Carbostyrile genus antibiotic preparation took orally

A technology for oral preparations of quinolones, which is applied in the field of oral preparations of quinolone antibiotics, can solve problems such as application limitations, and achieve the effects of low toxic and side effects, strong antibacterial effect, and broad antibacterial spectrum

Inactive Publication Date: 2007-12-05
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the increasingly widespread use of fluoroquinolones, certain bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa have developed resistance to existing species headed by ciprofloxacin
In addition, some quinolone varieties have relatively serious side effects, so the clinical application of earlier second-generation or even third-generation quinolone antibiotics has begun to be limited

Method used

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  • Carbostyrile genus antibiotic preparation took orally
  • Carbostyrile genus antibiotic preparation took orally

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Make 1000 oral ordinary tablets with the raw and auxiliary materials in the following weight ratio, with a tablet weight of about 385mg:

[0022] Quinolones Antibiotics 200g

[0023] Pregelatinized starch 50g

[0024] Microcrystalline Cellulose 100g

[0025] 3% HPMC 40% ethanol solution appropriate amount

[0026] Sodium carboxymethyl starch 30g

[0027] Talc powder 3g

[0028] Preparation Process:

[0029] 1. Pulverize the quinolone antibiotic raw material and auxiliary materials respectively, and pass through a 100-mesh sieve.

[0030] 2. The main ingredient is mixed with pregelatinized starch and microcrystalline cellulose in proportion by weight, and soft materials are made with 3% HPMC40% ethanol solution, granulated, and granulated after drying.

[0031] 3. Add sodium carboxymethyl starch and magnesium stearate, mix well, and press into tablets.

Embodiment 2

[0033] 1. Prepare 6% ethanol solution of Opadry enteric coating solution

[0034] 2. Take the plain tablet obtained in Example 1 and pour it into a coating pan for coating to obtain an enteric-coated tablet. Coating powder relative to tablet core weight gain: 4.0-5.0%.

Embodiment 3

[0036] Make 1000 oral ordinary tablets with the raw and auxiliary materials in the following weight ratio, with a tablet weight of about 220mg:

[0037] Quinolones Antibiotics 100g

[0038] 20g pregelatinized starch

[0039] Microcrystalline Cellulose 80g

[0040] 3% HPMC 40% ethanol solution appropriate amount

[0041] Sodium carboxymethyl starch 15g

[0042] Magnesium Stearate 2g

[0043] Preparation Process:

[0044] 1. Pulverize the quinolone antibiotic raw material and auxiliary materials respectively, and pass through a 100-mesh sieve.

[0045] 2. The main ingredient is mixed with pregelatinized starch and microcrystalline cellulose in proportion by weight, and soft materials are made with 3% HPMC40% ethanol solution, granulated, and granulated after drying.

[0046] 3. Add sodium carboxymethyl starch and magnesium stearate, mix well, and press into tablets.

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PUM

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Abstract

The present invention provides one kind of orally taken quinolone antibiotic preparation, which contains quinolone antibiotic, its salt or their hydrate, and may be prepared into tablet, dispersed tablet, coated tablet, enteric coated tablet, slow released tablet, capsule or granule. The quinolone antibiotic preparation has dosage of 20-1000 mg, and contains stuffing in 10-60 wt% and disintegrant in 5-30 wt%. Quinolone antibiotic has phamacodynamic activity similar to that of levofloxacin, and possesses broad antibiotic spectrum, less toxic side effect and other advantages. The quinolone antibiotic preparation is stable, controllable, easy in taking, safe and effective.

Description

technical field [0001] The invention relates to an oral preparation of quinolone antibiotics. Background technique [0002] Since the first quinolone synthetic antibiotics came into the market in the 1960s, such drugs have been developed rapidly. However, with the increasingly widespread use of fluoroquinolones, certain bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa have developed resistance to existing varieties led by ciprofloxacin. In addition, some quinolones have serious side effects. Therefore, the clinical application of earlier second-generation or even third-generation quinolone antibiotics has begun to be limited. Contents of the invention [0003] In order to solve the above problems, the present invention provides an oral preparation of quinolone antibiotics obtained by adding amino groups based on levofloxacin. [0004] In order to make the quinolone antibiotics into oral preparations convenient for clinical use, the present invention adop...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K9/14A61K31/5383A61P31/04
Inventor 严明
Owner 严明
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