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Sustained-release injection containing kanamycin

A slow-release injection and kanamycin technology, applied in the field of medicine, can solve the problems of difficulty in obtaining an effective bactericidal concentration, increase the dose and side effects, etc., and achieve the effects of facilitating drug application, reducing the course of treatment, and reducing drug tolerance.

Inactive Publication Date: 2008-10-08
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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PUM

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Abstract

The invention relates to a slow-released injection comprising kanamycin, which comprises a slow-released microsphere and a dissolvent; the slow-released microsphere comprises a slow-release adjuvant and the aminoglycoside antibiotic; the dissolvent is the special dissolvent which comprises a suspending agent such as sodium carboxymethylcellulose, etc., and the viscosity of which is 100cp-3000cp (at 20 DEG C-30 DEC C); the slow-release adjuvant can be selected from EVAc, polifeprosan, PLA, PLGA, sebacic acid copolymer, albumen glue and gelatin, etc.; the slow-released microsphere also can be made into a slow-released implant and an ointment. The slow-released implant and the slow-released injection can be partially placed or injected in a bacterial focus to release locally and slowly for more than 5-30 days, thereby obviously reducing the toxicity of the entire body while getting and maintaining a valid medicine density in the local focus effectively. The slow-released injection comprising the kanamycin of the invention has obvious special treatment effect for focus of local infection such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot, osteonecrosis of femoral head and various abscesses, etc., caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococcus and meningococcus, etc.

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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K31/7036A61K47/30A61P31/04
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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