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Sustained-release agent containing penicillins antibiotics and uses thereof

A technology of antibiotics and penicillin, which is applied in the field of medicine, can solve the problems of side effects of increasing doses, 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: 2008-11-12
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

[0111] 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 Add 100 milliliters of dichloromethane to each container, dissolve and mix well, add 10 mg carboxyphene penicillin, 10 mg flucloxacillin, and 20 mg mezlocillin respectively, and prepare 10% carboxylicin by spray drying after re-shaking. Thiophene penicillin, 10% flucloxacillin and 20% mezlocillin 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 350cp-550cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 6-12 days, and the drug release time in mice subcutaneous is about 14-22 days.

Embodiment 2

[0113] 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:

[0114] (1) 2-50% of penicillin, penicillin V, carboxyphene penicillin, procaine penicillin, nodosaur penicillin, carbapenem penicillin antibiotics, penicillin penicillin antibiotics, thiamycin, sulbenicillin, sulbenicillin sodium, furubicillin, ticarcillin, droperazine penicillin, oxypiperazine penicillin, mecillin, heptacillin, or heptacillin potassium;

[0115] (2) 2-50% of apacillin sodium, pimecillin, azlocillin, azlocillin sodium, apoxicillin, amcloxacillin sodium, azidecillin, flucloxacillin, flucloxacillin sodium, penicillin Alkanoic acid, varacillin sodium, oxacillin sodium, 1,3,4-thiadiazole carbapenem compound, methicillin or cloxacillin sodium;

[0116] (3) 2-50% oxacillin, oxacillin sodium, o-cloxacillin sodium, amoxicillin, piperacillin, piperacillin sodium, heba...

Embodiment 3

[0119] 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 ampicillin, 30mg carbenicillin, 30mg mezlocillin into three containers respectively, shake again and prepare injection containing 30% ampicillin, 30% carbenicillin, 30% mezlocillin by spray drying method Use microspheres. 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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PUM

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Abstract

The invention discloses a sustained release injection containing penicillin antibiotics, which consists of sustained release microspheres and menstruum, wherein, the sustained release microspheres contain sustained release excipient and penicillin antibiotics, the menstruum is special menstruum containing suspending agents such as sodium carboxymethyl cellulose and so on, and the viscosity is between 100 and 3000cp (at the temperature of between 20 and 30 DEG C); the sustained release excipient is selected from EVAc, polifeprosan, PLA, PLGA, decanedioic acid copolymers, albumin glue, gelatin and so on; and the sustained release microspheres can also be prepared into sustained release implant. The sustained release implant and the sustained release injection are locally placed or injected on a bacteria focus, which can slowly release medicine at a local lesion for 5 to 30 days and apparently decrease the systemic toxicity of the medicine when the effective medicine concentration of the local lesion is effectively obtained and maintained. The sustained release injection has a remarkable and unique treatment effect on infections caused by staphylococcus, streptococcus, peptostreptococcus, acne propionate bacillus, enterobacter, tubercle bacillus, gonococcus or meningococcus and so on, particularly on local lesions such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot and femoral head necrosis of diabetes, and various abscesses and so on.

Description

(1) Technical field [0001] The invention relates to a slow-release agent containing penicillin antibiotics and an application thereof, belonging to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing penicillin 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 penicillin, 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 treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/10A61K9/00A61K31/55A61K31/431A61K47/30A61P31/04
Inventor 孔庆忠贺润平栾永祖
Owner SHANDONG LANJIN PHARMA
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