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Topically applied sustained-release antibiotic preparation

A technology for topical application and antibiotics, applied in the direction of topical antibacterial agents, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The effect of facilitating drug application, reducing the course of treatment, and overcoming limitations

Inactive Publication Date: 2006-12-27
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

[0112] 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 Add 100 ml of dichloromethane to each container, dissolve and mix well, add 10 mg of aztreonam, 10 mg of meropenem, and 20 mg of vancomycin respectively, and prepare 10% aztreonam by spray drying after re-shaking. Nan, 10% meropenem and 20% vancomycin 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 release time of the slow-release injection in physiological saline in vitro is 5-10 days, and the release time in mice subcutaneous is about 10-20 days.

Embodiment 2

[0114] The method steps of processing into sustained-release injections are the same as in Example 1, but the difference is that the antibacterial active ingredients and their weight percentages are: 2-50% of aztreonam, calumonam sodium, imipenem, Cilastine, meropenem, chloramphenicol, thiamphenicol, lindamycin, virginiamycin, clindamycin, infanttoin, trimethoprim, sulfamethazine, omeprene , sulfachlordazine, sulfadiazine, sulfathiazole, sulfisoxazole, vancomycin, vancomycin, norvancomycin, lincomycin, clindamycin, fosfomycin, polymyxin B. Colistin, innovative mycin, novobiocin, bacitracin, sodium fusidate, teicoplanin, liuyangmycin or boramycin.

Embodiment 3

[0116] 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 imipenem, 30mg linopenem, 15mg imipenem and 15mg cleomycin to three containers respectively, re-shake well and use spray drying method to prepare 30% imipenem, 30% lint Microspheres for injection with 15% imipenem and 15% zimycin. 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

Disclosed is a topical applicated antibiotics slow release agent as a slow release injection or a slow release implantation agent, comprising slow release microspheres and menstruum. Said release microsphere comprises slow release assist materials and antibiotics, and said menstruum is a special menstruum comprising suspending agents of sodium carboxymethylcellulose, etc, with a viscosity of 100cp-3000cp(at 20-30 DEG C). Said slow release assist materials are selected from the group of EVAc, polifeprosan, PLA, PLGA, sebacic acid copolymer, albumen glue, gelatin, and etc. Said slow release implantation agent is prepared with slow release microspheres or by melt method, etc. The disclosed slow release agent can release drugs for 10 days by topical applicated or injected at a focus, decreasing whole body toxicity obviously while obtaining and sustaining effective topical drug concentration at the focus.

Description

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

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/427A61K31/407A61K31/357A61K31/37A61K31/7036A61K31/7048A61K31/7056A61K31/665A61K38/14A61K9/10A61K47/32A61K47/34A61K47/38A61K47/36A61K47/10A61K47/26A61P31/02
Inventor 孙晋海
Owner JINAN KANGQUAN PHARMA TECH
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