Sustained-release injection containing antibiotic sarafloxacin and uses thereof

A slow-release injection, safloxacin technology, applied in the field of medicine, can solve the problems of difficulty in obtaining an effective bactericidal concentration, increase the dose and side effects, etc., and achieve the effects of facilitating drug application, reducing the course of treatment, and overcoming limitations.

Inactive Publication Date: 2008-10-08
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 ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] 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

[0112] 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:

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

[0114] (2) 2-50% penicillin, difloxacin, aureomycin, carbadol, cloxacillin, marbofloxacin or pemafloxacin;

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

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

Embodiment 3

[0118] 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-release formulation containing sarafloxacin as antibiotic, which is slow-released injection or slow-released implant; the injection is composed of a slow-released microsphere and dissolvent; the slow-released microsphere contains a slow-released adjuvant and the antibiotic; the dissolvent is a special dissolvent containing suspending agent such as sodium carboxymethylcellulose, etc. and the viscosity of the dissolvent is 100cp-3000cp (at the temperature of 20 DEG C-30 DEC C); the slow-released adjuvant is selected from EVAc, polifeprosan, PLA, PLGA, sebacic acid copolymer, albumen glue, gelatin, etc.; the slow-released implant is prepared with the slow-released microsphere or by other methods. The slow-released implant can be partially placed or injected in a bacterial focus to release medicine on a partial disease focus for more than 10 days slowly; valid medicine concentration on the partial focus is obtained and maintained effectively, at the same time toxicity of an entire body is remarkably reduced. The slow-release formulation containing the sarafloxacin as the antibiotic has remarkable and special treatment effect on infection caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococci and meningococcus, etc., and particularly the partial focus such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot, femoral head necrosis and various abscesses, 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): A61K9/08A61K9/10A61K9/00A61K31/496A61K47/30A61P31/04
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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