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Slow release formulation containing antibiotic and its uses

A technology for antibiotics and sustained-release injections, applied in the field of sustained-release preparations, sustained-release injections containing antibiotics and sustained-release implants, can solve the problems of increased dose side effects, difficulty in obtaining effective bactericidal concentrations, etc. The effect of convenient drug application and cost reduction

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 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 Then add 100 milliliters of dichloromethane to each container, after dissolving and mixing, add 10 mg dafloxacin, 10 mg cephalexin, and 20 mg tylosin respectively, and prepare 10% Dafloxacin containing 10% Dafloxacin by spray drying method after re-shaking Flufloxacin, 10% cephalexin and 20% Tylosin 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 300cp-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 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:

[0115] (1) 2-50% apramycin, betamycin, dafloxacin, lincomycin, spectinomycin, doxycycline or streptomycin;

[0116] (2) 2-50% penicillin, difloxacin, aureomycin, carbadol, cloxacillin, marbofloxacin or pemafloxacin;

[0117] (3) 2-50% pilimycin, safloxacin, enunomycin, tylosin, cephalexin, ceftiofur or neomycin; or

[0118] (4) 2-50% salinomycin, novobiocin, ibafloxacin, gentamicin sulfate, sulfadiazine or sulfisoxazole.

Embodiment 3

[0120] 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 lincomycin, 30mg doxycycline, 15mg lincomycin and 15mg doxycycline to three containers respectively, re-shake and use spray drying method to prepare 30% lincomycin, 30% doxycycline Injectable microspheres containing lincomycin, 15% lincomycin and 15% doxycycline. 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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Abstract

The invention relates to a slow-releasing agent or rslow-releasing implanting agent containing antibiotics. The injection comprises slow-releasing micro-sphere and dissolvent. The slow-releasing micro-sphere contains slow-releasing findings and antibiotics, and dissolvent contains suspending adjuvant agent such as sodium carboxymethyl cellulose with the adhesive degree being 100cp-3000cp (at 20-30 Deg. C). The slow-releasing findings comprises EVAc, polyphenyl, PLA, PLGA, decanedioic acid copolymer, albumen glue and gelatin; the slow-releasing implanting agent is prepared with slow-releasing micro-sphere or through other methods. When said antibiotics is placed or injected into bacteria, the medicine can be released slowly for more than 10 days, and toxicity is dramatically reduced at the same time when effective medicine concentration is got and maintained. The said slow-releasing agent is specially effective for chronic medullitis, bedsore, intractable ulcer on skin, diabetes femoral head necrosis and other abscessus, which are caused by Staphylococcus, Streptococcus, Streptococcus, acne Propionibacteriaceae, Enterobacter, Enterobacter, gonotoxin or parameningococcus.

Description

(1) Technical field [0001] The invention relates to an antibiotic-containing slow-release agent and application thereof, belonging 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/415A61K31/43A61K31/431A61K31/505A61K31/70A61K31/7028A61K31/7036A61K31/7048
Inventor 孔庆忠刘恩祥张婕
Owner SHANDONG LANJIN PHARMA
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