Sustained-release injection containing antibiotic and application thereof

A technology of slow-release injections and antibiotics, applied in the field of medicine, can solve the problems of increased dose side effects, difficulty in obtaining effective bactericidal concentration, etc., and achieve the effects of reducing the course of treatment, facilitating drug application, and reducing costs

Inactive Publication Date: 2008-10-15
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 dif

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 provides a sustained-release injection or sustained-release implant containing tylosin antibiotic. The sustained-release injection comprises sustained-release microspheres and solvent. The microspheres contain sustained-release adjuvants and antibiotics, and the solvent is a special solvent containing suspending agent such as sodium carboxymethylcellulose and having viscosity of 100-3000cp (20-30 DEG C); and the sustained-release adjuvants are selected from poly(ethylene-co-vinylacetate) (EVAc), polifeprosan, poly(lactic acid) (PLA), poly(lactic-co-glycolic acid) (PLGA), sebacic acid copolymer, albumin glue and gelatin. The sustained-release implant is made from microspheres or by other methods. The sustained-release implant or injection can be locally placed or injected into foci to locally sustained-release of drug for more than 10 days, so as to obtain and maintain local drug effective concentration while remarkably reduce the systemic toxicity of the drug. The sustained-release injection has distinct and unique therapeutic effect on local infection diseases caused by Staphylococci, Streptococci, Peptostreptococcus, Propionibacterium acnes, Enterobacter, Mycobacterium tuberculosis, Gonococcus or Meningococcus, such as chronic osteomyelitis, severe decubital ulcer, refractory skin ulcer, diabetic foot, femoral head necrosis, abscess, etc.

Description

(1) Technical field [0001] The invention relates to an antibiotic-containing sustained-release injection and an 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 ot...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K31/7048A61K47/30A61P31/04
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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