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Slow-release preparation containing beta-lactamase inhibitor and cephalosporin and its use

A technology of cephalosporin and lactamase, which is applied in the direction of medical preparations containing active ingredients, antibacterial drugs, local antibacterial agents, etc., can solve the problems of increasing dose side effects and difficulty in obtaining effective bactericidal concentration, etc.

Inactive Publication Date: 2006-10-25
JINAN SHUAIHUA 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

[0113] Put 90, 80 and 70 mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20: 80) copolymer into (A), (B) and (C) three Then add 100 milliliters of dichloromethane in each container, after dissolving and mixing, add 10 mg cephalexin, 20 mg sulbactam, 10 mg cephalexin and mg20 sulbactam respectively, shake up again and prepare the mixture containing 10% cephalexin, 20% sulbactam, 10% cephalexin and 20% sulbactam sustained-release 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 400cp-680cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 5-14 days, and the drug release time in mice subcutaneous is about 15-25 days.

Embodiment 2

[0115] 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 percentages by weight are: 1-20% flumoxef sodium, latamoxef sodium, flumoceph, cephalosporin Ampicillin, cephalexin, fluorenated methyl ester, cefprozil, cefpodoxime axetil, cefuroxime, cefuroxime sodium, cefmenoxime, cefaclor, cephradine, cefidine, cefixime, cefixime sodium, cefathiamidine , Cefmetazole, Cefminox Sodium, Cefnicillin Sodium, Cefoperazone Sodium, Cefpiramide, Cefpiramide Sodium, Cefadroxil, Ceftriaxone Sodium, Cefalotin, Cefalotin Sodium, Cefotaxime, Ceftiofur, Ceftiofur Sodium, Ceftiofur Hydrochloride, Cefotaxime Sodium, Ceftazidime, Cefotetan, Cefotetan Disodium, Cefoxitin Sodium, Cefotiam, Cefotaxime, Ceftizoxime, Ceftizoxime Sodium, cefazolin, cefazolin sodium, cefoxadin, cefbuperazone sodium, roracarb, cefepime, cefepime hydrochloride, cefpodoxime axetil, ceftibuten,...

Embodiment 3

[0117] 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 , respectively add 30 mg of tibactam or cefaxenil and 15 mg of tibactam and 15 mg of cefaxenil into three containers, and prepare 30% tibactam or cefaxenil by spray drying method after re-shaking And sustained-release microspheres for injection containing 15% tibactam and 15 mg cephalexin. 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 460cp-660cp (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 14-21 days.

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Abstract

The present invention relates to a slow-released preparation containing beta-lactamase inhibitor and cephalosporin. Said slow-released preparation can be made into antibiotic slow-released injection or slow-released implant preparation. Said injection is formed from slow-released microsphere and solvent, the slow-released microsphere contains slow-released auxiliary material and beta-lactamase inhibitor with antibacterial effective dose and cephalosporin, the solvent is special one containing suspension adjuvant of carboxymethyl cellulose sodium, etc. and its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C). The slow-released auxiliary material is selected from EVAc, polylactic acid copolymer, sebacic acid copolymer, albumin glue and gelatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application method. and can obtain obvious therapeutic effect for curing various infective diseases.

Description

(1) Technical field [0001] The invention relates to a sustained-release preparation containing a β-lactamase inhibitor and a cephalosporin and an application thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release injection and slow-release implant containing cephalosporin and β-lactamase inhibitor, which can be used for treating bacterial infection. The sustained-release preparation is mainly applied locally by injection or placement, and the effective drug concentration is obtained and maintained in the infected local area. (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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/43A61K31/431A61K31/545A61K31/546A61K45/00A61K47/26A61K47/34A61P31/02A61P31/04
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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