Sustained-release agent containing sulbenicillin and uses thereof

A technology of sulfobenicillin and sustained-release injections, applied in the field of sustained-release preparations, can solve the problems of increasing dose side effects, difficult to obtain effective bactericidal concentration, etc., and achieve the effects of reducing the course of treatment, facilitating the application of drugs, and enhancing the therapeutic effect.

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 dif

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0110] Example 1.

[0111] 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 carboxythiophene penicillin, 10 mg of flucloxacillin, and 20 mg of mezlocillin. Shake again and spray-dry to prepare a 10% carboxyl Thiphenicillin, 10% flucloxacillin and 20% mezlocillin injection microspheres. 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 350cp-550cp (at 20℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 6-12 days, and the release time under the skin of mice is about 14-22 days.

Example Embodiment

[0112] Example 2.

[0113] 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:

[0114] (1) 2-50% of penicillin, penicillin V, carboxythiophene penicillin, procaine penicillin, jellyfish penicillin, carbapenem penicillin antibiotics, penicillin penicillin antibiotics, thiomycin, sulfbenicillin, Sulbenicillin Sodium, Furbuscillin, Ticarcillin, Dropperazine, Oxypiperazine, Mecillin, Metacillin, or Metacillin potassium;

[0115] (2) 2-50% of apacillin sodium, pimecillin, azlocillin, azlocillin sodium, apocillin, ampicillin sodium, aziridin, flucloxacillin, flucloxacillin sodium, penicillin Alkanoic acid, valrocillin sodium, oxacillin sodium, 1,3,4-thiadiazole carbapenem compound, methicillin or cloxacillin sodium;

[0116] (3) 2-50% of oxacillin, oxacillin sodium, o-cloxacillin sodium, amoxicillin, peracillin, piperacillin sodium, heba penicillin V, cycl...

Example Embodiment

[0118] Example 3.

[0119] 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 ampicillin, 30mg carbenicillin, 30mg mezlocillin into three containers, shake well and spray dry to prepare injections containing 30% ampicillin, 30% carbenicillin, 30% mezlocillin Use microspheres. 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

A sustained release preparation containing sulbenicillin 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 30 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): A61K9/08A61K9/10A61K9/00A61K31/43A61K31/431A61K47/30A61P31/04
Inventor 孔庆忠贺润平栾永祖
Owner SHANDONG LANJIN PHARMA
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