemical bonds are formed, main acting force is achieved through hydrogen bonds, bond energy is low, and medicine molecules can be easily released. The roxithromycin controlled-release preparation is simple in preparation technology and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a slow-controlled release preparation of roxithromycin. Background technique [0002] The chemical name of roxithromycin is 9-[O-[(2-methoxyethoxy)-methyl]oximino]erythromycin, molecular formula C 14 h 76 N 2 o 15 , molecular weight 837.05. Macrolide antibiotics have experienced more than 40 years of development since their discovery, and are still widely used in various infectious diseases. Roxithromycin is a derivative of erythromycin ether oxime. Roxithromycin overcomes the disadvantages of large side effects and poor tolerance of erythromycin through the modification of erythromycin molecules, improves antibacterial activity and antibacterial spectrum, and has good oral absorption, high peak concentration, long half-life, tissue and Strong intracellular penetration, balanced blood drug concentration, and MIC with most bacteria 90 It has the characteristics...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/48A61K31/7048A61K47/04A61P31/04
CPCA61K9/0002A61K9/1611A61K9/2009A61K9/2077A61K31/7048
Inventor 李成胜
Owner 西安远大德天药业股份有限公司
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