Azithromycin sustained release tablets and method of preparing the same

A technology of azithromycin and sustained-release tablets, which is applied in the field of medicine to achieve the effects of improving compliance and convenience, reducing drug resistance, and taking convenience

Inactive Publication Date: 2008-10-08
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Method used

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  • Azithromycin sustained release tablets and method of preparing the same
  • Azithromycin sustained release tablets and method of preparing the same
  • Azithromycin sustained release tablets and method of preparing the same

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Component weight / 1000 pieces

[0020] Azithromycin 500g

[0021] Hydroxypropyl Methyl Cellulose 140g

[0022] Lactose 220g

[0023] Microcrystalline Cellulose 130g

[0024] Magnesium Stearate 10g

[0025] 90% ethanol appropriate amount

[0026] Grind the ingredients and excipients of the prescription separately and pass through a 100-mesh sieve for later use; mix azithromycin, hydroxypropyl methylcellulose, microcrystalline cellulose and lactose through a 100-mesh sieve, and use an appropriate amount of 90% ethanol to make a soft material, 20 mesh Sieve to granulate, dry the wet granules at 60±5°C, sieve and granulate with 20 meshes; add magnesium stearate, mix well, and tablet. Release curve see figure 1 .

Embodiment 2

[0028] Component Weight

[0029] / 1000 pieces

[0030] Azithromycin 500g

[0031] Polyoxyethylene 200g

[0032] Hydroxypropyl Cortyl Cellulose 150g

[0033] Microcrystalline Cellulose 140g

[0034] Magnesium Stearate 10g

[0035] 90% ethanol appropriate amount

[0036] Grind the raw materials and auxiliary materials of the prescription separately and pass them through a 100-mesh sieve for later use; weigh the prescribed amount of azithromycin, hydroxypropyl methylcellulose, polyoxyethylene and microcrystalline cellulose and pass through a 100-mesh sieve to mix them evenly. It is a soft material made of adhesive, granulated with a 20-mesh sieve, dried at 60±5°C, granulated with a 20-mesh sieve; added magnesium stearate, mixed evenly, and compressed into tablets. Release curve see figure 2 .

Embodiment 3

[0038] Component Weight

[0039] / 1000 pieces

[0040] Azithromycin 500g

[0041] Sodium Alginate 250g

[0042] Lactose 150g

[0043] Microcrystalline Cellulose 90g

[0044] Magnesium Stearate 10g

[0045] 90% ethanol appropriate amount

[0046]Grind the raw materials and auxiliary materials of the prescription separately and pass through a 100-mesh sieve for later use; weigh the prescribed amount of azithromycin, sodium alginate, lactose and microcrystalline cellulose and mix them evenly through a 100-mesh sieve, and use an appropriate amount of 90% ethanol as a binder to make a soft material , 20-mesh sieve, granulated, wet granules were dried at 60±5°C, granulated with 20-mesh sieve; magnesium stearate was added, mixed evenly, and tableted. Release curve see image 3 .

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PUM

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Abstract

The invention pertains to the technical field of medicament and discloses azithromycin sustained release tablets and a preparation method thereof. The composition of a prescription of the azithromycin sustained release tablets is as follows: 10%-80% of azithromycin, 5%-50% of sustained release formulation, 1%-50% of bulking agent and 0.1%-5% of lubricant. The invention is prepared by the following method: the azithromycin, the sustained release formulation, the bulking agent are crushed, then passes 100 mesh sieve and mixed evenly; binder is added to make damp mass which is sieved for pelletization; a wet pellet is dried at the temperature of 50-80 DEC C; the dried pellet is sieved for granulating and then mixed with lubricant for tabletting. The invention is capable of reducing the higher peak concentration of the azithromycin and decreasing fluctuation and untoward response of a medicine, improving medicine concentration in tissue, lengthening the half-life period of the medicine, improving the compliance of a patient, thereby reducing the occurrence of medicine resistance to the utmost extent. The prescription is capable of reducing the side effect of the azithromycin, improving bioavailability, which has the advantages of lasting drug effect and being convenient for being taken.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to azithromycin sustained-release tablets and a preparation method thereof. Background technique: [0002] Azithromycin (azithromycin) is a broad-spectrum antibiotic derived from erythromycin A, the chemical name is 9-deoxy-10α-aza-10α-carbo-erythromycin, and it is the first one developed by Priva Pharmaceuticals in Croatia. 15-membered ring macrolide derivative. Azithromycin has a wider antibacterial spectrum than erythromycin, has strong antibacterial activity against Gram-positive bacteria, and has strong antibacterial activity against some Gram-negative bacteria, anaerobic bacteria and Chlamydia trachomatis. Azithromycin inhibits the synthesis of ribosomal 50s subunit protein in bacterial cells and hinders the process of bacterial transpeptide, thereby inhibiting the synthesis of bacterial proteins and achieving antibacterial effects. Suitable for infections caused by sensit...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/7052A61P31/04
Inventor 何仲贵宁婷孙进刘晓红杨亚军
Owner SHENYANG PHARMA UNIVERSITY
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