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Sustained-release injection containing antibiotic

A technology of slow-release injections and antibiotics, applied in the field of medicine, can solve the problems of difficulty in obtaining effective bactericidal concentration and side effects of increasing doses, so as to facilitate the application of medicines, reduce the course of treatment, and enhance the effect of treatment

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 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

[0110] Put 90, 90 and 80 mg of polystyrene (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into (A), (B) and (C) three Then add 100 ml of dichloromethane to each container. After dissolving and mixing, add 10 mg of danofloxacin, 10 mg of cephalexin, and 20 mg of tylosin. Shake again and spray-dry to prepare a 10% content of Dafloxacin. Flaxacin, 10% cephalexin and 20% Tylosin injection microspheres. Then the microspheres were suspended 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℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 5-10 days, and the release time under the skin of mice is about 10-20 days.

Embodiment 2

[0112] The process of processing into a sustained-release injection is the same as in Example 1, but the difference is that the antibacterial active ingredient and its weight percentage are:

[0113] (1) 2-50% apramycin, blebomycin, danofloxacin, lincomycin, spectinomycin, doxycycline or streptomycin;

[0114] (2) 2-50% Penicillin, Difloxacin, Chlortetracycline, Carbadol, Cloxacillin, Mabofloxacin or Pemafloxacin;

[0115] (3) 2-50% pyrithromycin, safloxacin, ennomycin, tylosin, cephalexin, ceftiofur or neomycin; or

[0116] (4) 2-50% salinomycin, novobiocin, ibafloxacin, gentamicin sulfate, sulfadiazine or sulfisoxazole.

Embodiment 3

[0118] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 10000 into three containers (A), (B) and (C), and then add 100 ml of dichloromethane to each, dissolve and mix well , Add 30mg lincomycin, 30mg doxycycline, 15mg lincomycin and 15mg doxycycline into three containers respectively, shake up again and use spray drying method to prepare 30% lincomycin, 30% doxycycline Microspheres for injection of vitamin C, 15% Lincomycin and 15% Doxycycline. The dried microspheres were suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding suspension type sustained-release injection. The viscosity of the injection is 400cp-600cp (at 20℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 7-15 days, and the release time under the skin of mice is about 15-25 days.

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Abstract

The invention provides a sustained-release injection or sustained-release implant containing antibiotics. 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 the 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 and abscess.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing antibiotics and an application thereof, and belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing antibiotics. The sustained-release agent is mainly applied locally, which can obtain and maintain an effective drug concentration in the local area of ​​bacterial infection. (2) Background technology [0002] With the advent of antibiotics, bacterial infections have become a treatable disease. However, due to non-standard treatment and long treatment time, many patients may forget to administer the medication in time, which often leads to the development of drug resistance. Many bacterial infections that should have been cured recur 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/10A61K9/00A61K31/7056A61K31/65A61K47/34A61P31/04
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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