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Antibiotic slow-release preparation for local use

A local application and sustained-release preparation technology, which is applied in the field of sustained-release injections, sustained-release implants, and sustained-release preparations of antibiotics. It can solve the problems of difficult to obtain effective bactericidal concentration, increase the dose and side effects, and achieve convenient drug application. , reduce the course of treatment, and reduce the effect of drug tolerance

Inactive Publication Date: 2006-10-25
JINAN KANGQUAN 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

[0107] 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 in each container, after dissolving and mixing, add 10 mg demeclocycline, 20 mg metacycline, and 30 mg polymycin respectively, and prepare 10 mg polymycin by spray drying method after shaking up again. % demeclocycline, 20% metacycline, 30% polymycin 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 450cp-600cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 5-15 days, and the drug release time in mice subcutaneous is about 12-20 days.

Embodiment 2

[0109] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the contained antibacterial active ingredient and its weight percentage are: 2-50% demeclocycline, metacycline, polymycin, tetracycline , Doxycycline, Guanacycline, Lysinetetracycline, Hydropyrrocycline, Minocycline, Demeclocycline, Minotetracycline, Oxytetracycline, Oxytetracycline, Deoxyoxytetracycline, Doxycycline Hydrochloride oxytetracycline hydrochloride, nystatin, sulbactam, sultacillin, potassium clavulanate, ticarcillin, clavulanic acid, sulbactam sodium, tibactam, or tementine.

Embodiment 3

[0111] 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 doxycycline, guanacycline or lysine tetracycline to three containers respectively, re-shake and prepare 30% doxycycline, guanacycline or lysine tetracycline by spray drying method microspheres for injection. 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 present invention relates to a slow-released preparation of antibiotic for local application, it is slow-released injection or slow-released implant preparation. The injection is composed of slow-released microspheres and solvent, the slow-released microsphere contains slow-released auxiliary material and beta-lactamase inhibitor or tetracyclines, the solvent is a special solvent containing suspension adjuvant of sodium cellulose glycollate, etc. its viscosity is 100 cp -3000 cp (20-30 deg.C), the slow-released auxiliary material is selected from EVAc, PLA, PLGA, sebacic acid copolymer, albumin glue and gelatin. The slow-released implant preparation is prepared by using slow-released microspheres or adopting melting process. Said invention also provides its application range.

Description

(1) Technical field [0001] The invention relates to a sustained-release preparation of locally applied antibiotics, which belongs to the technical field of medicines. Specifically, the present invention provides a slow-release injection and slow-release implant containing tetracycline antibiotics or β-lactamase inhibitors. 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 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 become chronic lesions. On the one hand, the treatment of drug-resistant patients or recurrent chronic lesions will prolong t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/43A61K31/4704A61K31/65A61P31/02
Inventor 孙中先
Owner JINAN KANGQUAN PHARMA TECH
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