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Slow-release preparation containing quinolones antibiotics

A technology of quinolones and antibiotics, applied in the direction of anti-inflammatory agents, antibacterial drugs, non-central analgesics, etc., can solve the problems of difficult to obtain effective bactericidal concentration, increase dose side effects, etc., to facilitate the application of drugs and reduce the course of treatment , the effect of shortening the treatment time

Inactive Publication Date: 2006-10-25
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, many new antibacterial drugs have shown good curative effect. However, for many chronic lesions, especially local lesions, it is difficult to obtain an effective bactericidal concentration with conventional therapy.
Increased dose or long-term use of drugs will have many side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Put 90, 80 and 70 mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20: 80) copolymer into (A), (B) and (C) three In two containers, add 100 milliliters of dichloromethane to each, after dissolving and mixing, add 10 mg pazufloxacin, 20 mg ciprofloxacin, and 30 mg fleroxacin respectively, re-shake and use spray-drying method to prepare 10% Pazufloxacin, 20% ciprofloxacin, 30% fleroxacin microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 450cp-600cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 5-15 days, and the drug release time in mice subcutaneous is about 12-20 days.

Embodiment 2

[0106] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the contained antibacterial active ingredients and their weight percentages are: 2-50% of Pazufloxacin, Ciprofloxacin, Clinfloxacin, and Fleroxacin , cillofloxacin, levofloxacin, enoxacin, grafloxacin, tosufloxacin, amfloxacin, lomefloxacin, R-lomefloxacin, prefloxacin, orbimycin, Prulifloxacin, Olafloxacin, Cadrifloxacin, Alatrafloxacin, Gatifloxacin, Moxifloxacin, Gemifloxacin, Sitafloxacin, Nilefloxacin, Norfloxacin, Danoxacin , enrofloxacin, difloxacin, marbofloxacin, pemafloxacin, safloxacin, ibafloxacin, rufloxacin, tosufloxacin, pefloxacin, or spafloxacin .

Embodiment 3

[0108] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 10,000 into three containers (A), (B) and (C) respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well , add 30mg of ciloxacin, levofloxacin and enoxacin to three containers respectively, re-shake and use spray drying method to prepare 30% ciloxacin, levofloxacin and enoxacin Microspheres for Injection of Floxacin. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 400cp-600cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 7-15 days, and the drug release time in mice subcutaneous is about 15-25 days.

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PUM

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Abstract

The present invention relates to an antibiotic slow-released preparation containing quinolones, including slow-released injection or slow-released implant preparation. Said injection is formed from slow-released microsphere and solvent, the slow-released microphere contains slow-released auxiliary material and antibiotic, the solvent is special solvent containing suspension adjuvant of sodium cellulose glycollate, its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C), the slow-released auxiliary material is selected from EVAc, PLA, PLGA, sebacic aid copolymer, albumin glue and gelatin. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Besides, said invention also provides its application range for curing various diseases.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent containing quinolone antibiotics, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing a sustained-release formulation of quinolone or naphthyridone antibiotics. The sustained-release agent is mainly applied locally, and can obtain and maintain effective drug concentration in the local area of ​​bacterial infection. (2) Background technology [0002] With the advent of antibiotics, bacterial infection became a treatable disease. However, because the treatment is not standardized and the treatment time is long, many patients may forget to dose the medicine in time, which often leads to the emergence of drug resistance. Many bacterial infections that should have been cured have recurred and become chronic lesions. On the one hand, the treatment of drug-resistant patients or recurrent...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/47A61K47/30A61P29/00A61P31/04
Inventor 王明华
Owner JINAN KANGQUAN PHARMA TECH
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