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Sustained-release agent containing TIC and use thereof

A technology of carboxythiophene penicillin and penicillin, which is applied in the field of sustained-release agents, can solve the problems of difficulty in obtaining effective bactericidal concentration, increased dosage and side effects, and achieve the effects of facilitating drug application, reducing the course of treatment, and reducing drug tolerance

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

A sustained release preparation containing ticarcillin consists of sustained release microsphere and dissolvant, wherein the sustained release microsphere contains sustained release auxiliary materials and penicillins antibiotic; the dissolvant is special dissolvant containing suspending agents such as sodium carboxymethyl cellulose, and the viscosity of the dissolvant is 100 to 3,000 cp (at a temperature of between 20 and 20 DEG C); the sustained release auxiliary materials are selected from EVAc, Polifeprosan, PLA, PLGA, sebacic acid copolymer, albumin glue and gelatin, etc.; the sustained release microsphere can also be made into a sustained release implantation agent. The sustained release implantation agent and sustained release injection can be partly placed or injected into a bacteria focus so as to slowly release medicine over local bacteria focus for 5 to more than 30 days, thereby obviously reducing whole-length toxicity while effectively obtaining and maintaining the effective drug concentration of local focus. The sustained release preparation has remarkable and unique therapeutic effects in curing infections caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococcus or meningococcus, etc., and local focuses in particular such as chronic osteomyelitis, severe bedsore, intractable skin ulcer, diabetic foot, femoral head necrosis and various abscesses.

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