Slow release agent containing aminoglycosides antibiotic and its uses

An aminoglycoside, antibiotic technology, applied in the field of medicine, can solve the problems of increasing the dose and side effects, difficult to obtain an effective bactericidal concentration, etc., and achieves the effects of reducing the course of treatment, facilitating the application of drugs, and reducing costs

Inactive Publication Date: 2006-10-11
SHANDONG LANJIN PHARMA +1
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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, especia

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] 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

[0102] 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

[0104] 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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PUM

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Abstract

The invention relates to a slow-releasing agent of antibiotics containing aminoglycoside, comprising slow-releasing micro-sphere containing slow-releasing findings and aminoglycoside antibiotics, and special dissolvent containing suspending adjuvant agent such as sodium carboxymethyl cellulose with the adhesive degree being 100cp-3000cp (at 20-30 Deg. C). The slow-releasing findings comprises EVAc, polyphenyl, PLA, PLGA, decanedioic acid copolymer, albumen glue and gelatin; the slow-releasing micro-sphere can be produced to slow-releasing implanting agent and unguent agent. When the slow-releasing implanting agent and injection is placed or injected into bacteria, the medicine can be released slowly for more than 5-30 days, and toxicity is dramatically reduced at the same time when effective medicine concentration is got and maintained. The said slow-releasing agent is specially effective for chronic medullitis, bedsore, intractable ulcer on skin, diabetes femoral head necrosis and other abscessus, which are caused by Staphylococcus, Streptococcus, Streptococcus, acne Propionibacteriaceae, Enterobacter, Enterobacter, gonotoxin or parameningococcus.

Description

(1) Technical field [0001] The invention relates to a sustained release agent 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 lesions wi...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/7052A61P3/02
Inventor 孔庆忠俞建江苏红清
Owner SHANDONG LANJIN PHARMA
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