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Slow-release preparation containing beta-lactamase inhibitor and its use

A technology of lactamase and sustained-release preparations, applied in the field of sustained-release injections, sustained-release implants, and sustained-release preparations, can solve the problems of difficulty in obtaining an effective bactericidal concentration, increasing doses and side effects, etc.

Inactive Publication Date: 2006-10-25
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

[0113] Put 90, 80 and 70 mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20: 80) copolymer into (A), (B) and (C) three Then add 100 milliliters of dichloromethane to each container, after dissolving and mixing, add 10 mg ampicillin, 20 mg sulbactam, 10 mg ampicillin and mg20 sulbactam respectively, shake up again and use the spray drying method to prepare the mixture containing 10% ampicillin, 20% sulbactam, 10% ampicillin and 20% sulbactam sustained-release 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 400cp-680cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 5-14 days, and the drug release time in mice subcutaneous is about 15-25 days.

Embodiment 2

[0115] The method steps of being processed into sustained-release injections are the same as in Example 1, but the difference is that the contained antibacterial active ingredients and their weight percentages are: 1-20% penicillin, penicillin V, carboxyphene penicillin, procaine penicillin, Benzathine Penicillin, Carbapenem Penicillin Antibiotics, Penicillin Penicillin Antibiotics, Thiamycin, Sulbenicillin Sodium, Furbusillin, Dropperazine Penicillin, Oxypiperazine Penicillin, Mecillin, Hetacillin Potassium, Apacillin sodium, pimacillin, azlocillin, azlocillin sodium, apoxicillin, amcloxacillin sodium, azidecillin, flucloxacillin, flucloxacillin sodium, penicillanic acid, valocillin sodium, Oxacillin sodium, 1,3,4-thiadiazole carbapenem compound, methicillin, cloxacillin sodium, oxacillin, oxacillin sodium, o-cloxacillin sodium, ampicillin, amoxicillin, Piracillin, piperacillin sodium, hebapenicillin V, heptacillin, cyclohexicillin, sulbenicillin, carficillin, carindencillin,...

Embodiment 3

[0117] 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 30 mg of Tybactam or carbenicillin and 15 mg of Tybactam and 15 mg of carbenicillin to three containers respectively, and prepare 30% Tybactam or carbenicillin by spray drying method after re-shaking And sustained-release microspheres for injection containing 15% Tybactam and 15 mg carbenicillin. 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 460cp-660cp (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 14-21 days.

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PUM

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Abstract

The present invention relates to a slow-released preparation containing beta-lactamase inhibitor. Said slow-released preparation can be made into antibiotic slow-released injection or slow-released implant preparation. Said injection is formed from slow-released microsphere and solvent, said slow-released microsphere contains slow-released auxiliary material and beta-lactamase inhibitor with antibacterial effective dose and penicillin antibiotics, the solvent is special solvent containing suspension adjuvant of carboxymethyl cellulose sodium, etc. its viscosity is 100 cp-3000 cp (20 deg.C-30deg.C); the slow-released auxiliary material is selected from EVAc, polylactic acid copolymer, sebacic acid copolymer, albumin glue and glatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application range and can obtain obvious therapeutic effect for curing various infective diseases.

Description

(1) Technical field [0001] The invention relates to a sustained release preparation containing β-lactamase inhibitors and penicillin antibiotics and application thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release injection and slow-release implant containing penicillin antibiotics and β-lactamase inhibitors, which can be used to treat bacterial infections. The sustained-release preparation is mainly applied locally by injection or placement, and the effective drug concentration is obtained and maintained in the infected local area. (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 becom...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/43A61K31/431A61K45/00A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P31/02A61P31/04
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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