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Slow release injection containing cefradine

A technology for sustained-release injections and cephalosporins, which is used in medical preparations containing active ingredients, antibacterial drugs, and medical preparations with non-active ingredients, etc. problems, to achieve the effect of facilitating drug application, reducing the course of treatment, and reducing drug tolerance

Inactive Publication Date: 2006-10-11
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, many new antibacterial drugs, especially cephalosporins, have shown good efficacy. However, for many chronic lesions, especially local lesions, it is difficult to obtain an effective bactericidal concentration by 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

[0109] Put 90, 90 and 80 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymers into (A), (B) and (C) three Then add 100 milliliters of dichloromethane to each container, after dissolving and mixing, add 10 mg of fluoxetin, 10 mg of cephalothin, and 20 mg of cefazolin respectively, and prepare 10% fluoride containing fluoride by spray drying method after shaking up again. cephalosporin, 10% cephalothin and 20% cefazolin 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 350cp-550cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 7-14 days, and the drug release time in mice subcutaneous is about 15-25 days.

Embodiment 2

[0111] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that contained antibacterial active ingredient and weight percentage thereof are:

[0112] (1) 2-50% flumoxef, latamoxef, flumoceph, cephalexin, cefprozil, cefuroxime, cefmenoxime, cefaclor, cephradine, cefixime, cefathiamidine, cefmetrex azole or cefminox;

[0113] (2) 2-50% of cefonicil, cefoperazone, cefpiramide, cefadroxil, ceftriaxone, cephalothin, cefotaxime, cefotaxime, ceftazidime, cefotetan, cefoxitin or cephalosporin For security;

[0114] (3) 2-50% of ceftizoxime, cefazolin, cefoxadin, cefbuperazone, loracarbef, cefepime, ceftibuten, cefdinir, cefodizime, ceflecin or cefuroxime Odd; or

[0115] (4) 2-50% of cefamandole, cefpirome, ceftazidime, cefditoren, cefacetonitrile, ceftizonam or fusidic acid.

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 , add 30mg cephalexin, 30mg cefaclor, and 30mg cefuroxime into three containers respectively, shake up again and prepare injection containing 30% cephalexin, 30% cefaclor, and 30% cefuroxime by spray drying method Use microspheres. 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 500cp-650cp (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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Abstract

Disclosed is a slow release injection containing cephalosporin, which comprises slow release microballoons and dissolvent, wherein the slow release microballoons include slow release auxiliary materials and cephalosporin, the dissolvent being specific one containing suspension adjuvant such as sodium carboxymethyl cellulose, the slow release auxiliary materials are selected from EVAc, PLA, PLGA, sebacylic acid copolymer, albumen glue or gelatin, the slow release microballoons can also be made into slow release implantation agent or ointment.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing cephalosporin, which belongs to the technical field of medicines. Specifically, the invention provides a cephalosporin-containing sustained-release injection and sustained-release implant. 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 chronic lesions will prolong the treatment time, and on the other hand, i...

Claims

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Application Information

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IPC IPC(8): A61K31/545A61K9/08A61K47/42A61K47/38A61K47/30A61P31/04A61K47/32A61K47/34
Inventor 孔庆忠张红军邹会凤
Owner SHANDONG LANJIN PHARMA
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