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Slow-release injecta containing amino glucosides antibiotics and use thereof

A technology of sustained-release injections and aminoglycosides, applied in the field of sustained-release injections, which can solve the problems of increased dose side effects, difficulty in obtaining effective bactericidal concentrations, etc., and achieve the effects of reducing the course of treatment, facilitating drug application, and reducing costs

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, there are many new antibacterial drugs, especially aminoglycoside antibiotics, which 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

[0098] 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 In two containers, add 100 milliliters of dichloromethane to each, after dissolving and mixing, add 10 mg arbekacin, 10 mg amikacin, and 20 mg asmitacin respectively, shake them up again, and use spray-drying method to prepare the mixture containing 10% arbekacin, 10% amikacin and 20% asmitacin 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 7-14 days, and the drug release time in mice subcutaneous is about 15-25 days.

Embodiment 2

[0100] The method steps of being processed into sustained-release injections are the same as in Example 1, but the difference is that the antibacterial active ingredients and their weight percentages are: 2-50% paromomycin, dibekacin, ribomycin, carbane Namycin, kanamycin B, amikacin B, dideoxykanamycin B, amikacin, rivamycin, tilmicosin, netilmicin , Tobramycin, Sisomicin, Etimicin, Penicillin A, Gentamicin, Vertimicin, Doxycycline, Small Normicin, Isopamicin, Isopamicin, Tylosin, Virginmycin, Salinomycin, Flavomycin, Tylomycin, Telosin, Virginmycin, Hiduramycin, Sisomycin, Lidamycin, Fluoride Benicol, rifaximin, or daptomycin.

Embodiment 3

[0102] 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 paromomycin, 30mg dibekacin, 30mg ribomycin respectively in three containers, shake up again and use spray-drying method to prepare containing 30% paromomycin, 30% dibekacin, 30 % Ribomycin 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 500cp-650cp (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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Abstract

The present invention relates to a slow-released injection containing aminoglycoside antibiotics. It composed of slow-released microsphere and solvent. Said slow-released microsphere contains slow-released auxiliary material and aminoglycoside antibiotics, and 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 gelatin, etc. The slow-released microsphere also can be made into slow-released implant preparation and ointment preparation. 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 injection containing aminoglycoside antibiotics and an application thereof, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing aminoglycoside 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 lesion...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/7028A61K31/7034A61K31/7036A61K45/00A61K47/26A61K47/34A61P31/00A61P31/02
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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