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Slow-release preparation containing macrolides anti biotics

A macrolide and antibiotic technology, which is applied in the directions of medical preparations containing active ingredients, topical antibacterial agents, and medical preparations with non-active ingredients, etc. problems, to achieve the effect of facilitating drug application, reducing the course of treatment, and shortening the treatment time

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

[0102] Put 90, 80 and 70 mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20: 80) copolymer into (A), (B) and (C) three Add 100 milliliters of dichloromethane to each container, dissolve and mix well, add 10 mg midecamycin, 20 mg roxithromycin, and 30 mg clarithromycin respectively, and prepare 10% Midecamycin, 20% roxithromycin, and 30% clarithromycin 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

[0104] 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 percentage by weight are: 2-50% carboxycin, metronidazole, erythromycin, erythromycin erythromycin Ethromycin, erythromycin ethyl succinate, kitamycin, midecamycin, acetyl midecamycin, josamycin, roxithromycin, melelamycin, clarithromycin, azithromycin, azithromycin, rotamycin Spiramycin, spiramycin, acetylspiramycin, monoacetylspiramycin, diacetylspiramycin, oleandomycin, midecamycin acetate, dirithromycin, clarithromycin, roxamicin, lactose erythromycin stearate or erythromycin stearate.

Embodiment 3

[0106] 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 of spiramycin, rotamycin and azithromycin to three containers respectively, reshake and prepare 30% spiramycin, rotamycin and azithromycin 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 containing macrolide antibiotics. Said slow-released preparation is slow-released injection or slow-released implant preparation. Said injection is composed of slow-released microsphere and solvent, said slow-released microsphere contains slow-released auxiliary material and macrolide antibiotics, the solvent is special solvent containing suspension adjuvant of carboxymethyl cellulose sodium, its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C); the slow-released auxiliary material is selected from EVAc, PLA, PLGA, sebacic acid copolymer, albumin glue and golatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application method, and can obtain obvious therapeutic effect for curing various infective diseases.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent containing macrolide antibiotics, which belongs to the technical field of medicines. Specifically, the invention provides a slow-release injection and a slow-release implant containing macrolide 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 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 the treatment time, and on the other han...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4164A61K31/7048A61K31/7052A61K45/00A61K47/34A61P31/02A61P31/04
Inventor 李士兰
Owner JINAN KANGQUAN PHARMA TECH
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