A sustained release injection containing cephalosporin and application thereof

A technology of slow-release injections and cephalosporins, which is applied in the field of medicine, can solve the problems of increasing doses of side effects, difficulty in obtaining effective bactericidal concentrations, etc., and achieve the effects of reducing the course of treatment, facilitating drug application, and reducing costs

Inactive Publication Date: 2006-12-20
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, 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

[0107] 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

[0109] 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:

[0110] (1) 2-50% flumoxef, latamoxef, flumoceph, cephalexin, cefprozil, cefuroxime, cefmenoxime, cefaclor, cephradine, cefixime, cefathiamidine, cefmetrex azole or cefminox;

[0111] (2) 2-50% of cefonicil, cefoperazone, cefpiramide, cefadroxil, ceftriaxone, cephalothin, cefotaxime, cefotaxime, ceftazidime, cefotetan, cefoxitin or cephalosporin For security;

[0112] (3) 2-50% of ceftizoxime, cefazolin, cefoxadin, cefbuperazone, loracarbef, cefepime, ceftibuten, cefdinir, cefodizime, ceflecin or cefuroxime Odd; or

[0113] (4) 2-50% of cefamandole, cefpirome, ceftazidime, cefditoren, cefacetonitrile, ceftizonam or fusidic acid.

Embodiment 3

[0115] 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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PUM

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Abstract

The invention relates to a release injection which contains cefradine, wherein it is formed by release micro ball and dissolvent; the release micro ball contains release findings and penicillin antibiotic; the dissolvent is the special one contains sodium carboxymethyl cellulose as suspension agent; the viscosity is 100cp-3000cp (20Deg. C-30Deg. C); the release agent is selected from EVAc, polyphenyl, PLA, PLGA, sebacic acid polymer, protein pastern, and dope; the release micro ball can be made into release implant agent; the release implant agent and release injection is laid on bacteria stove or injected, to release the medicine for 5-30 days, to keep the effective medicine density and reduce the whole toxicity. The invention can be used to cure the infection caused by staphylococcus, streptococcus, etc.

Description

(1) Technical field [0001] The invention relates to a cephalosporin-containing sustained-release injection and an application thereof, belonging 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, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/545A61K9/10A61K47/42A61K47/38A61K47/36A61K47/30A61K47/26A61K47/10A61P31/04A61P31/06A61P17/00A61P15/14A61P11/04A61P11/02A61P11/00A61P13/12A61P15/00A61P27/02A61P27/06A61P1/02A61P1/16A61P19/02A61P29/00
Inventor 刘玉燕
Owner JINAN SHUAIHUA PHARMA TECH
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