Dirithromycin enteric-coated tablet and preparation method thereof

A technology of dirithromycin and enteric-coated tablets, which is applied in the field of medicine, can solve the problems of poor product stability, unresolved, and decreased stability of dirithromycin, and achieve the effect of reducing the production of impurities

Active Publication Date: 2022-04-08
ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Dirithromycin enteric-coated tablets using dry granulation have certain disadvantages
Dry granulation will generate a certain amount of heat in the process of roller pressing and crushing, and there is a certain amount of moisture in the raw and auxiliary materials, which will lead to a decrease in the stability of dirithromycin after tableting
Although CN201711303866.X "a dirithromycin enteric-coated tablet enteric coating, its preparation method and a dirithromycin enteric-coated tablet" (application date 2017.12.11, publication date 2019.06.18) by optimizing enteric coating Coating prescription solves the problem of poor product stability caused by acid sensitivity, but does not solve the problem of poor product stability caused by mechanical heat and moisture in tablet compression

Method used

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  • Dirithromycin enteric-coated tablet and preparation method thereof
  • Dirithromycin enteric-coated tablet and preparation method thereof
  • Dirithromycin enteric-coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Preparation of Tablet Core 1

[0041] 1. Prescription

[0042] Get table 4 tablet core 1 prescription, be used to prepare 500 dirithromycin tablet cores whose specification is 0.125g and whose average tablet weight is 0.419g.

[0043] Table 4 Composition of Chip 1

[0044] composition mass (g) percentage(%) composition mass (g) percentage(%) Dirithromycin 62.50 29.8 Croscarmellose Sodium 2.92 1.4 microcrystalline cellulose 55.42 26.5 Sodium carboxymethyl starch 3.13 1.5 Heavy Magnesium Carbonate 59.17 28.2 Magnesium stearate 5.21 2.5 Hypromellose 20.21 9.6 colloidal silica 1.04 0.5

[0045] 2. Preparation method

[0046] Pass the raw material and auxiliary materials through a 40-mesh sieve, and set aside; take the prescribed amount of dirithromycin and colloidal silicon dioxide, mix them evenly for 5 minutes, and use them as premix 1 for later use; mix premix 1 with the prescribed amount...

Embodiment 2

[0047] Embodiment 2: preparation of tablet core 2

[0048] 1. Prescription

[0049] Get table 5 tablet core 2 prescription, be used to prepare 500 specifications and be 0.125g, the dirithromycin tablet core that average sheet weight is 0.385g.

[0050] Table 5 Composition of core 2

[0051] composition mass (g) percentage(%) composition mass (g) percentage(%) Dirithromycin 62.50 32.5 Sodium carboxymethyl starch 7.12 3.7 microcrystalline cellulose 48.65 25.3 polyethylene glycol 2.88 1.5 Heavy Magnesium Carbonate 33.46 17.4 Calcium stearate 1.54 0.8 pregelatinized starch 29.23 15.2 colloidal silica 4.62 2.4 Crospovidone 2.31 1.2 / / /

[0052] 2. Preparation process

[0053] Pass the raw material and auxiliary materials through a 50-mesh sieve, and set aside; take the prescribed amount of dirithromycin and colloidal silicon dioxide, mix them for 6 minutes, and use them as premix 1 for later use; mix ...

Embodiment 3

[0054] Embodiment 3: preparation of tablet core 3

[0055] 1. Prescription

[0056] Get table 6 tablet core 3 prescription, be used to prepare 500 dirithromycin tablet cores whose specifications are 0.125g and whose average tablet weight is 0.357g.

[0057] Table 6 Composition of core 3

[0058] composition mass (g) percentage(%) composition mass (g) percentage(%) Dirithromycin 62.50 35 Crospovidone 4.64 2.6 Heavy Magnesium Carbonate 44.29 24.8 Magnesium stearate 5.00 2.8 lactose 55.54 31.1 Talc powder (3000 mesh) 3.39 1.9 Croscarmellose Sodium 3.21 1.8 / / /

[0059] 2. Preparation process

[0060] Pass the raw material and auxiliary materials through a 60-mesh sieve, and set aside; take the prescribed amount of dirithromycin and talcum powder, mix for 10 minutes, and use it as premix 1 for later use; mix the premix 1 with the prescribed amount of heavy magnesium carbonate, lactose, Croscarmellose sodium an...

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Abstract

The invention provides a dirithromycin enteric-coated tablet and a preparation method thereof, the enteric-coated tablet comprises a tablet core, an isolation layer and an enteric-coated layer, the tablet core comprises 30%-35% (w/w) of dirithromycin, 55%-65% (w/w) of a diluent, 3%-5% (w/w) of a disintegrating agent, 0.5%-3% (w/w) of a flow aid and 0.5%-3% (w/w) of a lubricant. The weight of the isolating layer is increased by 3-9% (w/w) based on the weight of the tablet core, and the raw material comprises hydroxypropyl methyl cellulose; the weight of the enteric-coated layer is increased by 6-12% (w/w) based on the weight of the tablet core, and the enteric-coated layer is prepared from a methacrylic acid-ethyl acrylate copolymer. The preparation method comprises the following steps: uniformly mixing a flow aid and dirithromycin in advance, uniformly mixing the premix with a diluent, a disintegrating agent and a lubricant, and directly tabletting the obtained mixture powder to obtain a tablet core; and wrapping an isolating layer and an enteric-coated layer to prepare the enteric-coated tablet. Compared with a reference preparation, the dirithromycin enteric-coated tablet provided by the invention is more stable in quality and less in impurities; the dissolution is consistent, and the consistency evaluation requirement is met; the process is simple and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a dirithromycin enteric-coated tablet and a preparation method thereof. Background technique [0002] Dirithromycin is a macrolide antibiotic and a prodrug of erythromycin, used to treat mild and moderate infections caused by sensitive bacteria such as influenzae bacillus, Moraxella catarrhalis, Streptococcus pneumoniae, etc. , Acute exacerbation of chronic bronchitis and other diseases. Its mechanism of action is to inhibit protein synthesis by binding to the 50S ribosomal subunit of sensitive microorganisms. Dirithromycin has an antibacterial spectrum similar to that of erythromycin, and is characterized by excellent pharmacokinetic properties, long half-life, and relatively small adverse reactions. Compared with erythromycin, dirithromycin is more stable to acid, but it is still more sensitive to acidic media, and is easily degraded into erythromycin, which grea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K47/38A61K47/32A61K47/02A61K47/04A61K31/7048A61P31/04
CPCY02A50/30
Inventor 陆纪宏林琳王丽春金鑫谢晏星范珊珊平夏婷
Owner ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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