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Sustained-release injection containing antibiotic doxycycline and uses thereof

A slow-release injection, doxycycline technology, applied in the direction of antibacterial drugs, tetracycline active ingredients, pharmaceutical formulations, etc., can solve the problems of difficult to obtain effective bactericidal concentration, increase dose side effects, etc., to facilitate drug application and reduce the course of treatment. , the effect of reducing complications

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 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 the mixture again and spray-dry to prepare 10% Flaxacin, 10% cephalexin and 20% Tylosin microspheres for injection. Then the microspheres are 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 , Respectively add 30mg lincomycin, 30mg doxycycline, 15mg lincomycin and 15mg doxycycline into three containers, shake well and spray-dry to prepare 30% lincomycin, 30% doxycycline Microspheres for injections containing 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 relates to a slow-release formulation containing vibramycin 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 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-release formulation 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 vibramycin 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 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): A61K9/08A61K9/10A61K9/00A61K31/65A61K47/34A61P31/04A61K47/26
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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